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GABA A receptor agonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	GABA Receptor (42) 5-HT Receptor (2) Dopamine Receptor (1) Drug Metabolite (1) ERK (1) Histamine Receptor (1) iGluR (1) Isotope-Labeled Compounds (1)
By Research Areas:	Cardiovascular Disease (1) Metabolic Disease (3) Neurological Disease (43)

Inhibitors & Agonists

Screening Libraries

Isotope-Labeled Compounds

Targets Recommended: GABA Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-U00315

Gidazepam Gidasepam; Hidazepam; Hydazepam	GABA Receptor	Neurological Disease
Gidazepam is an agonist of GABA receptor channels (GABA RCs).

HY-100810

Isoguvacine hydrochloride 1 Publications Verification	GABA Receptor	Neurological Disease
Isoguvacine hydrochloride is a *GABA* receptor agonist.

HY-A0173

Progabide SL 76002	GABA Receptor	Neurological Disease
Progabide is a gamma-aminobutyric acid receptor (GABA) agonist.

HY-147736

GABAA receptor agonist 2	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 .

HY-147735

GABAA receptor agonist 1	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 .

HY-118259

L-663581 FG-8205	GABA Receptor	Neurological Disease
L-663581 (FG-8205) is an agonist of benzodiazepine receptor, acting as a partial agonist at GABA A receptor .

HY-19308

RWJ-51204	GABA Receptor	Neurological Disease
RWJ-51204 is a partial agonist of **GABA(A) receptor, with K_i** of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.

HY-103225

S-8510 phosphate SB-737552 phosphate	GABA Receptor	Neurological Disease
S-8510 (phosphate) is an inverse Benzodiazepine (BDZ) receptor agonist, with K_is of 34.6 nM, 36.2 nM for –GABA and +GABA respectively.

HY-108403

Phenibut β-Phenyl-GABA; 4-Amino-3-phenylbutanoic acid	GABA Receptor	Neurological Disease
Phenibut (β-Phenyl-GABA) is a *GABA-B* agonist . Phenibut acts as a GABA-mimetic, primarily at GABAB?receptors. Phenibut has anxiolytic and nootropic (cognition enhancing) effects .

HY-114685

S-8510 free base SB-737552 free base	GABA Receptor	Neurological Disease
S-8510 free base is an inverse Benzodiazepine (BDZ) receptor agonist, with K_is of 34.6 nM, 36.2 nM for –GABA and +GABA respectively.

HY-U00315S

Gidazepam-d5 Gidasepam-d₅; Hidazepam-d₅; Hydazepam-d₅	GABA Receptor	Neurological Disease
Gidazepam-d5 is a deuterium labeled Gidazepam. Gidazepam is an agonist of GABA receptor channels (GABA RCs), and has anticonvulsant effect .

HY-W041333

Phenibut hydrochloride β-Phenyl-GABA hydrochloride; 4-Amino-3-phenylbutanoic acid hydrochloride; 4-Amino-3-phenylbutyric acid hydrochloride	GABA Receptor	Neurological Disease
Phenibut (β-Phenyl-GABA) hydrochloride is an orally active *GABA-B* agonist . Phenibut hydrochloride acts as a GABA-mimetic, primarily at GABAB?receptors. Phenibut hydrochloride has anxiolytic and nootropic (cognition enhancing) effects .

HY-100124

Bamaluzole	GABA Receptor	Neurological Disease
Bamaluzole is a **GABA receptor** agonist extracted from patent WO 2012064642 A1.

HY-118490

T-2000 DMMDPB	GABA Receptor	Neurological Disease
T-2000 (DMMDPB) is an orally active **GABA receptor** agonist with anticonvulsant activities .

HY-14856

Atagabalin PD 0200390	GABA Receptor	Neurological Disease
Atagabalin (PD 0200390) is a selective *GABA* (gamma-aminobutyric acid) receptor agonist with antianxiety and sedative effects. Atagabalin enhances the activity of the *GABA* receptor by binding to the α2δ subunit of the *GABA* receptor, thereby increasing the *GABA* mediated inhibition. This enhancement results in reduced excitability of neurons, helping to reduce anxiety and improve sleep. Atagabalin can be used to study neuropsychiatric disorders, anxiety or sleep disorders .

