2. Signaling Pathways
  3. Membrane Transporter/Ion Channel
    Neuronal Signaling
  4. GABA Receptor

GABA Receptor

Gamma-aminobutyric acid Receptor; γ-Aminobutyric acid Receptor

GABA Receptor

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-17354A
    (R)-Baclofen hydrochloride
    		Agonist 98.12%
    (R)-Baclofen hydrochloride (Arbaclofen hydrochloride) is a selective GABAB receptor agonist.
    (R)-Baclofen hydrochloride
  • HY-108403R
    Phenibut (Standard)
    		Agonist
    Phenibut (Standard) is the analytical standard of Phenibut (HY-108403). This product is intended for research and analytical applications. 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.
    Phenibut (Standard)
  • HY-111052R
    AZD7325 (Standard)
    		Agonist
    AZD7325 (Standard) is the analytical standard of AZD7325. This product is intended for research and analytical applications. AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=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.
    AZD7325 (Standard)
  • HY-N1951R
    Miltirone (Standard)
    		Agonist
    Miltirone is an orally active natural compound found in the root of Salvia miltiorrhiza. Miltirone is a central benzodiazepine receptor partial agonist, with an IC50 of 0.3 μM. Miltirone induces ROS - and-p53 dependent apoptosis. Miltirone inhibits carboxylesterase 2 (CES2; Ki = 0.04 μM) and SARS-CoV main protease (Mpro).
    Miltirone (Standard)
  • HY-129105R
    Clomethiazole (Standard)
    		Agonist
    Clomethiazole (Standard) is the analytical standard of Clomethiazole. This product is intended for research and analytical applications. Chlormethiazole is an potent and orally active GABAA agonist. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus.
    Clomethiazole (Standard)
  • HY-123426
    JY-XHe-053
    		Agonist
    JY-XHe-053 is a potent and selective agonist of GABAA receptors containing the α5 subunit (Kis of 22.0 nM, 12.3 nM, 34.9 nM, 0.7 nM for α1, α2, α3, α5, respectively). JY-XHe-053 lacks significant anti-anxiety activity, despite its efficacy at α2- and α3-GABAA receptors.
    JY-XHe-053
  • HY-19082
    Y-23684
    		Agonist
    Y-23684 is a partial agonist of benzodiazepine receptor (BZR) with anticonvulsant and anxiolytic activities. Y-23684 can be used in the research of treatment of anxiety disorders.
    Y-23684
  • HY-117257
    PF-0713
    		Agonist
    PF 0713 is a GABAA receptor agonist..
    PF-0713
  • HY-105272R
    Loreclezole (Standard)
    		Agonist
    Loreclezole (Standard) is the analytical standard of Loreclezole. This product is intended for research and analytical applications. Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
    Loreclezole (Standard)
  • HY-14953R
    Imepitoin (Standard)
    		Agonist
    Imepitoin (Standard) is the analytical standard of Imepitoin. This product is intended for research and analytical applications. Imepitoin (AWD 131-138) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.
    Imepitoin (Standard)
  • HY-B1833S
    Afloqualone-d7
    		Agonist
    Afloqualone-d7 (HQ-495-d7) is deuterium labeled Afloqualone. Afloqualone (HQ-495) is an orally active central muscle relaxant and antivertiginous agent that can increase the sensitivity of GABA receptors in neurons of the lateral vestibular nucleus. Afloqualone (HQ-495) can be used in the research of low back pain and neck-arm-shoulder syndrome.
    Afloqualone-d<sub>7</sub>
  • HY-W012123R
    3,4,5-Trimethoxycinnamic acid (Standard)
    		Agonist
    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.
    3,4,5-Trimethoxycinnamic acid (Standard)
  • HY-19945R
    DAA-1106 (Standard)
    		Agonist
    DAA-1106 (Standard) is the analytical standard of DAA-1106. This product is intended for research and analytical applications. 0
    DAA-1106 (Standard)
  • HY-10061BR
    Lesogaberan hydrochloride (Standard)
    		Agonist
    Lesogaberan (hydrochloride) (Standard) is the analytical standard of Lesogaberan (hydrochloride) (HY-10061B). This product is intended for research and analytical applications. Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAA 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.
    Lesogaberan hydrochloride (Standard)
  • HY-100800R
    TACA (Standard)
    		Agonist
    TACA (Standard) is the analytical standard of TACA (HY-100800). This product is intended for research and analytical applications. TACA (trans-4-Aminocrotonic acid) is a potent agonist of GABAA and GABAC receptors (KD= 0.6 μM). TACA also is GABA uptake inhibitor and substrate for GABA-T. TACA produces late biphasic responses in the MPG neurons.
    TACA (Standard)
  • HY-19065
    Ru-32514
    		Agonist
    Ru-32514 is an agonist of benzodiazepine receptor.
    Ru-32514
  • HY-19250
    U-101017
    		Agonist
    U-101017 is a partial agonist of benzodiazepine receptor and GABAA receptor, with anxiolytic effects. 
    U-101017
  • HY-124225
    RU 33965
    		Agonist
    RU 33965 is an orally active benzodiazepine receptor weak partial inverse agonist.
    RU 33965
  • HY-107482R
    Picamilon (Standard)
    		Agonist
    Picamilon (Standard) is the analytical standard of Picamilon (HY-107482). This product is intended for research and analytical applications. Picamilon is an orally active derivative of γ-aminobutyric acid that has nootropic effect. Picamilon improves the epilepsy model in rats and promotes correction of functional disorders of the pancreas during Alloxan (HY-W017227)-induced diabetes mellitus in rats.
    Picamilon (Standard)
  • HY-103668AR
    SSD114 hydrochloride (Standard)
    		Agonist
    SSD114 hydrochloride (Standard) is the analytical standard of SSD114 hydrochloride (HY-103668A). This product is intended for research and analytical applications. SSD114 hydrochloride is a novel GABAB receptor positive allosteric modulator.
    SSD114 hydrochloride (Standard)
Cat. No. Product Name / Synonyms Application Reactivity