Pivagabine (CXB 722), a psychoactive drug, is a hydrophobic 4-aminobutyric acid derivative with neuromodulatory activity. Pivagabine penetrates the blood-brain barrier in rats. Pivagabine antagonizes the effects of foot shock on both GABAA receptor function and corticotropin-releasing factor (CRF) concentrations in rat brain[1][2].
Pivagabine (CXB 722) (200 mg/kg; i.p.; twice a day for 4 days and 1 hour before killing on the 5th day) prevents the effects of foot-shock stress on CRF concentration in both brain regions[2]. Animal Model: Adult male Sprague-Dawley CD rats (200-250 g)[2]
[1]. Esposito G, et al. Pivagabine: a novel psychoactive drug. Arzneimittelforschung. 1997 Nov;47(11A):1306-9. [2]. Serra M, et al. Antagonism by pivagabine of stress-induced changes in GABAA receptor function and corticotropin-releasing factor concentrations in rat brain. Psychoneuroendocrinology. 1999 Apr;24(3):269-84.