GABA Receptors

Flumazenil, an imidazobenzodiazepine derivative, antagonizes the actions of benzodiazepines on the central nervous system. Flumazenil competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex. Flumazenil is a weak partial agonist in some animal models of activity, but has little or no agonist activity in humans.

(+)-Bicuculline is a classical GABAA antagonist.

Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor.

2-Hydroxysaclofen is a potent and selective antagonist at GABAB receptors.

Cloflubicyne is a potent non-competitive GABA antagonist, convulsant, laboratory insecticide.

Ro 15-1788 is a benzodiazepine receptor antagonist.

U-93631 is a GABAA receptor ligand of novel chemical structure with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors.

(-)-Securinine is an alkaloid originally isolated from S. suffructicosa. Securinine, is a specific GABA receptor antagonist and has been found to have significant in vivo CNS activity.

Cgp 52432 is a GABA-A receptor antagonist.

CGP 36742 is a selective GABAB receptor antagonist that can penetrate the blood?Cbrain barrier after peripheral administration, with an IC50 of 32?μM. CGP 36742 is useful in treatment of depression.

Sarmazenil is a benzodiazepine receptor antagonist.

SCH 50911, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist.

Gabazine free base is a specific GABA receptor antagonist. Does not affect GABA-transaminase or glutamate-decarboxylase activitites.