2‐{4‐[ω‐[4‐(2‐甲氧基苯基)‐1‐哌嗪基]烷氧基]苯基}‐2H‐苯并三唑及其N -氧化物作为某些5‐羟色胺、多巴胺和肾上腺素受体亚型的配体

A. Sparatore, F. Sparatore
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引用次数: 3

摘要

我们制备并研究了一些新的2-甲氧基苯基哌嗪衍生物作为5-羟色胺5-HT1A和多巴胺D3受体亚型的组合配体。化合物对5-HT1A和D3受体的亲和力随着中间脂肪链的延长而增强。相反,与5-HT2A、D2和α1受体亚型的结合受链长度的影响不规则,且主要为阴性。与5-HT2A、D2和α1受体相比,含4-5个亚甲基的苯并三唑衍生物对5-HT1A和D3具有良好或极好的选择性。
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2‐{4‐[ω‐[4‐(2‐Methoxyphenyl)‐1‐piperazinyl]alkoxy]phenyl}‐ 2H‐benzotriazoles and their N‐Oxides as Ligands for some 5‐Hydroxytryptamine, Dopamine and Adrenergic Receptor Subtypes
We have prepared and studied some new 2-methoxyphenylpiperazine derivatives as combined ligands for 5-hydroxytryptamine 5-HT1A and dopamine D3 receptor subtypes. The compounds displayed affinity for 5-HT1A and D3 receptors, which improved with the lengthening of the intermediate aliphatic chain. Conversely, binding to 5-HT2A, D2 and α1-receptor subtypes was affected in an irregular, and mainly negative, manner by the chain length. Benzotriazole derivatives with 4–5 methylenes exhibited good or excellent selectivity for 5-HT1A and D3 vs 5-HT2A, D2 and α1-receptors.
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