(E)-GABABreceptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.GABABreceptor antagonist 1 is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.
SCH 50911 is (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid and is a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor (IC50: 1.1 μM). SCH 50911 antagonizes GABA(B) autoreceptors, increasi
CGP 36742 is a selective antagonist of the GABABreceptor that can penetrate the blood-brain barrier after peripheral administration (IC50: 32 μM). It is useful in the treatment of depression.
Lesogaberan is an effective and selective GABABreceptor agonist (EC50: 8.6 nM for human recombinant GABABreceptors). For rat brain GABAB and GABAA receptors, the binding affinity (Kis) is 5.1 nM and 1.4 μM, respectively.