GABA Receptor

Gamma-aminobutyric acid Receptor; γ-Aminobutyric acid Receptor

GABA Receptor

Related Products

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). It has long been recognized that the fast response of neurons to GABA that is blocked by bicuculline and picrotoxin is due to direct activation of an anion channel. This channel was subsequently termed the GABAA receptor. Fast-responding GABA receptors are members of family of Cys-loop ligand-gated ion channels. A slow response to GABA is mediated by GABAB receptors, originally defined on the basis of pharmacological properties.

GABA Receptor Related Products (767)
Antibodies (14)
Related Compound Screening Libraries (1)

By Effects:	Agonists (189)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-10061A

Lesogaberan napadisylate	Agonist
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-159826

Brexanolone caprilcerbate	Agonist
Brexanolone caprilcerbate is a potent GABAA receptor positive allosteric modulator.

HY-165444

CP-615003	Agonist
CP-615003 is a potent and subtype-selective partial agonist of GABA_A receptor (GABA_A receptor) (K_i = 1.1 μM). CP-615003 is mainly converted into the active metabolite CP-900725 through oxidative deamination in monkeys and humans, and the latter also has GABA_A receptor affinity. CP-615003 is a substrate of P-glycoprotein (P-gp/MDR1), resulting in severe limitation of its penetration into the central nervous system (CNS). CP-615003 can be used for the study of CNS-related indications.

HY-119605

DAA-1097	Agonist
DAA-1097 is an orally active and selective agonist for the peripheral benzodiazepine receptor (PBR). DAA-1097 has anxiolytic effects.

HY-106851

Panadiplon	Agonist
Panadiplon (FG 10571; PNU 78875), a benzodiazepine receptor, is a 5GABAA partial agonist. Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors.

HY-W722556

5α-Androstan-3α-ol	Agonist
5α-Androstan-3α-ol is a γ-aminobutyric acid (GABA) receptor agonist. 5α-Androstan-3α-ol can inhibit the transcriptional activity of the orphan nuclear receptor CAR (constitutive androstane receptor). 5α-Androstan-3α-ol negatively regulates the activity of CAR by binding to CAR and promoting its dissociation from coactivator proteins. 5α-Androstan-3α-ol can be used to study nuclear receptor-mediated hormone metabolism and drug detoxification mechanisms.

HY-177099

Lorotomidate	Agonist
Lorotomidate (Example 16) is a GABAA receptor agonist. Lorotomidate has anaesthetic effects (ED₅₀: i.v., 2 mg/kg in KM mice; LD₅₀: 46.5 mg/kg in KM mice). Lorotomidate has no inhibitory effect on the secretion of corticosteroids in animals, and thus has good safety.

HY-19438

Divaplon	Agonist
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-B0007B

(S)-Baclofen	Agonist
(S)-Baclofen is a GABAB receptor agonist that crosses the blood-brain barrier and is orally active, with IC₅₀ values of 1.77 μM for GABAB and 1564 μM for GABAA. (S)-Baclofen can be used in research on muscle disorders such as spasticity.

HY-19308

RWJ-51204	Agonist
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-107482A

Picamilon sodium	Agonist
Picamilon sodium is an orally active derivative of γ-aminobutyric acid that has nootropic effect. Picamilon sodium improves the epilepsy model in rats and promotes correction of functional disorders of the pancreas during Alloxan (HY-W017227)-induced diabetes mellitus in rats.

HY-117560

PWZ-029	Agonist
PWZ-029 is a selective inverse agonist for 5 GABA_A receptors. PWZ-029 is a benzodiazepine site ligand. PWZ-029 shows a weak but significant partial agonistic effect at 1- and 3-containing receptors. PWZ-029 significantly increases retention session latency in mouse fibroblast cells. PWZ-029 can improve object recognition in normal and scopolamine-treated rat model.

HY-N0067S4

γ-Aminobutyric acid-¹⁵N	Agonist
γ-Aminobutyric acid-¹⁵N (4-Aminobutyric acid-¹⁵N) is the ¹⁵N-labeled γ-Aminobutyric acid (HY-N0067). γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABA_A receptors) and metabotropic receptors (GABA_B receptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system.

HY-173616

GABAA receptor modulator-8	Agonist
GABAA receptor modulator-8 (10c) is a blood-brain barrier penetrated, selective and positive modulator of GABAA receptor, with excellent antiepileptic activity.

HY-168986

Moxetomidate	Agonist	98.58%
Moxetomidate is a GABAA receptor agonist with hypnotic effect.

HY-B1594R

Carbromal (Standard)	Agonist
Carbromal (Standard) is the analytical standard of Carbromal. This product is intended for research and analytical applications. Carbromal (Adalin; Adisomnol) is a sedative with centrally depressant effects.

HY-169193

Azocarnil	Agonist
Azocarnil is a GABAergic agonist-potentiator. Azocarnil can be used in neurological research.

HY-123249

HZ166	Agonist
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.

HY-U00199A

(S)-Norzopiclone	Agonist
(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 GABA_A receptor and inhibits nACh and NMDA receptors.

HY-14758

Adipiplon	Agonist
Adipiplon (NG2-73) is a selective GABA_A receptor positive allosteric modulator. Adipiplon is particularly useful in the research of a variety of central nervous system (CNS) disorders.

GABA Receptor Compound Library

Compound library containing various GABA receptor inhibitors and activators.

211compounds HY-L120

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GABA Receptor

GABA Receptor

GABA Receptor Related Products (767)

Antibodies (14)

Related Compound Screening Libraries (1)

GABA Receptor Related Products (767):