Search Result
Results for "
GABAA receptors
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
3
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-B1494
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Chloride Channel
GABA Receptor
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Neurological Disease
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Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM .
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- HY-109572
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- HY-103501
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GABA Receptor
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Neurological Disease
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SB-205384 is a GABAA receptor modulator. The primary effect of SB-205384 on GABAA-activated currents is a prolonged response decay half-life upon removal of the agonist .
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- HY-147421
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- HY-124534
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GABA Receptor
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Neurological Disease
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(1S,3R)-3-Aminocyclopentane carboxylic acid has GABAA receptor activity, but it doesn't show significant activity in inhibiting neuronal GABA uptake .
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- HY-B1494R
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Chloride Channel
GABA Receptor
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Neurological Disease
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Picrotoxinin (Standard) is the analytical standard of Picrotoxinin. This product is intended for research and analytical applications. Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM .
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- HY-124463
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- HY-103535
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- HY-124030
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Drug Metabolite
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Neurological Disease
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3-Hydroxyphenazepam is an active metabolite of Cinazepam. Cinazepam is a GABAA receptor agonist. 3-Hydroxyphenazepam can inhibit synaptosomal transporter-mediated [ 3H]GABA uptake .
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- HY-115854
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GABA Receptor
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Neurological Disease
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Ro 15-1310 is an imidazobenzodiazepine that exhibits high affinity and selectivity for alpha 5-containing GABAA receptors. Ro 15-1310 is promising for research of convulsions .
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- HY-N10887
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GABA Receptor
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Neurological Disease
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Withasomniferolide B is a withanolide. Withasomniferolide B can be isolated from a GABAA receptor positive activator methanol extract of the roots of Withania somnifera .
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- HY-A0134
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GABA Receptor
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Neurological Disease
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Isoflurane is a volatile general anaesthetic used for induction and maintenance of general anesthesia. Isoflurane binds to and enhances GABAA receptor. Isoflurane inhibits electron transfer in respiratory complex I .
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- HY-16716
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RG1662; RO5186582
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GABA Receptor
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Neurological Disease
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Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders .
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- HY-107782
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GABA Receptor
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Neurological Disease
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Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs with IC50 values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission .
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- HY-100991
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ZK 39106; LSU-65
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GABA Receptor
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Neurological Disease
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FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of?β-adrenoceptors in mouse cerebral cortex .
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- HY-100369A
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GABA Receptor
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Neurological Disease
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DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 ?receptors, respectively .
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- HY-107782R
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GABA Receptor
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Neurological Disease
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Picrotin (Standard) is the analytical standard of Picrotin. This product is intended for research and analytical applications. Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs with IC50 values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission .
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- HY-N2080
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GABA Receptor
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Cancer
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Songorine is a diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a GABAA receptor antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC) .
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- HY-145258
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GABA Receptor
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Neurological Disease
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GABAA receptor agent 6 (compound 2027) is a potent γ-GABAAR antagonist with an Ki of 0.56 µM. GABAA receptor agent 6 shows γ-GABAAR antagonist activity with low cellular membrane permeability .
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- HY-147736
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GABA Receptor
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Neurological Disease
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GABAA receptor agonist 2 (compound 4c) is a potent GABAA receptor agonist. GABAA receptor agonist 2 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 2 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 2 has the potential for the research of depression .
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- HY-147735
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GABA Receptor
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Neurological Disease
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GABAA receptor agonist 1 (compound 3e) is a potent GABAA receptor agonist. GABAA receptor agonist 1 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 1 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 1 has the potential for the research of depression .
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- HY-146100
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GABA Receptor
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Neurological Disease
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GABAA receptor agent 8 (compoud 5e) is a potent GABAA receptor positive modulator. GABAA receptor agent 8 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 8 has the potential for the research of epilepsy .
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- HY-146099
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GABA Receptor
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Neurological Disease
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GABAA receptor agent 7 (compoud 5c) is a potent GABAA receptor positive modulator. GABAA receptor agent 7 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 7 has the potential for the research of epilepsy .
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- HY-106851
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FG 10571; PNU 78875
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GABA Receptor
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Neurological Disease
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Panadiplon (FG 10571; PNU 78875), a benzodiazepine receptor, is a 5GABAA partial agonist. Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors .
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- HY-133486
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- HY-19308
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- HY-P5860
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Micrurotoxin 1
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GABA Receptor
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Neurological Disease
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MmTx1 toxin (Micrurotoxin 1) is an allosteric GABAA receptor modulator that increases GABAA receptor susceptibility to agonist .
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- HY-135482
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GABA Receptor
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Neurological Disease
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GABAA receptor agent 2 TFA is a potent and high-affinity GABAA receptor antagonist with an IC50 of 24 nM (human α1β2γ2 GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAA receptors). GABAA receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3) .
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- HY-145256
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GABA Receptor
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Neurological Disease
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GABAA receptor agent 4 (compound 1e) is a potent γ-GABAAR antagonist with an Ki of 0.18 µM. GABAA receptor agent 4 efficiently rescues inhibition of T cell proliferation. GABAA receptor agent 4 has the immunomodulatory potential .
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- HY-129927
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Others
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Others
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Thiomuscimol is a GABAA receptor agonist (IC50=19 nM). It has been used as a photoaffinity label for the purification and identification of GABA binding sites within the GABAA receptor complex.
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- HY-161784
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GABA Receptor
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Neurological Disease
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GABAA receptor modular-3 (Compound S28) is a modulator for (γ-aminobutyric acid)A receptor (GABAA receptor), with EC50 of 56 nM and 10 nM, for α1β2γ2 and α4β3δ subtype. GABAA receptor modular-3 exhibits good pharmacokinetic characteristics in rats. GABAA receptor modular-3 is slightly toxic toxicity in rats with a loss of rollover reflex (LORR) threshold dose of 23.3 μmol/kg, and exhibits potential ameliorating the postpartum depression .
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- HY-103513
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GABA Receptor
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Others
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GABAA receptor agent 2 (compound 13) is a compound used to study the structure and orthosteric ligand binding of GABA(A) receptors. The relevant model of GABAA receptor agent 2 can be used to understand the details of orthosteric ligand binding, and a detailed binding mode hypothesis was created through structure-activity relationships with two homologous series of orthosteric GABA(A)R antagonists.
