Receptor GABA

COR659: suppresses alcohol/chocolate intake in rats; enhances GABAB receptor, blocks CB1 receptor.

Diproqualone, analogous to methaqualone, exhibits sedative, anxiolytic, anti-inflammatory, and analgesic properties [1].

FGIN-1-27 is a high-affinity agonist of the translocator protein and a specific peripheral benzodiazepine receptor (PBR) ligand(Ki = 5.0 nM).

CGP 64213 is a GABAb receptor agonist.

CGP55845 hydrochloride is a potent and selective GABAB receptor antagonist with an IC 50 of 6 nM which can be used in neurological research [1] [2].

PZ-II-029 is a modulator of α6β3γ2-selective GABAA channel.

Potent GABAA antagonist; IC50: 24 nM (α1β2γ2), Ki: 28 nM (rat); inactive on human GABA transporters.

Org-21465, a gamma-aminobutyric acid (GABA) receptor agonist, is used potentially for the use of anesthesia.

Timelotem represents a class of 1,2-fused 1,4-benzodiazepine drugs. Timelotem exhibits significant antipsychotic properties. It produces sedative, anxiolytic, and anticonvulsant effects by enhancing the action of the neurotransmitter γ-aminobutyric acid (GABA). Timelotem may be used in research on schizophrenia and other psychiatric disorders.

(R)-4-Amino-3-hydroxybutyric acid, also known as (R)-GABOB, acts as a modulator of GABA receptors, specifically binding to both GABAA and GABAB receptors and blocking GABA reuptake in rat brain synaptosomes. Additionally, it serves as a GABAC receptor agonist, triggering currents in patch-clamp assays with Xenopus oocytes that express the human receptor. In vivo studies reveal its capability to suppress electrical discharges in the amygdala in cats undergoing N-amidinobenzamide-triggered seizures, indicating its potential therapeutic application in managing seizure disorders.

NCS-382 (sodium) is a potent antagonist of the GABA receptor, exhibiting anti-sedative and anti-hypnotic properties, with applications in neurological disease

GABA-IN-2 (Compound 5), a GABA inhibitor, exhibits both larvicidal and insecticidal properties, achieving an 87% mortality rate at a concentration of 50 mg/L [1

TPA 023 is a selective agonist of GABAA α2/α3 subtype (Kis = 0.19 - 0.41 nM).

CGP 55845: potent, selective GABAB blocker, IC50=5 nM, hinders agonist binding, reduces GABA/glutamate release.

JM-1232 is a sedative and hypnotic drug being researched as a potential anesthetic.

L-822179 (α5IA) is a selective inverse agonist for the Α5 subtype of GABAA receptor with higher intrinsic activity at the A5 subtype than other drugs.

CGP-54626 is a selective antagonist of the GABAB receptor (IC50 = 4 nM ).

(-)-Bicuculline methochloride is a potent antagonist of GABAA receptor.

Cinazepam is a GABAA receptor partial agonist and a benzodiazepine derivative with anxiolytic and sedative properties. Cinazepam can be utilized in research related to sleep disorders.

6,2'-Dihydroxyflavone is a novel antagonist of GABAA receptor.