Ginos J Z, Doroski D
J Pharmacol Exp Ther. 1979 Apr;209(1):79-86.
N-Methyl-1,2,3,4-tetrahydroisoquinoline (MTIQ) antagonized apomorphine (APO)-induced stereotypy in a dose-related manner when injected i.p. in rats and attenuated L-dopa-induced hyperactivity in mice. 1,2,3,4-Tetrahydroisoquinoline (TIQ) and its homolog, N-n-propyl-, also blocked APO-induced stereotypy when given similarly. No significant difference was found between the amounts of radioactivity in the brain homogenates of MTIQ- and saline-pretreated rats after injection with [3H] APO. This suggested that MTIQ did not antagonize the behavioral effects of APO by blocking its entry into the brain. Mice fed ad libitum for 90 days with Purina Chow mixed with TIQ (5.0 mg/g) displayed behavioral supersensitivity in comparison with controls when injected with L-dopa (0.40 g/kg i.p.) after pretreatment with carbidopa. This was parallelled by a significant increase of dopamine-related adenylate cyclase activity measured in homogenates of caudate nuclei. The similarity between the behavioral effects induced by some neuroleptics and those observed with TIQ and its homologs suggests that the latter may be a new class of short-acting neuroleptics.
N-甲基-1,2,3,4-四氢异喹啉（MTIQ）腹腔注射给大鼠时，能以剂量相关的方式拮抗阿扑吗啡（APO）诱导的刻板行为，并减弱左旋多巴诱导的小鼠多动。1,2,3,4-四氢异喹啉（TIQ）及其同系物N-正丙基-以类似方式给药时，也能阻断APO诱导的刻板行为。注射[3H]APO后，MTIQ预处理组和生理盐水预处理组大鼠脑匀浆中的放射性量无显著差异。这表明MTIQ并非通过阻止APO进入脑内来拮抗其行为效应。用含TIQ（5.0 mg/g）的普瑞纳饲料随意喂养90天的小鼠，在用卡比多巴预处理后腹腔注射左旋多巴（0.40 g/kg）时，与对照组相比表现出行为超敏性。这与尾状核匀浆中测得的多巴胺相关腺苷酸环化酶活性显著增加相平行。一些抗精神病药物诱导的行为效应与TIQ及其同系物观察到的效应相似，这表明后者可能是一类新型的短效抗精神病药物。