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- HY-Y1176
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- HY-117257
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- HY-19250
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- HY-100686
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GABA Receptor
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Neurological Disease
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U93631 is a GABAA receptor ligand of novel chemical structure with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors.
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- HY-145257
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GABA Receptor
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Neurological Disease
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GABAA receptor agent 5 (compound 018) is a potent γ-GABAAR antagonist with an Ki of 0.020 µM. GABAA receptor agent 5 shows γ-GABAAR antagonist activity with low cellular membrane permeability .
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- HY-114871
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GABA Receptor
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Neurological Disease
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SL651498 is a full agonist of α2 and α3 GABAA receptors, and a partial agonist of α1 and α5 GABAA receptors. SL651498 shows anxiolytic and anticonvulsant activities .
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- HY-103533
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- HY-N2079
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- HY-N6628
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- HY-117256
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- HY-11048
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NS11394
3 Publications Verification
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GABA Receptor
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Neurological Disease
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NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABAA-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties .
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- HY-B0009
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- HY-B0799
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Ergoloid mesylates
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GABA Receptor
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Neurological Disease
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Dihydroergotoxine mesylate is a series of alkaloid salt mixtures with high binding activity to GABAA receptors.
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- HY-118844
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- HY-159826
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- HY-123249
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GABA Receptor
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Neurological Disease
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HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects . HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-P5857
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Micrurotoxin 2
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GABA Receptor
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Neurological Disease
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MmTx2 toxin is a GABAA receptor modulator that enhances GABAA receptor sensitivity to agonists. MmTx2 toxin can be obtained from venom of coral snake. MmTx2 toxin can be used in the study of neurological diseases such as epilepsy, schizophrenia and chronic pain .
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- HY-W015793
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GABA Receptor
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Others
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6-Aminonicotinic acid is a GABAA receptor agonist with Ki value of 4.4 nM .
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- HY-153584
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GABA Receptor
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Neurological Disease
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MRK-898 is an orally active GABA(A) receptor modulator. MRK-898 binds to α1, α2, α3 or α5 subunit of GABA(A) receptor with Ki values of 1.2 nM, 1.0 nM, 0.73 nM, and 0.50 nM, respectively. However, α1-containing GABA(A) receptors are identified as the "sedative" and α2- and/or α3-containing receptors as the "anxiolytic" subtype(s) .
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- HY-101639
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- HY-N6648
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GABA Receptor
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Neurological Disease
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Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors, with antidepressant, anxiolytic and antinociceptive activities.
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- HY-101639A
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- HY-129105A
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Others
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Neurological Disease
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Chlormethiazole (edisylate) is a sedative-hypnotic with active allosteric modulatory activity at GABAA receptors .
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- HY-121393
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GABA Receptor
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Neurological Disease
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Imidazenil is a partial positive allosteric modulator of GABAA receptors with anxiolytic, antipanic and anticonvulsant activities.
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- HY-147657
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GABA Receptor
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Neurological Disease
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GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABAAR negative allosteric modulator (NAM) with a Ki of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety .
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- HY-103524
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(-)-Valerenic Acid
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GABA Receptor
5-HT Receptor
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Neurological Disease
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Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABAA receptors. Valerenic acid is also a partial agonist of the 5-HT5a receptor. Valerenic acid mediates anxiolytic activity via GABAA receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties .
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- HY-Y1683
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Racementhol
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GABA Receptor
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Others
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DL-Menthol is a relative configuration of (-)-Menthol. DL-Menthol relates to the activation of GABAA receptor .
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- HY-116813
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- HY-P5964
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- HY-116564
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Parasite
GABA Receptor
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Infection
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Lotilaner is a parasiticide, acts as a potent non-competitive antagonist of insects GABACl receptors, with an IC50 of 23.84 nM for Drosophila melanogaster GABA receptor. No effect on a dog GABAA receptor .
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- HY-N10884
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Others
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Others
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Withasomniferolide A is a withanolide, isolated from a GABAA receptor positive activator methanol extract of the roots of Withania somnifera .
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- HY-P5964A
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- HY-101665
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(+)-RP-59037; IP-456; RP-62955
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GABA Receptor
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Neurological Disease
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Pagoclone is an active (+)-enantiomer of the racemate RP 59037. Pagoclone is a partial GABA(A) receptor agonist used for the treatment of panic and anxiety disorders.
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- HY-124467
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- HY-123426
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GABA Receptor
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JY-XHe-053 is a potent and selective agonist of GABAA receptors containing the α5 subunit (Kis of 22.0 nM, 12.3 nM, 34.9 nM, 0.7 nM for α1, α2, α3, α5, respectively). JY-XHe-053 lacks significant anti-anxiety activity, despite its efficacy at α2- and α3-GABAA receptors .
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- HY-139145
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Trimethylopropane phosphate
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GABA Receptor
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Neurological Disease
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Etbicyphat (Trimethylopropane phosphate) is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors .
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- HY-B0649
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- HY-100370
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GABA Receptor
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Cancer
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MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77?and 1.4?nM for human?GABAA?α1β3γ2, GABAA?α2β3γ2, GABAA?α3β3γ2, and GABAA?α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
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- HY-103524R
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(-)-Valerenic Acid (Standard)
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5-HT Receptor
GABA Receptor
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Neurological Disease
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Valerenic acid (Standard) is the analytical standard of Valerenic acid. This product is intended for research and analytical applications. Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABAA receptors. Valerenic acid is also a partial agonist of the 5-HT5a receptor. Valerenic acid mediates anxiolytic activity via GABAA receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties .
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- HY-120970
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Cholinesterase (ChE)
GABA Receptor
iGluR
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Neurological Disease
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Bis(7)-tacrine dihydrochloride is a dimeric AChE inhibitor derived from tacrine. Bis(7)-tacrine dihydrochloride prevents glutamate-induced neuronal apoptosis by blocking NMDA receptors. Bis(7)-tacrine dihydrochloride is a potent GABAAreceptor antagonist. Bis(7)-tacrine dihydrochloride has the potential for the research of Alzheimer's disease .
