GABA Receptor
Gamma-aminobutyric acid Receptor; γ-Aminobutyric acid Receptor
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.
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GABA Receptor Inhibitors
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GABA Receptor Agonists
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GABA Receptor Antagonists
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GABA Receptor Activators
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GABA Receptor Modulators
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GABA Receptor Controls
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GABA Receptor Ligands
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GABA Receptor Related Products (782)
Related Products (782)
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Antibodies (14)
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Related Compound Screening Libraries (1)
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GABAA receptor modulator-10
0 ImagesCat. No.: HY-175670GABAA receptor modulator-10 is an orally active, potent positive allosteric modulator (PAM) of the α1β2γ2 GABAA receptor with favorable blood-brain barrier (BBB) penetration. GABAA receptor modulator-10 enhances α1β2γ2 GABAA receptor function and potentiates GABA-evoked currents. GABAA receptor modulator-10 demonstrates potent antiepileptic efficacy in both the Pentetrazol (PTZ)- and Kainic Acid (KA) (HY-N2309)-induced mice epilepsy models. GABAA receptor modulator-10 can be used for the study of epilepsy.
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Gabazine free base
0 ImagesCat. No.: HY-117256CAS No.: 105538-73-6Synonyms: SR95531 free baseGabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of 0.2 μM for GABA receptor.
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2-Ethyl-3-methylpyrazine
0 ImagesCat. No.: HY-W012832CAS No.: 15707-23-02-Ethyl-3-methylpyrazine is a GABAA receptor potentiator, Antibacterial agent and Antifungal agent, with a Kp of 1.14 mM for GABAA. 2-Ethyl-3-methylpyrazine forms via the Maillard reaction in sunflower seeds and also exists in the crust of wheat bread. 2-Ethyl-3-methylpyrazine regulates mood or states of consciousness via central GABAA receptors. 2-Ethyl-3-methylpyrazine inhibits the growth of Ralstonia solanacearum and Magnaporthe oryzae. 2-Ethyl-3-methylpyrazine acts as an anxiolytic. 2-Ethyl-3-methylpyrazine is one of the sources of cocoa aroma, imparting nutty, corn-like, burnt, cereal, roasted and earthy flavors to foods. 2-Ethyl-3-methylpyrazine can be used in studies related to anxiety disorders and plant bacterial, fungal and oomycete infections.
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LI-633
0 ImagesCat. No.: HY-185007CAS No.: 1849624-82-3LI-633 is a selective and orally active GABAA receptor positive allosteric modulator (PAM) with a Ki of 21 nM. LI-633 produces robust potentiation of GABA-induced inward current, with EC50 values ranging from 8 nM (α5β2γ2) to 128 nM (α3β2γ2). LI-633 potentiates muscimol-induced GABAergic currents in rat dorsal root ganglion (DRG) neurons with an EC50 of 70.4 nM. LI-633 can be used for the study of visceral pain.
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Lesogaberan napadisylate
0 ImagesCat. No.: HY-10061ACAS No.: 477956-38-0Synonyms: AZD-3355 napadisylateLesogaberan (AZD-3355) napadisylate is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan napadisylate 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 napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
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Brexanolone caprilcerbate
0 ImagesCat. No.: HY-159826CAS No.: 2681264-65-1Brexanolone caprilcerbate is a potent GABAA receptor positive allosteric modulator.
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mGAT3/4-IN-1
0 ImagesCat. No.: HY-146280CAS No.: 2556833-57-7mGAT3/4-IN-1 (compound 19b) is a potent mGAT3/mGAT4 inhibitor, with pIC50 values of 5.31 and 5.24, respectively. mGAT3/4-IN-1 exhibits a significant tactile allodynia reduction in diabetic neuropathic mice.
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Methionine (Standard)
0 ImagesMethionine (Standard) is the analytical standard of Methionine. This product is intended for research and analytical applications. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
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Picrotin (Standard)
0 ImagesCat. No.: HY-107782RCAS No.: 21416-53-5Picrotin (Standard) is the analytical standard of Picrotin. This product is intended for research and analytical applications. Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs with IC50 values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission.
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Flupirtine hydrochloride
0 ImagesCat. No.: HY-W709349CAS No.: 33400-45-2Synonyms: D 9998 hydrochlorideFlupirtine (D 9998) hydrochloride is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine hydrochloride is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine hydrochloride stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine hydrochloride exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine hydrochloride functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine hydrochloride can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.
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CP-615003
0 ImagesCat. No.: HY-165444CAS No.: 329016-45-7Synonyms: NGD-913CP-615003 is a potent and subtype-selective partial agonist of GABAA receptor (GABAA receptor) (Ki = 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 GABAA 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.
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Etbicyphat
0 ImagesEtbicyphat (Trimethylopropane phosphate) is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors.
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DAA-1097
0 ImagesCat. No.: HY-119605CAS No.: 220551-79-1DAA-1097 is an orally active and selective agonist for the peripheral benzodiazepine receptor (PBR). DAA-1097 has anxiolytic effects.
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Amentoflavone (Standard)
0 ImagesAmentoflavone (Standard) is the analytical standard of Amentoflavone. This product is intended for research and analytical applications. Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase.
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Panadiplon
0 ImagesCat. No.: HY-106851CAS No.: 124423-84-3Synonyms: FG 10571; PNU 78875Panadiplon (FG 10571; PNU 78875), a benzodiazepine receptor, is a 5GABAA partial agonist. Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors.
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Thiazesim hydrochloride
0 ImagesCat. No.: HY-105857ACAS No.: 3122-01-8Thiazesim hydrochloride is a CNS-penetrant GABAA receptor inhibitor, exerting anticonvulsant and antidepressant effects. Thiazesim hydrochloride depresses amygdala output, disrupts conditioned avoidance response in rats. Thiazesim hydrochloride can be used for the research of depression and epilepsy.
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Cholesteryl γ-aminobutyrate
0 ImagesCat. No.: HY-177573CAS No.: 89210-68-4Cholesteryl γ-aminobutyrate is a γ-aminobutyric acid (GABA)-mimetic prodrug. Cholesteryl γ-aminobutyrate inhibits the orthodromically-evoked discharge of pyramidal cells in the CA1 region of the hippocampus. Cholesteryl γ-aminobutyrate suppresses the open-field activity of mice and rats in a dose-dependent manner and inhibits Bicuculline (HY-N0219)-induced seizures in mice. Cholesteryl γ-aminobutyrate can be used for the study of CNS diseases related to impaired GABAergic neuronal function.
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5α-Androstan-3α-ol
0 ImagesCat. No.: HY-W722556CAS No.: 7657-50-3Synonyms: 3α,5α-Androstanol5α-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.
