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GABAA

" in MedChemExpress (MCE) Product Catalog:

225

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1

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1

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6

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39

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8

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22

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3

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-133486

    GABA Receptor Neurological Disease
    GABAA receptor agent 1 is a high affinity ligand for GABAA receptor, with potent anticonvulsant activity .
    GABAA receptor agent 1
  • HY-109572

    GABA Receptor Neurological Disease
    GABAA receptor module-4 (9eey) is a GABAA receptor modulator that can be used in the study of central nervous system diseases .
    GABAA receptor modular-4
  • HY-135482

    GABA Receptor Neurological Disease
    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) .
    GABAA receptor agent 2 TFA
  • HY-145258

    GABA Receptor Neurological Disease
    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 .
    GABAA receptor agent 6
  • HY-147736

    GABA Receptor Neurological Disease
    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 .
    GABAA receptor agonist 2
  • HY-147735

    GABA Receptor Neurological Disease
    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 .
    GABAA receptor agonist 1
  • HY-146100

    GABA Receptor Neurological Disease
    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 .
    GABAA receptor agent 8
  • HY-146099

    GABA Receptor Neurological Disease
    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 .
    GABAA receptor agent 7
  • HY-161784

    GABA Receptor Neurological Disease
    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 .
    GABAA receptor modular-3
  • HY-145256

    GABA Receptor Neurological Disease
    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 .
    GABAA receptor agent 4
  • HY-147657

    GABA Receptor Neurological Disease
    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 .
    GABAA receptor modulator-2
  • HY-103513

    Others Others
    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.
    GABAA receptor agent 2
  • HY-145257

    GABA Receptor Neurological Disease
    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 .
    GABAA receptor agent 5
  • HY-103501

    GABA Receptor Neurological Disease
    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 .
    SB-205384
  • HY-116813

    GABA Receptor Neurological Disease
    ZK 93423 is a potent benzodiazepine GABAA receptor agonist with a certain cooling effect on rodents .
    ZK 93423
  • HY-147421

    GABA Receptor Neurological Disease
    Xilmenolone is a GABAA receptor positive allosteric modulator .
    Xilmenolone
  • HY-B1494
    Picrotoxinin
    3 Publications Verification

    Chloride Channel GABA Receptor Neurological Disease
    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 .
    Picrotoxinin
  • HY-116622

    L-822179

    GABA Receptor Neurological Disease
    α5IA (L-822179) is a selective α5 GABAA receptor inverse agonist with neuroprotective potential .
    α5IA
  • HY-B1494R

    Chloride Channel GABA Receptor Neurological Disease
    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 .
    Picrotoxinin (Standard)
  • HY-N10884

    Others Others
    Withasomniferolide A is a withanolide, isolated from a GABAA receptor positive activator methanol extract of the roots of Withania somnifera .
    Withasomniferolide A
  • HY-103524
    Valerenic acid
    1 Publications Verification

    (-)-Valerenic Acid

    GABA Receptor 5-HT Receptor Neurological Disease
    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 .
    Valerenic acid
  • HY-129408

    GABA Receptor Neurological Disease
    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 .
    SGE-516
  • HY-113346

    Tetrahydro-11-deoxycorticosterone

    GABA Receptor Endogenous Metabolite Neurological Disease
    Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .
    Tetrahydrodeoxycorticosterone
  • HY-103524R

    (-)-Valerenic Acid (Standard)

    5-HT Receptor GABA Receptor Neurological Disease
    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 .
    Valerenic acid (Standard)
  • HY-103535

    GABA Receptor Neurological Disease
    GBLD345, a nonbenzodiazepine anxiolytic agent, is a non- selective, potent GABAA receptor positive allosteric modulator (PAM) .
    GBLD345
  • 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 .
    Propanidid
  • HY-124030

    Drug Metabolite Neurological Disease
    3-Hydroxyphenazepam is an active metabolite of Cinazepam. Cinazepam is a GABAA receptor agonist. 3-Hydroxyphenazepam can inhibit synaptosomal transporter-mediated [ 3H]GABA uptake .
    3-Hydroxyphenazepam
  • HY-124463

    5α,3β-THDOC

    GABA Receptor iGluR Neurological Disease
    Epiallopregnanolone (5α,3β-THDOC), a 3β-hydroxy neurosteroid, an antagonist at GABAA receptors and a NMDA receptor enhancer .
    Epiallopregnanolone
  • HY-115854

    Others Neurological Disease
    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 .
    Ro 15-1310
  • HY-16716
    Basmisanil
    1 Publications Verification

    RG1662; RO5186582

    GABA Receptor Neurological Disease
    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 .
    Basmisanil
  • HY-N10887

    GABA Receptor Neurological Disease
    Withasomniferolide B is a withanolide. Withasomniferolide B can be isolated from a GABAA receptor positive activator methanol extract of the roots of Withania somnifera .
    Withasomniferolide B
  • HY-120837

    GABA Receptor Neurological Disease
    PZ-II-029 is a GABAA positive allosteric modulator that selectively binds with high affinity to α6β3γ2. PZ-II-029 shows anti-migraine effects .
    PZ-II-029
  • HY-100991

    ZK 39106; LSU-65

    GABA Receptor Neurological Disease
    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 .
    FG 7142
  • 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 .
    (S)-Norzopiclone
  • 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 .
    Chlorothymol
  • HY-133596

    Potassium Channel GABA Receptor Neurological Disease
    12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca 2+-activated K + (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive GABAA antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca 2+ and stimulates transmitter release .
    12,14-Dichlorodehydroabietic acid
  • HY-N2080

    GABA Receptor Cancer
    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) .
    Songorine
  • HY-100369A

    GABA Receptor Neurological Disease
    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 .
    DMCM hydrochloride
  • HY-N0301

    GABA Receptor 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 .
    Thiocolchicoside
  • HY-10233
    Gaboxadol hydrochloride
    1 Publications Verification

    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 .
    Gaboxadol hydrochloride
  • HY-107782

    GABA Receptor Neurological Disease
    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 .
    Picrotin
  • 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 .
    2'MeO6MF
  • 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 .
    Thiocolchicoside (Standard)
  • HY-107782R

    GABA Receptor Neurological Disease
    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 .
    Picrotin (Standard)
  • HY-106851

    FG 10571; PNU 78875

    GABA Receptor Neurological Disease
    Panadiplon (FG 10571; PNU 78875), a benzodiazepine receptor, is a 5GABAA partial agonist. Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors .
    Panadiplon
  • HY-19308

    GABA Receptor Neurological Disease
    RWJ-51204 is a partial agonist of GABA(A) receptor, with Ki of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.
    RWJ-51204
  • 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 .
    MmTx1 toxin
  • HY-100370

    GABA Receptor Cancer
    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.
    MRK-016
  • 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 .
    PF-06372865
  • HY-129927

    Others Others
    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.
    Thiomuscimol

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