Hexocyclium derivatives with a high selectivity for smooth muscle muscarinic receptors. |
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Authors: | R. Micheletti A. Schiavone E. Cereda A. Donetti |
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Affiliation: | Department of Pharmacology, Istituto De Angeli, Milano, Italy. |
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Abstract: | 1. The affinity of a number of derivatives of the muscarinic antagonist, hexocyclium, containing an amidine cationic head, for guinea-pig cardiac and ileal receptors was investigated. 2. All the compounds studied displayed a greater affinity for muscular than for cardiac muscarinic receptors. 3. The 5 fold ileal selectivity of hexocyclium was increased by a number of chemical substitutions. The largest discrimination between receptors (about 200 fold) was found for the formamidine derivative. 4. The selectivity displayed by the hexocyclium derivatives stemmed from a greater decrease in affinity towards cardiac as compared to ileal receptors. |
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