- 生物活性
Progabide 是一种 γ-氨基丁酸 (GABA) 受体激动剂。
- 靶点
GABA receptor
- 体内研究
Progabide is a gamma-aminobutyric acid receptor (GABA) agonist. Doses of 50, 100 and 200 mg/kg Progabide given IP to male Wistar rats increase the plasma corticosterone levels by 244, 365 and 476% respectively (t=6.44 to12.55, p<0.01). 10 mg/kg of Progabide fails to change the concentration of corticosterone in plasma (t=0.76, N.S.). The increased plasma corticosterone level induced by administration of 200 mg/kg Progabide is evident 30 (t=2.625, p<0.05), 60 (t=13.13, p<0.001) and 120 min (t=4.07, p<0.01) after drug injection, but returns to the control value 240 min after drug injection (t=0.86, N.S.). The greatest corticosterone rise (compare with the corresponding control) is reached 60 min following the administration of Progabide.
- 化学性质
从环己烷和甲苯结晶，熔点133～135℃；可能有第二个晶体，熔点142.5℃。UV最大吸收(甲醇)：332，250，210(ε4200，10900，24000)。急性毒性LD
50
小鼠(mg/kg)：900腹腔注射。
- 拟氨基丁酸药，为γ-氨基丁酸受体的直接激动药。用于癫痫(特别是部分性发作)及痉挛状态。
