泽替多林，一种在啮齿动物脑中无抗血清素能活性的特异性多巴胺拮抗剂。

Zetidoline, a specific dopamine antagonist devoid of antiserotonergic activity in rodent brain.

作者信息

Pugnetti P, Barone D, Peruzzi M, Restelli A

出版信息

Pharmacol Res Commun. 1985 Dec;17(12):1141-51. doi: 10.1016/0031-6989(85)90026-8.

Abstract

In the present study the interaction of zetidoline, a new antipsychotic, with the serotonergic system of the rodent brain was investigated in comparison with known neuroleptics. The pharmacological tests were L-5-hydroxytryptophan syndrome in mice and tryptamine-induced clonic seizures in rats. Biochemical tests were the in vitro binding of 3H-zetidoline to rat brain membranes and the serotonin metabolism and turnover in vivo in the rat cerebral cortex and brainstem. The results indicate that zetidoline, unlike haloperidol and chlorpromazine, at doses higher than those active on the dopaminergic system, shows no or very weak antiserotonergic activity in behavioral tests.

摘要

在本研究中，将新型抗精神病药物泽替多林与已知的抗精神病药物相比较，研究了其与啮齿动物脑内血清素能系统的相互作用。药理试验包括小鼠的L-5-羟色氨酸综合征和大鼠的色胺诱导的阵挛性惊厥。生化试验包括3H-泽替多林与大鼠脑膜的体外结合以及大鼠大脑皮层和脑干内血清素的体内代谢和周转。结果表明，与氟哌啶醇和氯丙嗪不同，泽替多林在高于对多巴胺能系统有活性的剂量时，在行为试验中没有或仅有非常微弱的抗血清素能活性。