Pharmacological profile of enantiomerically pure chiral muscarinic agonists: Desoxymuscarines

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• 作者：De Amici ; Marco ; Dallanoce ; Clelia ; De Micheli ; Carlo ; Angeli ; Piero ; Marucci ; Gabriella ; Cantalamessa ; Franco ; et. al.
• 关键词：Muscarinic receptor subtypes ; Muscarine enantiomers ; Desoxymuscarine enatinomers
• 刊名：Life Sciences
• 出版年：2000
• 期刊代码：62_00243205
• 类别：imm
• 出版时间：June 9, 2000
• 卷：67
• 期：3
• 页码：317-326
• 文件大小：134 K

摘要

The enantiomers desoxymuscarine 6 were tested in vitro on guinea pig tissues, and their muscarinic potency was evaluated at M₂ (heart force and rate) and M₃ (ileum and bladder) receptor subtypes together with the enantiomers of the parent compound muscarine 1. The eutomers (+)-1 and (+)-6 and distomers (−)-1 and (−)-6 were also assayed in vivo on pithed rat. Affinity, relative efficacy and enantioselectivity were also determined for the compounds under study at M₂ (heart force and rate) and M₃ (ileum and bladder), in order to investigate muscarinic receptor heterogeneity. The results of this study have been discussed in comparison with the data previously reported for the structurally related fluoromuscarine (+)-4 and difluoromuscarines (+)-5 and (−)-5.