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 Controls
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GABA Receptor Ligands
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GABA Receptor Related Products (778)
Related Products (778)
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Antibodies (14)
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Related Compound Screening Libraries (1)
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CHF-2993
0 ImagesCat. No.: HY-118018CAS No.: 202914-21-4CHF-2993 is an orally active anticonvulsant. CHF-2993 antagonizes Bicuculline (HY-N0219)- and Picrotoxin (HY-101391)-induced tonic convulsions in mice, shows no activity against Pentylenetetrazole-induced clonic convulsions in mice, and partially reduces Veratridine (HY-N6691)-induced aspartate efflux in rat cortical synaptosomes. CHF-2993 can be used in the research of epilepsy.
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LY81067
0 ImagesCat. No.: HY-119105CAS No.: 87186-60-5LY81067, a diaryltriazine, effectively protects against Pentylenetetrazole- and Picrotoxin-induced convulsions in mice. LY81067 exerts its anticonvulsant effects by binding to or near Picrotoxin (HY-101391) binding sites.
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GABAA receptor agent 2
0 ImagesCat. No.: HY-103513CAS No.: 1236105-75-1GABAA receptor agent 2 (compound 13) is a compound used to study the structure and orthosteric ligand binding of GABA(A) receptors. The relevant model of GABAA receptor agent 2 can be used to understand the details of orthosteric ligand binding, and a detailed binding mode hypothesis was created through structure-activity relationships with two homologous series of orthosteric GABA(A)R antagonists.
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Divaplon
0 ImagesCat. No.: HY-19438CAS No.: 90808-12-1Synonyms: RU 32698Divaplon is a GABA receptor agonist with the EC50 values of 31 and 2 nM for α3β2γ2 and α5β2γ2, respectively. Divaplon shows anxiolytic activity.
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GABAA receptor agent 8
0 ImagesCat. No.: HY-146100CAS No.: 2376841-54-0GABAA receptor agent 8 (compoud 5e) is a potent GABAA receptor positive modulator. GABAA receptor agent 8 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 8 has the potential for the research of epilepsy.
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CI-966
0 ImagesCat. No.: HY-123240CAS No.: 110283-79-9CI-966 is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC50s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 exhibits anticonvulsant and neuroprotective activities.
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TG 41
0 ImagesCat. No.: HY-111298CAS No.: 850339-33-2TG 41 is positive modulator of GABAA receptor. TG 41 enhances the binding both of GABA and of Flunitrazepam to rat cerebral cortical membranes.
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AA29504
0 ImagesCat. No.: HY-103522CAS No.: 945828-50-2AA29504 is a ethyl carbamate with γ-aminobutyric acid (GABAA(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 .
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(S)-Baclofen
0 Images(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.
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Magnolia obovata extract
0 ImagesCat. No.: HY-N19977Magnolia obovata extract is an extract of Magnolia obovata that exerts its anti-anxiety effect by enhancing GABA receptor function and through anti-neuroinflammatory mechanisms.
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Etiocholanolone-d2
0 ImagesCat. No.: HY-113320S1CAS No.: 2687960-82-1Synonyms: 5β-Androsterone-d2Etiocholanolone-d2 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form.
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SH-053-S-CH3-2'F
0 ImagesCat. No.: HY-115857CAS No.: 872874-00-5SH-053-S-CH3-2'F is a selective positive allosteric modulator that produces mild to partial agonistic activity at α(1) GABA(A) receptors. SH-053-S-CH3-2'F showed anxiety-relieving effects at a dose of 30 mg/kg. SH-053-S-CH3-2'F completely avoids the memory impairment commonly caused by benzodiazepine site agonists. SH-053-S-CH3-2'F shows strong selectivity at GABA(A) receptors, which could potentially be used to develop more selective anti-anxiety drugs.
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GABA-palmitamide
0 ImagesGABA-palmitamide is a GABA-responsive compound. GABA-palmitamide exhibits a dose-dependent bidirectional regulatory effect on the stereotyped behavior induced by Apomorphine (HY-12723): high doses inhibit motor behavior, while low doses enhance stereotyped behaviors in the oral cavity. GABA-palmitamide can be used in research on behavior regulation.
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Denzimol hydrochloride
0 ImagesCat. No.: HY-105059ACAS No.: 77234-90-3Denzimol hydrochloride is an orally active anticonvulsant agent. Denzimol hydrochloride inhibits cytochrome P450, and interacts with benzodiazepine receptors. Denzimol hydrochloride selectively antagonizes tonic components of Metrazol-induced seizures in rats and mice. Denzimol hydrochloride can be used for the research of epilepsy and convulsions.
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Flupirtine-d6 hydrochloride
0 ImagesCat. No.: HY-W709349SSynonyms: D 9998-d6 hydrochlorideFlupirtine-d6 (D 9998-d6) hydrochloride is the deuterium labeled Flupirtine hydrochloride (HY-W709349). Flupirtine 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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2-AEMP
0 ImagesCat. No.: HY-129907CAS No.: 321882-95-5Synonyms: 2-Aminoethyl methylphosphonate2-AEMP (2-Aminoethyl methylphosphonate) is an anti-GABA(A)-ρ1 receptor compound with antagonist activity. 2-AEMP exhibits competitive inhibition compared to TPMPA with an IC(50) value of 18 μM, compared to 7 μM for TPMPA. The release rate of inhibition at termination of 2-AEMP is significantly higher than that of TPMPA. The preincubation time required for the onset of inhibition of 2-AEMP is much shorter than that of TPMPA. Some analogs of 2-AEMP, especially those with benzyl or n-butyl substituents, show lower potency in terms of biological activity.
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Californidine perchlorate
0 ImagesCat. No.: HY-W739289CAS No.: 17939-31-0Californidine perchlorate is an orally active γ-aminobutyric acid (GABA) receptor and serotonin receptor modulator. Californidine perchlorate enhances GABA-mediated chloride influx and inhibits cytochrome P450 enzymes. Californidine perchlorate is promising for research of anxiety.
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BTS 72664
0 ImagesCat. No.: HY-182548CAS No.: 165383-52-8BTS 72664 is a broad-spectrum, non-sedating, orally effective anticonvulsant. Its anticonvulsant effect mainly arises from enhancing GABAA receptor (GABAA receptor)-mediated chloride channel currents, while it exerts weak blocking effects on Na+ channels (Ki = 350 μM) and NMDA receptors (NMDA receptor) (IC50 = 43 μM). BTS 72664 prevents the elevation of extracellular glutamate, glycine and serine concentrations in neurons, reduces cerebral infarct size, promotes functional recovery, prevents multiple types of epileptic seizures, and has low sedative potential. BTS 72664 can be used for the research of epilepsy, stroke and migraine.
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Rac-Vigabatrin-13C,d2
0 ImagesCat. No.: HY-W778008CAS No.: 1330171-61-3Rac-Vigabatrin-13C,d2 (Major) is the deuterium and 13C labeled Vigabatrin (HY-15399). Vigabatrin (γ-Vinyl-GABA), an inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.
