[在神经紧张素的背景下寻找具有抗精神病活性的小分子]。

Bioorganicheskaia khimiia Pub Date : 2012-01-01
R U Ostrovskaia, T A Gudasheva, N A Krupina, S B Seredin
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引用次数: 0

摘要

已知三肽神经紧张素(NT)在脑内给药时发挥神经安定剂样作用。以NT为背景构建了具有系统活性的酰基脯氨酸二肽基团,并选择了n -己丙基- l-脯氨酸- l-酪氨酸甲酯(Dilept)进行进一步开发。本文讨论了Dilept设计的主要原理,并分析了其对精神分裂症“翻译”模型的影响的实验数据-由多巴胺模拟物阿波啡或非竞争性nmda阻滞剂氯胺酮引起的声惊反应的脉冲前抑制缺陷。双肽被证明在腹腔和口服给药的情况下都能减轻这些缺陷。二苯乙酯被认为是一种潜在的抗精神病药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
[The search of small molecules with antipsychotic activity on the background of neurotensin].

Tridecapeptide neurotensin (NT) is known to exert the neuroleptic-like effects in case of its intracerebral administration. The group of systemically active dipeptides , acylprolyltyrosines, was constructed on the background of NT. Methyl ester of N-caproyl-L-prolyl-L-tyrosine (Dilept) was chosen for further development. The paper is dealing with main principles of Dilept'design and with analysis of the experimental data concerning its effect on the "translational" model of schizophrenia--the deficit of prepulse inhibition of the acoustic startle-reaction caused by either dopamine-mimetic, apomorphine, or by the uncompetitive NMDA-blocker, ketamine. Dilept was shown to attenuate these deficits both in case ofintraperitoneal and peroral administration. Dilept is considered as a potential antipsychotic.

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