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Sigma Receptor Binding Profile of a Series of Analgesic Tropane Derivatives
Archiv der Pharmazie ( IF 5.1 ) Pub Date : 2002-01-01 , DOI: 10.1002/1521-4184(200201)335:1<39::aid-ardp39>3.0.co;2-h
Orazio Prezzavento 1 , Fulvio Gualtieri , Agostino Marrazzo , Maria Novella Romanelli , Giuseppe Ronsisvalle , Elisabetta Teodori
Affiliation  

The binding profile on sigma receptor subtypes of a family of tropane derivatives, previously studied as analgesic and nootropic drugs, is reported. The results show that the sigma receptors are not involved in the enhancement of acetylcholine release and of the consequent analgesic activity of this class of drugs. Structure‐affinity relationships for σ receptor subtypes are discussed.They lead to the identification of a few useful leads for further development of potent sigma ligands within the series.

中文翻译:

一系列镇痛托烷衍生物的 Sigma 受体结合概况

报告了之前作为镇痛和促智药物研究的托烷衍生物家族的 sigma 受体亚型的结合特征。结果表明,σ 受体不参与乙酰胆碱释放的增强和此类药物随后的镇痛活性。讨论了 σ 受体亚型的结构-亲和力关系。它们导致确定了一些有用的先导物,以进一步开发该系列中的有效 sigma 配体。
更新日期:2002-01-01
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