Gerhardt S, Gerber R, Liebman J M
Life Sci. 1985 Dec 23;37(25):2355-63. doi: 10.1016/0024-3205(85)90102-x.
SCH 23390 induced only a negligible incidence of the acute dyskinetic syndrome, a predictor of neuroleptic-induced extrapyramidal liability, in squirrel monkeys. However, haloperidol-induced dyskinesias were potentiated by SCH 23390 and were blocked by the D-1 agonist, SKF 38393. When administered orally or intraperitoneally to mice, SCH 23390 showed a considerably wider dose separation than did conventional neuroleptics between antagonism of apomorphine climbing and antagonism of stereotyped sniffing. Clinically relevant distinctions may exist between D-1 and D-2 antagonists, with D-1 antagonists (exemplified by SCH 23390) showing lower, although possibly not negligible, potential to cause extrapyramidal side effects.
SCH 23390在松鼠猴中仅诱发了可忽略不计的急性运动障碍综合征发生率,该综合征是抗精神病药物所致锥体外系反应倾向的一个预测指标。然而,氟哌啶醇诱发的运动障碍被SCH 23390增强,且被D-1激动剂SKF 38393阻断。当对小鼠口服或腹腔注射SCH 23390时,与传统抗精神病药物相比,在阿扑吗啡攀爬拮抗作用和刻板性嗅探拮抗作用之间,SCH 23390显示出明显更宽的剂量间隔。D-1和D-2拮抗剂之间可能存在临床相关差异,D-1拮抗剂(以SCH 23390为例)引起锥体外系副作用的可能性较低,尽管可能并非可忽略不计。