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 enantio-selectivity 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. (C) 2000 Elsevier Science Inc.

Pharmacological profile of enantiomerically pure chiral muscarinic agonists - Desoxymuscarines / M. De Amici, C. Dallanoce, C. De Micheli, P. Angeli, G. Marucci, F. Cantalamessa, L. Sparapassi. - In: LIFE SCIENCES. - ISSN 0024-3205. - 67:3(2000), pp. 317-326.

Pharmacological profile of enantiomerically pure chiral muscarinic agonists - Desoxymuscarines

M. De Amici;C. Dallanoce;C. De Micheli;
2000

Abstract

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 enantio-selectivity 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. (C) 2000 Elsevier Science Inc.
Settore CHIM/08 - Chimica Farmaceutica
LIFE SCIENCES
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2434/183392
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