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- HY-121877
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Valmethamide
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GABA Receptor
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Neurological Disease
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Valnoctamide (Valmethamide), a derivative of valproate, suppresses benzodiazepine-refractory status epilepticus. Valnoctamide (Valmethamide) acts directly on GABAA receptors .
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- HY-113346
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Tetrahydro-11-deoxycorticosterone
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GABA Receptor
Endogenous Metabolite
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Neurological Disease
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Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .
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- HY-103498
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GABA Receptor
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Neurological Disease
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Org20599 is a positive allosteric modulator and at higher concentrations direct agonist of GABAA receptor with an EC50 of 1.1 μM .
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- HY-N2338
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Cholesteryl myristate; Cholesteryl tetradecanoate
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nAChR
GABA Receptor
Potassium Channel
Endogenous Metabolite
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Cancer
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Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, GABAA receptor, and the inward-rectifier potassium ion channel.
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- HY-19872
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- HY-14426
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- HY-W001692
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DOV 273547
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GABA Receptor
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Neurological Disease
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Ocinaplon (DOV 273547) is a partial GABAA receptor positive allosteric modulator with relatively high efficacy at the α1 subunit .
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- HY-160189
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- HY-B0007B
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GABA Receptor
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Neurological Disease
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(S)-Baclofen is a selective GABAB receptor agonist with the IC50 values of 1.77 μM and 1564 μM for GABAB and GABAA, respectively .
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- HY-N6630
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- HY-112426
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- HY-116622
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- HY-111298
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GABA Receptor
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Neurological Disease
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TG 41 is positive modulator of GABAA receptor. TG 41 enhances the binding both of GABA and of Flunitrazepam to rat cerebral cortical membranes .
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- HY-103526
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GABA Receptor
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Neurological Disease
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DPNI-GABA is a nitroindoline cage compound that inhibits GABA(A) receptors and reduces GABA-evoked peak responses with an IC50 value of 0.5 mM .
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- HY-103497
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- HY-N2079R
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GABA Receptor
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Neurological Disease
Cancer
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(-)-Securinine (Standard) is the analytical standard of (-)-Securinine. This product is intended for research and analytical applications. (-)-Securinine is plant-derived alkaloid and also a GABAA receptor antagonist.
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- HY-120276
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GR3027
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GABA Receptor
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Neurological Disease
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Golexanolone is a GABAA receptor modulating steroid antagonist. Golexanolone reduces peripheral inflammation and neuroinflammation and improves cognitive and motor function in hyperammonemic rats .
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- HY-108204
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THRX 918661
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Others
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Others
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AZD 3043 (THRX 918661) is a positive allosteric modulator of GABA(A) receptors with sedative and hypnotic activity. AZD 3043 can enhance GABA(A) receptor-mediated chloride currents in vitro and produce hypnotic and electroencephalographic inhibitory effects in vivo. Due to its esterase-dependent metabolic pathway, it has a short duration of action and can be quickly cleared even after long-term infusion, which may have clinical application potential.
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- HY-105272
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R 72063
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GABA Receptor
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Neurological Disease
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Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors .
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- HY-105272A
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R 72063 hydrochloride
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GABA Receptor
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Neurological Disease
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Loreclezole hydrochloride, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors .
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- HY-13694
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- HY-101869
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MRK-409
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GABA Receptor
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Neurological Disease
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MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic .
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- HY-132806
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RG-7816; RO-7017773
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GABA Receptor
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Neurological Disease
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Alogabat (example 8) is a GABAA α5 receptor positive allosteric modulators (PAMs) (extracted from patent WO2018104419A1) .
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- HY-B0009R
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GABA Receptor
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Neurological Disease
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Flumazenil (Standard) is the analytical standard of Flumazenil. This product is intended for research and analytical applications. Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
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- HY-118844R
-
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GABA Receptor
Drug Metabolite
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Neurological Disease
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Flumazenil acid (Standard) is the analytical standard of Flumazenil acid. This product is intended for research and analytical applications. Flumazenil acid is a metabolite of Flumazenil . Flumazenil is a GABAA receptor antagonist .
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- HY-W013150
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- HY-123489
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THDOC
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GABA Receptor
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Neurological Disease
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3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
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- HY-139145S
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Trimethylopropane phosphate-13C3
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GABA Receptor
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Neurological Disease
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Etbicyphat- 13C3 is the 13C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors[1][2].
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- HY-19371
-
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GABA Receptor
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Neurological Disease
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Lorediplon is a novel non-benzodiazepine drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.
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- HY-14758
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NG2-73
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GABA Receptor
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Neurological Disease
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Adipiplon (NG2-73) is a selective GABAA receptor positive allosteric modulator. Adipiplon is particularly useful in the research of a variety of central nervous system (CNS) disorders.
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- HY-100799
-
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GABA Receptor
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Neurological Disease
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ZAPA sulfate is an agonist at low affinity GABAA-receptors. ZAPA sulfate induces membrane hyperpolarization of the Ascaris muscle cell with an EC50 of 10.3 μM .
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- HY-129408
-
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GABA Receptor
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Neurological Disease
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SGE-516 is a neuroactive steroid that is a potent positive allosteric modulator of synaptic and extra-synaptic GABAA receptors. SGE-516 has anticonvulsant activity .
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- HY-106965
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GABA Receptor
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Neurological Disease
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Org 21465 is an agent that can relieve pain. Org 21465 causes no cardiovascular or respiratory depression. Org 21465 can inhibit GABAA receptor in vivo .
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- HY-N0067
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4-Aminobutyric acid
|
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system .
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-
- HY-103511
-
|
GABA Receptor
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Neurological Disease
|
TCS1105 is a benzodiazepine ligand with agonist for α2-subunit containing GABAA receptors and antagonist for α1-subunit containing GABAA receptors. TCS1105 reduces anxiety-like behavior in mice. TCS1105 enhances offensive behavior and social dominance. TCS1105 blocks Sema3A induced AGC (axonal growth cones) collapse in a concentration-dependent fashion .