HY-B1833

Afloqualone HQ-495	GABA Receptor	Neurological Disease
Afloqualone (HQ-495) is a GABAergic agent and has agonist activity at the β subtype of the GABAα receptor. Afloqualone has antivertiginous effects thought to be attributable to the increased sensitivity of GABA receptors of the LVN neuron site .

HY-106025

Radequinil AC-3933	GABA Receptor	Neurological Disease
Radequinil (AC-3933) is a benzodiazepine receptor (BzR) partial inverse agonist. AC-3933 binds to *GABA(-)* and GABA(+) ligand with K_is of 5.15 and 6.11 nM, respectively .

HY-101665

Pagoclone (+)-RP-59037; IP-456; RP-62955	GABA Receptor	Neurological Disease
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.

HY-106635

Suriclone RP31264	GABA Receptor	Neurological Disease
Suriclone (RP31264) is a **GABA receptor** agonist. Suriclone is an anxiolytic agent with a high affinity for the benzodiazepine receptors. Suriclone has oral activity .

HY-17030

Acamprosate calcium Calcium N-acetylhomotaurinate	GABA Receptor	Neurological Disease
Acamprosate calcium(Campral EC) is a GABA receptor agonist and modulator of glutamatergic systems; reduces alcohol consumption in animal models of alcohol addiction.

HY-129927

Thiomuscimol	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.

HY-115763

3-Aminopropylphosphinic acid 3-APPA; CGP 27492; CGA 147823	GABA Receptor	Neurological Disease
3-Aminopropylphosphinic acid (3-APPA) is a phosphonic analog of GABA. 3-Aminopropylphosphinic acid is a potent, selective GABA_B receptor agonist .

HY-B1833R

Afloqualone (Standard)	GABA Receptor	Neurological Disease
Afloqualone (Standard) is the analytical standard of Afloqualone. This product is intended for research and analytical applications. Afloqualone (HQ-495) is a GABAergic agent and has agonist activity at the β subtype of the?GABAα receptor. Afloqualone has antivertiginous effects thought to be attributable to the increased sensitivity of GABA receptors of the LVN neuron site .

HY-100800

TACA trans-4-Aminocrotonic acid	GABA Receptor	Neurological Disease
TACA (trans-4-Aminocrotonic acid) is a potent agonist of GABA_A and GABA_C receptors (K_D= 0.6 μM). TACA also is GABA uptake inhibitor and substrate for GABA-T. TACA produces late biphasic responses in the MPG neurons .

HY-17030S

Acamprosate-d3 calcium	GABA Receptor	Neurological Disease
Acamprosate-d₃ (calcium) is the deuterium labeled Acamprosate calcium. Acamprosate calcium is a GABA receptor agonist and modulator of glutamatergic systems[1][2].

HY-110233S

Acamprosate-d6 calcium	GABA Receptor	Neurological Disease
Acamprosate-d₆ (calcium) is the deuterium labeled Acamprosate calcium. Acamprosate calcium (Campral EC) is a GABA receptor agonist and modulator of glutamatergic systems[1].

HY-B0007

Baclofen Maximum Cited Publications 6 Publications Verification	GABA Receptor	Neurological Disease
Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic *GABA_B receptor* (GABA_BR)** agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABA_B receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research .

HY-B0007C

Baclofen hydrochloride	GABA Receptor	Neurological Disease
Baclofen hydrochloride, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic *GABA_B receptor* (GABA_BR)** agonist. Baclofen hydrochloride mimics the action of GABA and produces slow presynaptic inhibition through the GABA_B receptor. Baclofen hydrochloride has high blood brain barrier penetrance. Baclofen hydrochloride has the potential for muscle spasticity research .

HY-14856A

iso-Atagabalin hydrochloride iso-PD 0200390 hydrochloride	GABA Receptor	Others
iso-Atagabalin (iso-PD 0200390) hydrochloride is a stereoisomer of Atagabalin (HY-14856). Atagabalin is a selective GABA (gamma-aminobutyric acid) receptor agonist with antianxiety effect .

HY-124030

3-Hydroxyphenazepam	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 .

