Morelli M, Di Chiara G
Eur J Pharmacol. 1985 Nov 5;117(2):179-85. doi: 10.1016/0014-2999(85)90602-8.
The ability of SCH 23390 as compared to haloperidol to produce catalepsy in rats was evaluated in three tests for catalepsy. SCH 23390 produced catalepsy in all three tests with ED50 (mg/kg s.c.) of 0.017 on the vertical grid, 0.023 on the horizontal bar and 0.038 on the 'four corks'. Haloperidol produced catalepsy with ED50 (mg/kg s.c.) of 0.048 on the vertical grid, 0.042 on the horizontal bar and 0.065 on the four corks. Catalepsy by SCH 23390 and by haloperidol was prevented by scopolamine and potentiated by alpha-methyl-p-tyrosine pretreatment. Catalepsy induced by SCH 23390 was also prevented by specific D-2 receptor agonists such as pergolide, lisuride and bromocriptine but not by the D-1 receptor agonist SKF 38393. The results demonstrate that SCH 23390 is potently cataleptogenic and that the catalepsy it produces has a pharmacologic profile typical of that produced by potent and specific D-2 antagonists.
在三项僵住症测试中评估了SCH 23390与氟哌啶醇相比在大鼠中产生僵住症的能力。SCH 23390在所有三项测试中均产生僵住症,垂直网格试验的半数有效剂量(ED50,mg/kg皮下注射)为0.017,水平杆试验为0.023,“四个软木塞”试验为0.038。氟哌啶醇产生僵住症的垂直网格试验ED50(mg/kg皮下注射)为0.048,水平杆试验为0.042,四个软木塞试验为0.065。东莨菪碱可预防SCH 23390和氟哌啶醇所致的僵住症,α-甲基-对-酪氨酸预处理可增强僵住症。特异性D-2受体激动剂如培高利特、利苏瑞肽和溴隐亭可预防SCH 23390诱导的僵住症,但D-1受体激动剂SKF 38393则不能。结果表明,SCH 23390具有强效致僵住症作用,其产生的僵住症具有强效特异性D-2拮抗剂所产生僵住症的典型药理学特征。