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 (349)
Antibodies (2)

By Effects:	Inhibitors (64) Agonists (96) Antagonists (77) Activators (35) Modulators (33)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-16716

Basmisanil	Inhibitor	99.91%
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 K_i value of 5 nM and IC₅₀ value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders.

HY-121599

CGP 36742	Antagonist	≥98.0%
CGP 36742 is a selective GABA_B receptor antagonist that can penetrate the blood–brain barrier after peripheral administration, with an IC₅₀ of 32 μM. CGP 36742 is useful in treatment of depression.

HY-W012123

3,4,5-Trimethoxycinnamic acid	Agonist	99.79%
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-14426

L-655708	Inhibitor	99.92%
L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (K_i=0.45 nM).

HY-100228A

SKF89976A hydrochloride	Inhibitor	99.70%
SKF89976A hydrochloride is a selective GABA transporter (GAT-1) inhibitor with IC₅₀s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.

HY-10233

Gaboxadol hydrochloride	Modulator	99.80%
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABA_A receptor and an antagonist of GABA_C 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.

HY-16579A

Etifoxine	Activator	99.96%
Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABA_A receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.

HY-B1833

Afloqualone	Agonist	99.94%
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-B0135A

Furosemide sodium	Antagonist	99.89%
Furosemide sodium is a potent and orally active inhibitor of Na⁺/K⁺/2Cl^- (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide sodium is also a GABA_A 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-Y0313

p-Hydroxybenzaldehyde	Antagonist	99.98%
p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABA_A receptor of the α₁β₂γ₂S subtype at high concentrations.

HY-N0700

alpha-Asarone	Activator	99.88%
alpha-Asarone (α-Asarone) is one of the main psychoactive compounds, and possesses an antidepressant-like activity in mice.

HY-111052

AZD7325	Agonist	99.27%
AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (K_i=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.

HY-103474

Bicuculline methiodide	Inhibitor	99.24%
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 Ca²⁺ -activated K⁺ channels. Bicuculline methiodide facilitates burst firing via blocking apamin-sensitive Ca²⁺ -activated K⁺ current.

HY-101411

4-Acetamidobutanoic acid	Agonist	≥98.0%
4-Acetamidobutanoic acid (N-acetyl GABA), the main metabolite of GABA, exhibits antioxidant and antibacterial activities.

HY-U00228

Rilmazafone hydrochloride		99.75%
Rilmazafone hydrochloride (450191S) is a benzodiazepine (omega) ligand.

HY-120874

PF-06372865	Activator	98.42%
PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABA_A positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABA_A receptors containing α1/α2/α3/α5 subunits (K_is 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.

HY-100370

MRK-016	Antagonist	99.27%
MRK-016 is a selective, orally bioavailable inverse agonist of GABA_A α5 receptor, with an EC₅₀ of 3 nM for GABA_A α5, and K_is of 0.83, 0.85, 0.77 and 1.4 nM for human GABA_A α1β3γ2, GABA_A α2β3γ2, GABA_A α3β3γ2, and GABA_A α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.

HY-116152

Cipepofol	Agonist	99.42%
Cipepofol (Ciprofol), a novel 2,6-disubstituted phenol derivative, is a positive allosteric modulator and direct agonist of the GABA_A 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.

HY-B0033

Vigabatrin hydrochloride	Inhibitor	≥98.0%
Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin hydrochloride is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.

HY-N2096

Kavain	Activator	99.82%
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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GABA Receptor

GABA Receptor

GABA Receptor Related Products (349)

Antibodies (2)

GABA Receptor Related Products (349):