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γ-aminobutyric acid receptors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	GABA Receptor (30) Akt (1) Biochemical Assay Reagents (1) Chloride Channel (2) Dopamine Receptor (1) Endogenous Metabolite (3) ERK (1) iGluR (1) Isotope-Labeled Compounds (1) JNK (1) Parasite (2) Phosphodiesterase (PDE) (1) Sodium Channel (1)
By Research Areas:	Cardiovascular Disease (2) Infection (2) Inflammation/Immunology (4) Metabolic Disease (1) Neurological Disease (27)

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: GABA Receptor Amino acid Transporter Amino Acid Derivatives Hydroxycarboxylic Acid Receptor (HCAR) Free Fatty Acid Receptor Fatty Acid Synthase (FASN) Apical Sodium-Dependent Bile Acid Transporter G protein-coupled Bile Acid Receptor 1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N0067S3

γ-Aminobutyric acid-13C4 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].

HY-N0067

γ-Aminobutyric acid 3 Publications Verification 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 (GABA_A receptors) and metabotropic receptors (GABA_B receptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system .

HY-N2096

Kavain	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 .

HY-N7110

6-Hydroxyflavone	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 (GABA_A) receptors. 6-Hydroxyflavone shows a clear preference for α2 - and α3 - subtypes, which play an anti-anxiety role .

HY-N0301

Thiocolchicoside	GABA Receptor	Neurological Disease Inflammation/Immunology
Thiocolchicoside is a competitive **γ-aminobutyric acid type A (GAB_AA) 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 .

HY-N0067R

γ-Aminobutyric acid (Standard) 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 .

HY-107151

ABP-700	GABA Receptor	Neurological Disease
ABP-700, an Etomidate analog and anesthetic, is a γ-aminobutyric acid type receptor agonist .

HY-103522

AA29504	GABA Receptor	Neurological Disease
AA29504 is a ethyl carbamate with γ-aminobutyric acid (GABA_A(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-116457

Propanidid Sombrevin; Fabantol	GABA Receptor	Cardiovascular Disease Neurological Disease
Propanidid (Sombrevin; Fabantol) is a **γ-aminobutyric acid type A (GABA_A) receptor** agonist and a short-acting non-barbiturate general agent that can suppress or relieve pain. Propanidid can decrease the arterial pressure .

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-P2602

α-Casozepine	GABA Receptor	Neurological Disease
α-Casozepine is a bioactive peptide derived from the α protein S1 casein in milk and has an affinity for γ-aminobutyric acid (GABA) receptors in the brain. α-Casozepine has anti-anxiety effects .

HY-16974

Afoxolaner	GABA Receptor Chloride Channel Parasite	Infection
Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod .

HY-N2096R

Kavain (Standard)	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-N0301R

Thiocolchicoside (Standard)	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 (GAB_AA) 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 .

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-16974R

Afoxolaner (Standard)	GABA Receptor Chloride Channel Parasite	Infection
Afoxolaner (Standard) is the analytical standard of Afoxolaner. This product is intended for research and analytical applications. Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod .

HY-12783

SCH 50911 hydrochloride	GABA Receptor	Neurological Disease
SCH 50911 hydrochloride, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor with IC₅₀ of 1.1 μM. SCH 50911 hydrochloride antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated ³H overflow with an IC₅₀ of 3 μM.

HY-A0173

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

HY-12783A

SCH 50911	GABA Receptor	Neurological Disease
SCH 50911, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor with IC₅₀ of 1.1 μM. SCH 50911 antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated ³H overflow with an IC₅₀ of 3 μM .

HY-163855

KGP-25	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 (GABA_A) in the central nervous system (CNS) for general anesthesia .

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-161784

GABAA receptor modular-3	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 .

HY-117955

GMA-839 WAY 141839; Co 2-6749	GABA Receptor	Neurological Disease
GMA-839 is a selective modulator of the **γ-aminobutyric acid A receptor (GABA_A) 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 .

HY-100936

Etazolate hydrochloride 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 (GABA_A) 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 .

HY-14856A

iso-Atagabalin hydrochloride iso-PD 0200390 hydrochloride	Others	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-116152A

(S)-Cipepofol (S)-Ciprofol; (S)-HSK3486	GABA Receptor	Neurological Disease
(S)-Cipepofol is the isomer of Cipepofol (HY-116152).Cipepofol (HSK3486) is a sleep-promoting active molecule and a gamma-aminobutyric acid (GABA) receptor enhancer .

HY-59302

Indole-5-carboxylic acid, 98%	Biochemical Assay Reagents	Others
Indole-5-carboxylic acid, 98% is an oxytocin that interacts with serotonin receptors and gamma-aminobutyric acid (GABA) receptors. It has also been reported to interact with various enzymes such as cyclooxygenase-2 (COX-2) and 5-hydroxytryptamine (5-HT) receptors.

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-101078A

(±)-Epibatidine dihydrochloride CMI 545 dihydrochloride	Dopamine Receptor	Neurological Disease
(±)-Epibatidine (CMI 545) dihydrochloride is an agonist of nicotinic with potent analgetic activity. (±)-Epibatidine (CMI 545) dihydrochloride is an alkaloid originally characterized from frog skin. (±)-Epibatidine (CMI 545) dihydrochloride have little or no activity at a variety of other central receptors, including opioid receptors, muscarinic receptors, adrenergic receptors, dopamine receptors, serotonin receptors, and gamma-aminobutyric acid receptors .

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-105056

Bretazenil Ro 16-6028	GABA Receptor	Neurological Disease
Bretazenil (Ro 16-6028) is a partial agonist at the gamma-aminobutyric acid A (GABA_A) 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 .

HY-103496

U-90042	GABA Receptor	Others
U-90042 is a **gamma-aminobutyric acidA receptor agonist of α1, α3 and α6 subtypes with K_i** values of 7.8 nM, 9.5 nM and 11.0 nM, respectively. U-90042 suppresses locomotor activity and impairs rotarod performance in mice. U-90042 produces sedation and ataxia and prolongs sleeping time in mice, rats and monkeys. U-90042 can be used as a sedative and hypnotic agent .

Cat. No.	Product Name

HY-L120

GABA Receptor Compound Library	152 compounds
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.

GABA Receptor Compound Library

152 compounds

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.

Cat. No.	Product Name	Type