HY-125508

CCD-3693	GABA Receptor	Neurological Disease
CCD-3693 is an orally active *GABA* receptor agonist. CCD-3693 has anxiolytic, anticonvulsant and sedative hypnotic activities and can be used in research related to neurological diseases .

HY-B0007S

Baclofen-d4	GABA Receptor	Neurological Disease
Baclofen-d₄ is the deuterium labeled Baclofen. Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research[1][2][3].

HY-19006

ZK-91296	Others	Neurological Disease
ZK-91296 is a GABA receptor agonist with anxiolytic activity. ZK-91296 can reduce anxiety in animals without causing sedation. ZK-91296 may have pharmacological selectivity for interaction with specific types of benzodiazepine receptors .

HY-105627A

Profadol hydrochloride CI-572 hydrochloride	GABA Receptor iGluR	Cardiovascular Disease
Profadol (CI-572) hydrochloride is a potent analgesic agent. Profadol is a *µ-opioid receptor* (MOR)** agonist. Profadol hydrochloride activates the γ-aminobutyric acid (GABA) receptors and inhibits the N-methyl-D-aspartate (NMDA) receptor. Profadol increases the mRNA and protein expression of MOR .

HY-B0007R

Baclofen (Standard)	GABA Receptor	Neurological Disease
Baclofen (Standard) is the analytical standard of Baclofen. This product is intended for research and analytical applications. Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic *GABA_B receptor* (GABA_BR)** agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABA_B receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research .

HY-B0007S2

Baclofen-d5 hydrochloride	GABA Receptor Isotope-Labeled Compounds	Neurological Disease
Baclofen-d₅ hydrochloride is deuterated labeled Baclofen (HY-B0007). Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic *GABA_B receptor* (GABA_BR)** agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABA_B receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research .

HY-113726

Nerisopam GYKI52322; EGIS-6775	GABA Receptor	Neurological Disease
Nerisopam is an orally active gamma-aminobutyric acid (GABA) receptor agonist. Nerisopam is an anxiolytic and antipsychotic homophthalazine. Nerisopam induces rapid, intense expression of Fos-like immunoreactivity in the rostral, dorsomedial and lateral parts of the striatum in the rat .

HY-19438

Divaplon RU 32698	GABA Receptor	Neurological Disease
Divaplon is a *GABA* receptor agonist with the EC₅₀ values of 31 and 2 nM for α3β2γ2 and α5β2γ2, respectively. Divaplon shows anxiolytic activity .

HY-103133

WAY208466 dihydrochloride	5-HT Receptor	Neurological Disease
WAY 208466 dihydrochloride is a potent and selective 5-HT₆ receptor agonist (EC₅₀=7.3 nM for the human 5-HT₆ receptor). WAY-208466 dihydrochloride elevates cortical GABA levels in rat frontal cortex . WAY 208466 dihydrochloride exhibits antidepressant and anxiolytic-like effects .

HY-W050122

S-(+)-GABOB	Others	Neurological Disease
S-(+)-GABOB is an endogenous ligand with antiepileptic activity. S-(+)-GABOB is a metabolite of GABA and may function as a neurotransmitter. S-(+)-GABOB behaves as a full agonist when bound to the ρ(1) wild-type receptor. S-(+)-GABOB acts as a competitive antagonist in the ρ(1) T244S mutant receptor .

HY-10061

Lesogaberan AZD-3355	GABA Receptor	Metabolic Disease
Lesogaberan (AZD-3355) is a potent and selective GABA_B receptor agonist with an EC₅₀ of 8.6 nM for human recombinant GABA_B receptors. The affinity (K_is) of Lesogaberan for rat GABA_B and GABA_A 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 .

HY-10061B

Lesogaberan hydrochloride AZD-3355 hydrochloride	GABA Receptor	Metabolic Disease
Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABA_B receptor agonist with an EC₅₀ of 8.6 nM for human recombinant GABA_B receptor. The affinity (K_is) of Lesogaberan hydrochloride for rat GABA_B and GABA_A 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-114076

CGP55845	GABA Receptor	Neurological Disease
CGP55845 is a potent and selective GABAB receptor antagonist with activity that blocks agonist binding. The IC50 value of CGP55845 is 5 nM, indicating that it exhibits significant activity in inhibiting GABA and glutamate release. The apparent Kd of CGP55845 when forming a complex with the GABAB receptor is 30 nM, indicating its high affinity for this receptor. CGP55845 is as potent as 100 μM CGP 35348 in relieving the inhibitory effect of (R)-(-)-baclofen .