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-
- HY-B1240
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Dehydrobenzperidol
|
Dopamine Receptor
GABA Receptor
nAChR
|
Neurological Disease
|
Droperidol (Dehydrobenzperidol) is a butyrophenone pamine-2 receptor antagonist that inhibits the activation of GABA(A) and neuronal nicotinic receptors (nAChR), with IC50 values of 12.6 nM and 5.8 μM. Droperidol has anesthetic and sedative properties .
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-
- HY-N0301
-
|
GABA Receptor
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Neurological Disease
Inflammation/Immunology
|
Thiocolchicoside is a competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties .
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-
- HY-10232
-
THIP
1 Publications Verification
Gaboxadol
|
GABA Receptor
|
Neurological Disease
|
THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 µM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders .
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-
- HY-Y0313
-
-
- HY-P1083
-
|
Dynamin
|
Neurological Disease
|
Dynamin inhibitory peptide competitively blocks binding of dynamin to amphiphysin, thus preventing endocytosis. Dynamin inhibitory peptide blocks the dopamine D3 effect on GABAA receptors .
|
-
- HY-N0067S3
-
4-Aminobutyric acid-13C4
|
Isotope-Labeled Compounds
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
γ-Aminobutyric acid- 13C4 is the 13C-labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
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-
- HY-N2096
-
|
GABA Receptor
|
Neurological Disease
|
Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor .
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-
- HY-B0649R
-
2,6-Diisopropylphenol (Standard)
|
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
Cancer
|
Propofol (Standard) is the analytical standard of Propofol. This product is intended for research and analytical applications. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic .
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-
- HY-P1083A
-
|
Dynamin
|
Neurological Disease
|
Dynamin inhibitory peptide TFA competitively blocks binding of dynamin to amphiphysin, thus preventing endocytosis. Dynamin inhibitory peptide TFA blocks the dopamine D3 effect on GABAA receptors .
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-
- HY-W025443
-
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Others
|
Others
|
6-(4-Methoxyphenyl)pyridazin-3-amine is an aminopyridazine derivative, and can be used for the synthesis of SR 95103. SR 95103 is a selective and competitive GABA-A receptor antagonist .
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-
- HY-114706
-
MDL-26479
|
GABA Receptor
|
Neurological Disease
|
Suritozole (MGL-26479) is a cognitive enhancer that acts as a partial inverse agonist of benzodiazepine receptor sites on GABAA ion channel complexes. Suritozole can be used in the study of neurodegenerative diseases .
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- HY-Y1683R
-
|
GABA Receptor
|
Others
|
DL-Menthol (Standard) is the analytical standard of DL-Menthol. This product is intended for research and analytical applications. DL-Menthol is a relative configuration of (-)-Menthol. DL-Menthol relates to the activation of GABAA receptor .
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-
- HY-100783
-
l-Bicuculline methobromide
|
GABA Receptor
|
Neurological Disease
|
(-)-Bicuculline methobromide (l-Bicuculline methobromide) is a potent GABAA receptor antagonist. (-)-Bicuculline methobromide blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons .
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-
- HY-100783A
-
d-Bicuculline methochloride
|
GABA Receptor
|
Neurological Disease
|
(+)-Bicuculline methochloride (l-Bicuculline methochloride) is a potent GABAA receptor antagonist. (+)-Bicuculline methochloride blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons .
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-
- HY-131941
-
|
GABA Receptor
|
Neurological Disease
|
SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface .
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-
- HY-113320
-
5β-Androsterone
|
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity . Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form .
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-
- HY-103510
-
|
GABA Receptor
|
Neurological Disease
|
TB-21007 is an inverse agonist of α5β3γ2 subunit-containing GABAA receptor with a Ki of 1.6 nM. TB-21007 enhanced spatial memory in rats .
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-
- HY-U00199A
-
(S)-N-Desmethyl zopiclone; SEP-174559
|
GABA Receptor
nAChR
iGluR
|
Neurological Disease
|
(S)-Norzopiclone ((S)-N-Desmethyl zopiclone; SEP-174559) is a metabolite of Zopiclone with anxiolytic and anticonvulsant effects. (S)-Norzopiclone has benzodiazepine-like actions at γ2-bearing subtypes of the GABAA receptor and inhibits nACh and NMDA receptors .
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-
- HY-116457
-
Sombrevin; Fabantol
|
GABA Receptor
|
Cardiovascular Disease
Neurological Disease
|
Propanidid (Sombrevin; Fabantol) is a γ-aminobutyric acid type A (GABAA) receptor agonist and a short-acting non-barbiturate general agent that can suppress or relieve pain. Propanidid can decrease the arterial pressure .
|
-
- HY-101359
-
|
GABA Receptor
|
Neurological Disease
|
TPMPA, a hybrid of isoguvacine and 3-APMPA, is the first selective antagonist for a GABAC receptor (KB = 2.1 μM), but not to interact with GABAA (KB = 320 μM) or GABAB receptors (EC50 = 500 μM). TPMPA has the potential for the research of suppressing orientation selectivity in ganglion cells .
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-
- HY-107790
-
|
DNA/RNA Synthesis
|
Neurological Disease
|
5-Methoxyflavone, belonged to Flavonoid family, is a DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. possess central nervous system (CNS) depressant effect mediated through the ionotropic GABAA receptors.
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-
- HY-N0301R
-
|
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
Thiocolchicoside (Standard) is the analytical standard of Thiocolchicoside. This product is intended for research and analytical applications. Thiocolchicoside is a competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties .
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-
- HY-N0067R
-
4-Aminobutyric acid (Standard)
|
Endogenous Metabolite
GABA Receptor
|
Neurological Disease
|
γ-Aminobutyric acid (Standard) is the analytical standard of γ-Aminobutyric acid. This product is intended for research and analytical applications. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system .
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-
- HY-100800
-
trans-4-Aminocrotonic acid
|
GABA Receptor
|
Neurological Disease
|
TACA (trans-4-Aminocrotonic acid) is a potent agonist of GABAA and GABAC receptors (KD= 0.6 μM). TACA also is GABA uptake inhibitor and substrate for GABA-T. TACA produces late biphasic responses in the MPG neurons .
