Pharmacological profile of enantiomerically pure chiral muscarinic agonists - Desoxymuscarines

The enantiomers desoxymuscarine 6 were tested in vitro on guinea pig tissue s, and their muscarinic potency was evaluated at M-2 (heart force and rate) and M-3 (ileum and bladder) receptor subtypes together with the enantiomer s of the parent compound muscarine 1. The eutomers (+)-1 and (+)-6 and dist omers (-)-1 and (-)-6 were also assayed in vivo on pithed rat. Affinity, re lative efficacy and enantioselectivity were also determined for the compoun ds under study at M-2 (heart force and rate) and M-3 (ileum and bladder), i n order to investigate muscarinic receptor heterogeneity. The results of th is study have been discussed in comparison with the data previously reporte d for the structurally related fluoromuscarine (+)-4 and difluoromuscarines (+)-5 and (-)-5, (C) 2000 Elsevier Science Inc. All rights reserved.