HY-10061A

Lesogaberan napadisylate AZD-3355 napadisylate	GABA Receptor	Metabolic Disease
Lesogaberan (AZD-3355) napadisylate is a potent and selective GABA_B receptor agonist with an EC₅₀ of 8.6 nM for human recombinant GABA_B receptors. The affinity (K_is) of Lesogaberan napadisylate for rat GABA_B and GABA_A 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-123525

COR628	Others	Neurological Disease
COR628 is a positive allosteric modulator of GABA(B) receptors with the activity of enhancing GABA-induced GTPγS stimulation. COR628 showed significant activity in in vitro studies but did not exhibit endogenous agonist activity. COR628 has shown efficacy in experiments in mice by enhancing the sedation/hypnosis induced by baclofen, shortening the onset time and extending the duration of loss of righting reflex when combined with non-sedating doses of baclofen . The cytotoxic effect of COR628 is comparable to or higher than that of GS39783 or BHF177 in concentration .

HY-115857

SH-053-S-CH3-2'F	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-129636

CLH304a (E)-GABAB receptor antagonist 1	GABA Receptor ERK	Neurological Disease
CLH304a (compound 14) is a specific and noncompetitive GABA_B receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC₅₀ of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABA_B receptor .

HY-111136

BL-1020 mesylate	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 K_i of 0.066, 0.062 and 0.21 nM, for D2L, D2S and 5-HT2A receptors, respectively. BL-1020 mesylate is agonist for GABA_A receptor with K_i of 3.74 μM, and enhances the GABA release. BL-1020 mesylate exhibits high affinity with histamine receptor (K_i 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-100991

FG 7142 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 (K_i=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 .

Cat. No.	Product Name

HY-L070

Neuroprotective Compound Library

1,213 compounds

Neurodegenerative diseases are characterised by progressive dysfunction and death of neurons, such as Alzheimer’s disease, Parkinson’s disease, and multiple sclerosis (MS). Neuroprotection is an approach to preserve neurons so that neurons cannot be hurt by different pathological factors in neurodegenerative diseases. Neuroprotectors are some agonists and antagonists targeting some key targets in neuroprotactive signal pathways, such as calcium and sodium channel blockers, GABA receptor agonists, NMDA receptor Antagonists, etc. Current neuroprotectors cannot reverse existing damage, but they may protect against further nerve damage and slow down any degeneration of the central nervous system (CNS) and still play important roles in the treatment of neurodegenerative diseases.

MCE offers a unique collection of 1,213 compounds with potential neuroprotective activities. These compounds mainly act on some key targets in neuroprotetive signal pathways, such as calcium channel, sodium channel, adenosine A1 receptor, etc. MCE Neuroprotective Compopund Library is a useful tool in neuroprotective drug discovery.

Cat. No.	Product Name	Chemical Structure

HY-U00315S

Gidazepam-d5
Gidazepam-d5 is a deuterium labeled Gidazepam. Gidazepam is an agonist of GABA receptor channels (GABA RCs), and has anticonvulsant effect .

HY-17030S

Acamprosate-d3 calcium
Acamprosate-d₃ (calcium) is the deuterium labeled Acamprosate calcium. Acamprosate calcium is a GABA receptor agonist and modulator of glutamatergic systems[1][2].

HY-B0007S

Baclofen-d4

Baclofen-d₄ is the deuterium labeled Baclofen. Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research[1][2][3].

HY-110233S

Acamprosate-d6 calcium
Acamprosate-d₆ (calcium) is the deuterium labeled Acamprosate calcium. Acamprosate calcium (Campral EC) is a GABA receptor agonist and modulator of glutamatergic systems[1].

HY-B0007S2

Baclofen-d5 hydrochloride

Baclofen-d₅ hydrochloride is deuterated labeled Baclofen (HY-B0007). Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABA_B receptor (GABA_BR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABA_B receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research .

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