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-
- HY-N2096R
-
|
GABA Receptor
|
Neurological Disease
|
Kavain (Standard) is the analytical standard of Kavain. This product is intended for research and analytical applications. Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor .
|
-
- HY-10061
-
AZD-3355
|
GABA Receptor
|
Metabolic Disease
|
Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
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-
- HY-10061B
-
AZD-3355 hydrochloride
|
GABA Receptor
|
Metabolic Disease
|
Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
|
-
- HY-Y0313S1
-
-
- HY-108295
-
CXB-722
|
GABA Receptor
|
Neurological Disease
|
Pivagabine (CXB 722) is a hydrophobic 4-aminobutyric acid derivative with neuromodulatory activity. Pivagabine penetrates the blood-brain barrier in rats. Pivagabine antagonizes the effects of foot shock on both GABAA receptor function and corticotropin-releasing factor (CRF) concentrations in rat brain .
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-
- HY-Y0313R
-
|
Endogenous Metabolite
GABA Receptor
|
Neurological Disease
|
p-Hydroxybenzaldehyde (Standard) is the analytical standard of p-Hydroxybenzaldehyde. This product is intended for research and analytical applications. p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
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-
- HY-10061A
-
AZD-3355 napadisylate
|
GABA Receptor
|
Metabolic Disease
|
Lesogaberan (AZD-3355) napadisylate is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan napadisylate for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
|
-
- HY-16579
-
HOE 36-801 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents .
|
-
- HY-16579A
-
HOE 36-801
|
GABA Receptor
|
Neurological Disease
|
Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents .
|
-
- HY-103528
-
Salicylidene salicylhydrazide
|
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
SCS (Salicylidene salicylhydrazide) is a potent, allosteric and selective inhibitor of β1-containing GABAA receptors with an IC50 of 32 nM against α2β1γ1θ by VIPR measurement. SCS is also a chelator of metal ions .
|
-
- HY-103522
-
|
GABA Receptor
|
Neurological Disease
|
AA29504 is a ethyl carbamate with γ-aminobutyric acid (GABAA(HY-L120) receptor activity. AA29504 inhibits the delivery of the neurotransmitter gamma-aminobutyric acid in the central nervous system. AA29504 can be used to research anxiety, insomnia and other neuropsychiatric diseases .
|
-
- HY-106437
-
|
GABA Receptor
|
Neurological Disease
|
ELB-139 is a progesterone analogue. ELB-139 is a GABAA receptor partial agonist. ELB-139 has anxiolytic and anticonvulsant activity. ELB-139 induces increase of extracellular 5-HT in the striatum and the medial prefrontal cortex of rats .
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-
- HY-105115
-
ZK 112119
|
GABA Receptor
|
Neurological Disease
|
Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of GABAA receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM. Abecarnil can be used for epilepsy research .
|
-
- HY-B0135
-
|
NKCC
GABA Receptor
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
Furosemide is a potent and orally active inhibitor of Na +/K +/2Cl -?(NKCC) cotransporter, NKCC1 and NKCC2 .?Furosemide is also a GABAA?receptors antagonist and displays 100-fold selectivity for?α6-containing receptors than?α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema .
|
-
- HY-B0135A
-
|
NKCC
GABA Receptor
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
Furosemide sodium is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2 . Furosemide sodium is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide sodium acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema .
|
-
- HY-103520
-
|
GABA Receptor
|
Neurological Disease
|
DS2 is a selective positive allosteric modulator of δ-GABAA receptor. DS2 selectively potentiates GABA responses mediated by α4β3δ receptor. DS2 does not enhance activity at α4β3γ2 and α1β3γ2 receptors. DS2 relieves pain and has the potential for sleep disorders research .
|
-
- HY-107717
-
|
iGluR
|
Neurological Disease
|
MNI-caged-NMDA is a light-sensitive amino acid with rapid release properties suitable for use in the study of fast synaptic receptor mechanisms. MNI-caged-NMDA shows metered release of NMDA receptors, inducing rapid and sustained receptor activation in cerebellar interneurons. MNI-caged-NMDA is able to achieve rapid transient responses and generate large inward currents by local laser photolysis. The use of MNI-caged-NMDA can effectively study neurotransmitter signaling and its inhibitory effects on GABA-A receptors .
|
-
- HY-100783B
-
(+)-Bicuculline methobromide; d-Bicuculline methobromide
|
GABA Receptor
|
Neurological Disease
|
Bicuculline methobromide is a selective GABAA Receptor antagonist with an IC50 value of 3 μM. Bicuculline methobromide induces clonic tonic convulsions in mammals and can also be used to block Ca 2+ activated potassium channels. Bicuculline methobromide can be used in studies of epilepsy and other related psychiatric disorders .
|
-
- HY-115857
-
|
Others
|
Neurological Disease
|
SH-053-S-CH3-2'F is a selective positive allosteric modulator that produces mild to partial agonistic activity at α(1) GABA(A) receptors. SH-053-S-CH3-2'F showed anxiety-relieving effects at a dose of 30 mg/kg. SH-053-S-CH3-2'F completely avoids the memory impairment commonly caused by benzodiazepine site agonists. SH-053-S-CH3-2'F shows strong selectivity at GABA(A) receptors, which could potentially be used to develop more selective anti-anxiety drugs .
|
-
- HY-115685
-
|
GABA Receptor
|
Neurological Disease
|
3-Methyl-GABA is a potent GABA aminotransferase activator. 3-Methyl-GABA can fit the binding pocket of GABAA receptor (GABAaR). 3-Methyl-GABA can activate L-glutamic acid decarboxylase (GAD). 3-Methyl-GABA has anticonvulsant activity .
|
-
- HY-169432
-
|
GABA Receptor
|
Neurological Disease
|
TET-13 is a positive allosteric modulator of GABAA receptor with an EC50 of 5.65 μM, lower than that of Etomidate (EC50: 9.29 μM). TET-13 shows potent anesthetic effects in both mice and rats (ED50: 0.48 mg/kg and 0.69 mg/kg, respectively) .
|
-
- HY-N6084
-
α-Lupulic acid
|
COX
GABA Receptor
Apoptosis
|
Cardiovascular Disease
|
Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABAA receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties .
|
-
- HY-N0219
-
Bicuculline
Maximum Cited Publications
23 Publications Verification
(+)-Bicuculline; d-Bicuculline
|
GABA Receptor
|
Neurological Disease
|
Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca 2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .
|
-
- HY-137790
-
(-)-Bicuculline methochloride; l-Bicuculline methochloride
|
GABA Receptor
|
Neurological Disease
|
Bicuculline ((+)-Bicuculline; d-Bicuculline) methochloride is a selective GABAA receptor antagonist with an IC50 value of 3 μM. Bicuculline methochloride induces clonic tonic convulsions in mammals and can also be used to block Ca 2+ activated potassium channels. Bicuculline methochloride can be used in studies of epilepsy and other related psychiatric disorders .
|
-
- HY-B1606
-
Chlorthymol; 6-Chlorothymol
|
GABA Receptor
Bacterial
|
Neurological Disease
Inflammation/Immunology
|
Chlorothymol (Chlorthymol) is a potent GABAA receptor subunit LGC-37 positive modulator. Chlorothymol is an effective anticonvulsant. Chlorothymol is protective in several mouse seizure assays, including the 6-Hz 44-mA model of pharmacoresistant seizures. Chlorothymol possess GABAergic, membrane-modifying, antioxidant and topical antiseptic properties .
|
-
- HY-162757
-
|
GABA Receptor
Sodium Channel
|
Neurological Disease
|
Anticonvulsant agent 5 (Compound 5c) exhibits high affinity for GABAA receptors and NaV1.3 receptors. Anticonvulsant agent 5 shows anticonvulsant efficacy in mice psychomotor epilepsy test with an ED50 of 107 mg/kg. Anticonvulsant agent 5 exhibits neuroprotective activity against Kainic acid (HY-N2309) with an IC50 of 113 μM. Anticonvulsant agent 5 is blood-brain barrier (BBB) penetrable .
|
-
- HY-131997
-
|
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABAA receptors. 2'MeO6MF has anxiolytic and psychomotor stabilizing properties. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response .
|
-
- HY-W012123
-
|
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
3,4,5-Trimethoxycinnamic acid is a phenylpropanoid isolated from the roots of Polygala tenuifolia
WILLD, with anti-stress effect, prolonging the sleeping time in animals . 3,4,5-Trimethoxycinnamic acid increases expression of GAD65 and γ-subunit of GABAA receptor, but shows no effect on the amounts of α-, β-subunits .
|
-
- HY-123840
-
|
GABA Receptor
|
Neurological Disease
|
MRK-623 (Compound 14k) is an orally active, high-affinity GABAA receptor agonist, with the Ki values of 0.85 nM, 3.7 nM, 4.0 nM, and 0.53 nM for α1, α2, α3, and α5, respectively. MRK-623 shows anxiolytic effect .
|
-
- HY-111136
-
|
GABA Receptor
5-HT Receptor
Dopamine Receptor
Histamine Receptor
|
Neurological Disease
|
BL-1020 mesylate is the mesylate salt form of BL-1020. BL-1020 mesylate is an antipsychotic agent. BL-1020 mesylate is inhibitor for dopamine receptor and serotonin receptor (5-HT receptor), with Ki of 0.066, 0.062 and 0.21 nM, for D2L, D2S and 5-HT2A receptors, respectively. BL-1020 mesylate is agonist for GABAA receptor with Ki of 3.74 μM, and enhances the GABA release. BL-1020 mesylate exhibits high affinity with histamine receptor (Ki is 0.47 nM). BL-1020 mesylate reduces Amphetamine-induced hyperactivity, with lower catalepsy and sedation. BL-1020 mesylate is blood-brain barrier penetrate .
|
-
- HY-B0135R
-
|
NKCC
GABA Receptor
|
Metabolic Disease
Cancer
|
Furosemide (Standard) is the analytical standard of Furosemide. This product is intended for research and analytical applications. Furosemide is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2 . Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema .
|
-
- HY-121299
-
mCPBG
|
5-HT Receptor
|
Neurological Disease
|
m-Chlorophenylbiguanide (mCPBG) is a potent high-affinity agonist of the 5-HT3 receptor, exhibiting an inhibitory effect on long-term potentiation (LTP) in the mossy fiber-CA3 system. mCPBG attenuates the magnitude of LTP at concentrations of 0.3-1 microM, demonstrating its role in modulating synaptic plasticity. Additionally, the impact of mCPBG on LTP is reversible by the GABAA receptor antagonist bicuculline, indicating a connection between its action and GABAergic neurotransmission.
|
-
- HY-W028263
-
-
- HY-16579AR
-
|
GABA Receptor
|
Neurological Disease
|
Etifoxine (Standard) is the analytical standard of Etifoxine. This product is intended for research and analytical applications. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents .
|
-
- HY-163855
-
|
Sodium Channel
GABA Receptor
|
Neurological Disease
|
KGP-25 is an inhibitor of voltage-gated sodium channel 1.8 (Nav1.8), which can be used for analgesia by targeting Nav1.8 in the peripheral nervous system (PNS). KGP-25 can also target γ-aminobutyric acid subtype A receptor (GABAA) in the central nervous system (CNS) for general anesthesia .
|
-
- HY-123801
-
GL-II-93
|
GABA Receptor
|
Others
|
MIDD0301 (GL-II-93) is an orally effective, anti-asthmatic positive allosteric modulator of GABAA receptor. MIDD0301 had no significant adverse immune reactions at repeated doses and was better than Prednisone (HY-B0214). MIDD0301 relaxes histamine contractions in guinea pig and human tracheal smooth muscle for the study of bronchial systolic diseases .
|
-
- HY-N8852
-
6-MeOF
|
GABA Receptor
|
Neurological Disease
|
6-Methoxyflavanone (6-MeOF) is an orally active flavonoid compound. 6-Methoxyflavanone has anxiolytic properties. 6-Methoxyflavanone targets unique sites on GABA-A receptors, different from traditional benzodiazepines. 6-Methoxyflavanone can be used to study anxiety disorders. 6-Methoxyflavanone readily crosses the blood brain barrier (BBB) .
|
-
- HY-19505
-
|
GABA Receptor
|
Neurological Disease
|
TPA-023B is a high-affinity and orally active GABAA receptor α2/α3 subtype (Kis of 0.73 nM/2 nM) partial agonist and a α1 subtype (Ki of 1.8 nM) antagonist. TPA-023B has non-sedating anxiolytic-like properties .
|
-
- HY-103474
-
(-)-Bicuculline methiodide; l-Bicuculline methiodide
|
GABA Receptor
|
Neurological Disease
|
Bicuculline methiodide is a potent GABA(A) receptors blocker. Bicuculline methiodide alters membrane properties and firing pattern. Bicuculline methiodide reduces the Apamin-sensitive afterhyperpolarization, while Apamin is a toxin isolated from bee venom to block small conductance Ca 2+ -activated K + channels. Bicuculline methiodide facilitates burst firing via blocking apamin-sensitive Ca 2+ -activated K + current .
