唑替平抗躁狂作用与5HT1受体活性的可能关系。

T Harada, T Ebara, S Otsuki
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引用次数: 5

摘要

佐替平(ZTP)是藤泽制药有限公司(Fujisawa Pharmaceutical Co.)合成的一种可能用作抗精神病药物的药物,临床上具有非常迅速和有效的抗躁狂作用。为了阐明zotepine的精神药理学机制,我们试图测量ZTP与其他抗精神病药物在大脑中与多巴胺、5-羟色胺(5- ht1,5 - ht2)、去甲肾上腺素(NA)和乙酰胆碱相关的结合位点竞争的效力。在试验药物中,佐替平对5HT1受体的活性最强。氯丙嗪和噻嗪属于吩噻嗪类,临床抗躁狂作用较弱,它们对NA受体的活性与ZTP相同,但对5HT1受体的活性低于ZTP。这些结果表明药物对5HT1受体的活性可能与抗躁狂作用有关。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Possible relationship between antimanic effect and activity of zotepine to 5HT1 receptor.

Zotepine (ZTP), synthesized by Fujisawa Pharmaceutical Co., Ltd. for possible use as an antipsychotic drug, clinically features a very rapid and potent antimanic effect. To elucidate the psychopharmacological mechanisms of zotepine, we have attempted to measure the potency of ZTP compared with other neuroleptic drugs in competing for binding sites in the brain associated with dopamine, serotonin (5-HT1, 5-HT2), noradrenaline (NA) and acetylcholine. Zotepine was found to have the most potent activity to the 5HT1 receptor among the test drugs. Chlorpromazine and thioridazine, which belong to phenothiazines and clinically have less potent antimanic effect, shared ZTP's potent activity to the NA receptor, while they were less potent than ZTP in activity to the 5HT1 receptor. These results show that the activity of the drugs to the 5HT1 receptor may be associated with the antimanic effect.

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