CGP52432 is a GABA_B receptor antagonist, with an IC₅₀ of 85 nM. IC50 & Target: IC50: 85 nM (GABA_B receptor)^[1] In Vitro: CGP52432 is a GABA_B receptor antagonist, with an IC₅₀ of 85 nM, 35- and 100-fold lower than at the receptors regulating somatostatin and glutamate overflow, respectively^[1]. In Vivo: CGP52432 (10, 30 mg/kg) shows no effect on the total arm entries and total head dips of mice on the elevated-plus maze^[2]. CGP52432 (100 nmol/kg, i.v., or 1 nmol/kg, i.c.v.) abolishes the suppressive effects of GABA ( 50 μmol/kg, i.v.) on enhanced renal sympathetic nerve activity (RSNA) during ischaemia, causeing elimination of the renoprotective effects of GABA in rats^[3].