Receptor GABA

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

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

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

(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.

Tuclazepam (KC 1956) is a derivative of the benzodiazepine class of drugs, exhibiting anti-anxiety and sedative properties.

5α-Androstan-3α-ol is a γ-aminobutyric acid (GABA) receptor agonist. It inhibits the transcriptional activity of the orphan nuclear receptor CAR (constitutive androstane receptor). By binding to CAR and promoting its dissociation from coactivator proteins, 5α-Androstan-3α-ol negatively regulates CAR's activity. This compound is useful for studying hormone metabolism and drug detoxification mechanisms mediated by nuclear receptors.

Refisolone is an antagonist of the GABAA receptor.

Compound 3e, a potent GABAA agonist, targets GABA sites and has potential anti-depressive effects in mice.

β-CCM is a benzodiazepine receptor inverse agonist with anxiogenic and convulsant effects. It enhances emotional reactivity and reduces interference sensitivity in spatial working memory tasks. β-CCM is applicable in research related to anxiety disorders.

EF1502 is a potent and selective GABA transporter inhibitor.

Fletazepam, a benzodiazepine derivative, exhibits sedative, anti-anxiety, and muscle-relaxant properties. It is utilized in neurological research.

benzodiazepine receptor antagonist,competitive

Thiomuscimol hydrobromide is an agonist of GABAA receptor.

CGS-9895 is a GABA antagonist that operates by interacting with the benzodiazepine binding site on GABA receptors containing the γ subunit (ag).

BGT1-IN-1 (compound 9) is an effective inhibitor of BGT1, demonstrating IC50 values of 13.9 µM for hBGT1 and 58.3 µM for GAT3. It exhibits no cytotoxic effects and possesses neuroprotective activity.

S-8510 phosphate is an agonist of inverse Benzodiazepine (BDZ) receptor(Kis of 34.6 nM, 36.2 nM for –GABA and +GABA respectively).

GABA-IN-4 (Compound 17) is a derivative of N-(indol-3-ylglyoxylyl)benzylamine. It exhibits high affinity for the benzodiazepine receptor (BzR), the binding site within the GABAA receptor complex, with a Ki value of 67 nM. Benzodiazepines are widely used as anxiolytic, sedative-hypnotic, and anticonvulsant agents.

Moxetomidate is a GABAA receptor (GABAA receptor) agonist with hypnotic properties.

Gabaculine, an irreversible GABA-T inhibitor (Ki: 2.9 μM), impacts plastid development and affects DPOR/GluTR levels.

Compound 4c, a potent GABAA agonist with anti-depressive effects in mouse FST/TST, shows promise in depression research.