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-
- HY-111052
-
|
GABA Receptor
Cytochrome P450
|
Neurological Disease
Inflammation/Immunology
|
AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes . AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro . AZD7325 has the potential for the investigation of anxiety and dravet syndrome . PAM: positive allosteric modulator.
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-
- HY-10233
-
Lu 02-030 hydrochloride; THIP hydrochloride
|
GABA Receptor
|
Neurological Disease
|
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 μM, a full agonist efficacy at α5 subunit (ED50=28-129 μM) and a superagonist efficacy at α4β3δ (ED50=6 μM). Gaboxadol hydrochloride is a non-opioid agent .
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- HY-B1803A
-
ICI 136753 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
Tracazolate (ICI 136753) hydrochloride is a potent GABAA receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC50=13.2 μM), α1β3γ2 (EC50=1.5 μM). Tracazolate hydrochloride has the potency (EC50) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity .
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- HY-N0219R
-
|
GABA Receptor
|
Neurological Disease
|
Bicuculline (Standard) is the analytical standard of Bicuculline. This product is intended for research and analytical applications. Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .
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- HY-105056
-
Ro 16-6028
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GABA Receptor
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Neurological Disease
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Bretazenil (Ro 16-6028) is a partial agonist at the gamma-aminobutyric acid A (GABAA) receptor-linked benzodiazepine site. Bretazenil is potent benzodiazepine examined, exhibiting an IC50 (concentration at which half-maximal inhibition of specific [35S]TBPS binding occurs) of 6.1 nM. Bretazenil shows an EC50 of 10 nM for recombinant α1β1γ2. Anticonvulsant effects .
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- HY-B1671
-
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GABA Receptor
Sodium Channel
Calcium Channel
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Neurological Disease
Metabolic Disease
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(+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na + and Ca 2+ channels . (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .
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- HY-117955
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WAY 141839; Co 2-6749
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GABA Receptor
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Neurological Disease
|
GMA-839 is a selective modulator of the γ-aminobutyric acid A receptor (GABAA) with an IC50 value of 230 nM. GMA-839 exhibits potent anxiolytic-like activity, demonstrating significant dose-dependent anxiolytic effects in animal models, with an effective oral dose of 1.6 mg/kg. Significant increases in punished responding were observed in squirrel monkeys and pigeons. GMA-839 shows promise for research in the field of anxiolytics .
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- HY-103476
-
|
GABA Receptor
|
Neurological Disease
|
Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR) . Ro15-4513 is a potent ethanol antagonist . Ro15-4513 has anti-anxiety effect . Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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-
- HY-110143
-
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Potassium Channel
|
Neurological Disease
|
CLP257 is a selective K +-Cl ? cotransporter KCC2 activator with an EC50 of 616 nM. CLP257 is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 restores impaired Cl ? transport in neurons with diminished KCC2 activity. CLP257 alleviates hypersensitivity in rats with neuropathic pain. CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally .
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-
- HY-100936
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SQ 20009; EHT 0202 hydrochloride
|
Phosphodiesterase (PDE)
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects .
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-
- HY-108584
-
BMS-204352
|
Potassium Channel
|
Neurological Disease
|
Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo .
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-
- HY-103512
-
|
GABA Receptor
|
Neurological Disease
|
TP003 is a non-selective benzodiazepine site agonist with EC50s of 20.3, 10.6, 3.24, 5.64 nM for α1β2γ2, α2β3γ2, α3β3γ2, α5β2γ2, respectively. TP003 induces anxiolysis via α2GABAA receptors .
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-
- HY-120874
-
|
GABA Receptor
|
Neurological Disease
|
PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy .
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-
- HY-130349
-
L-656,748
|
GABA Receptor
|
Infection
|
Emamectin B1a (L-656,748) is a semisynthetic derivative of avermectin B1a that binds to GABA receptors (Ki=17.6 nM in rat brain membranes) and enhances GABA responses. Emamectin B1a acitivates GABAA receptors α1β1γ2, α1β2γ2, and α1β3γ2 with IC50s of 57, 210, and 49.8 nM, respectively. Emamectin B1a also binds to glycine receptors, inhibiting glycine receptors with an IC50=218 nM in rat spinal cord. Emamectin B1a (1.067 ng/mL) caused 90% mortality of S. exigua larvae in foliar spray bioassays and topical application, making it more toxic than avermectin B1.
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-
- HY-120179
-
|
AAK1
|
Neurological Disease
|
LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 exhibits no significant activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors .
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-
- HY-120179A
-
|
AAK1
|
Neurological Disease
|
LP-922761 hydrate is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 hydrate also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 hydrate shows less activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors .
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-
- HY-B1671R
-
|
GABA Receptor
Sodium Channel
Calcium Channel
|
Neurological Disease
Metabolic Disease
|
(+)-Kavain (Standard) is the analytical standard of (+)-Kavain. This product is intended for research and analytical applications. (+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels . (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .
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-
- HY-W050162
-
TMCA
|
GABA Receptor
5-HT Receptor
|
Neurological Disease
|
(E)-3,4,5-Trimethoxycinnamic acid (TMCA) is a cinnamic acid substituted by multi-methoxy groups. (E)-3,4,5-Trimethoxycinnamic acid is an orally active and potent GABAA/BZ receptor agonist. (E)-3,4,5-Trimethoxycinnamic exhibits favourable binding affinity to 5-HT2C and 5-HT1A receptor, with IC50 values of 2.5 and 7.6 μM, respectively. (E)-3,4,5-Trimethoxycinnamic acid shows anticonvulsant and sedative activity. (E)-3,4,5-Trimethoxycinnamic acid can be used for the research of insomnia, headache and epilepsy .
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-
- HY-116152
-
Ciprofol; HSK3486
|
GABA Receptor
Sirtuin
Keap1-Nrf2
Apoptosis
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
Cipepofol (Ciprofol), a novel 2,6-disubstituted phenol derivative, is a positive allosteric modulator and direct agonist of the GABAA receptor. Cipepofol can cause the central nerve inhibition and promote sleep based on the structural modification of Propofol (HY-B0649). Cipepofol can activate the sirtuin1 (Sirt1)/Nrf2 pathway. Cipepofol protects the heart against Isoproterenol (ISO; HY-B0468)-induced myocardial infarction by reducing cardiac oxidative stress, inflammatory response and cardiomyocyte apoptosis .
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-
- HY-W009009
-
|
GABA Receptor
|
Neurological Disease
|
L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2 .
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-
- HY-W677042
-
5α-Androst-16-en-3α-ol
|
GABA Receptor
|
Neurological Disease
|
α-Androstenol (5α-Androst-16-en-3α-ol) is a steroid pheromone that has been found in boar testes and human male axillary sweat. α-Androstenol is also a positive modulator of GABAA receptors, which enhances GABA-activated currents in primary mouse cerebellar granule cells (EC50=0.4 μM). α-Androstenol decreases immobility time in the forced swim test and increases time spent in the open arms of the elevated plus maze in mice. α-Androstenol protects against seizures induced by Pentylenetetrazole or electroshock with anxiolytic-like activity in mice .
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-
- HY-N7110
-
|
Akt
ERK
JNK
GABA Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
6-Hydroxyflavone is an orally effective flavonoid compound. 6-Hydroxyflavone can inhibit LPS (HY-D1056) -induced NO production and has anti-inflammatory effects. 6-Hydroxyflavone promotes osteoblast differentiation by activating AKT, ERK 1/2 and JNK signaling pathways. 6-Hydroxyflavone has an inhibitory effect on bovine hemoglobin (BHb) glycosylation. 6-Hydroxyflavone has a kidney protective effect. In addition, 6-Hydroxyflavone enhances GABA-induced current through the Benzodiazepine sites of γ-aminobutyric acid (GABAA) receptors. 6-Hydroxyflavone shows a clear preference for α2 - and α3 - subtypes, which play an anti-anxiety role .
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-
- HY-117106
-
|
GABA Receptor
|
Others
|
PNU-107484A is a GABAA receptor ligand that exhibits target activity mechanisms dependent on α isoforms. In the α1β2γ2 subtype, PNU-107484A acts as a positive allosteric modulator, enhancing GABA-induced Cl - currents, while it inhibits the currents in the α3β2γ2 and α6β2γ2 subtypes. The half-maximal concentrations for the α1β2γ2, α3β2γ2, and α6β2γ2 subtypes are 3.1, 4.2, and 3.5 μM, respectively. PNU-107484A can be used as a probe to investigate the physiological roles of different α isoform subtypes .
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-
-
-
HY-L120
-
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152 compounds
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GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. There are two classes of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors), whereas GABAB receptors are G protein-coupled receptors (also known asmetabotropic receptors). GABA receptors are significant drug targets in the treatment of neuropsychiatric disorders such as epilepsy, insomnia, and anxiety, as well as in anesthesia in surgical operations.
MCE offers a unique collection of 152 GABA receptors inhibitors and activators, which is an efficient tool for neuropsychiatric disorders drugs discovery.
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Cat. No. |
Product Name |
Type |
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- HY-N2338
-
Cholesteryl myristate; Cholesteryl tetradecanoate
|
Drug Delivery
|
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, GABAA receptor, and the inward-rectifier potassium ion channel.
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P5964A
-
-
- HY-P1083
-
|
Dynamin
|
Neurological Disease
|
Dynamin inhibitory peptide competitively blocks binding of dynamin to amphiphysin, thus preventing endocytosis. Dynamin inhibitory peptide blocks the dopamine D3 effect on GABAA receptors .
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- HY-P5860
-
Micrurotoxin 1
|
GABA Receptor
|
Neurological Disease
|
MmTx1 toxin (Micrurotoxin 1) is an allosteric GABAA receptor modulator that increases GABAA receptor susceptibility to agonist .
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- HY-P5857
-
Micrurotoxin 2
|
GABA Receptor
|
Neurological Disease
|
MmTx2 toxin is a GABAA receptor modulator that enhances GABAA receptor sensitivity to agonists. MmTx2 toxin can be obtained from venom of coral snake. MmTx2 toxin can be used in the study of neurological diseases such as epilepsy, schizophrenia and chronic pain .
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- HY-P5964
-
-
- HY-P1083A
-
|
Dynamin
|
Neurological Disease
|
Dynamin inhibitory peptide TFA competitively blocks binding of dynamin to amphiphysin, thus preventing endocytosis. Dynamin inhibitory peptide TFA blocks the dopamine D3 effect on GABAA receptors .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-N0067S3
-
|
γ-Aminobutyric acid- 13C4 is the 13C-labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
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-
-
- HY-139145S
-
|
Etbicyphat- 13C3 is the 13C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors[1][2].
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-
-
- HY-Y0313S1
-
|
p-Hydroxybenzaldehyde- 13C is the 13C-labeled p-Hydroxybenzaldehyde. p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
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Cat. No. |
Product Name |
|
Classification |
-
- HY-103476
-
|
|
Azide
|
Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR) . Ro15-4513 is a potent ethanol antagonist . Ro15-4513 has anti-anxiety effect . Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-123249
-
|
|
Alkynes
|
HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects . HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-120276
-
GR3027
|
|
Alkynes
|
Golexanolone is a GABAA receptor modulating steroid antagonist. Golexanolone reduces peripheral inflammation and neuroinflammation and improves cognitive and motor function in hyperammonemic rats .
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Cat. No. |
Product Name |
|
Classification |
-
- HY-N2338
-
Cholesteryl myristate; Cholesteryl tetradecanoate
|
|
Cholesterol
|
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, GABAA receptor, and the inward-rectifier potassium ion channel.
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