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. 1990 May;100(1):150-2.
doi: 10.1111/j.1476-5381.1990.tb12067.x.

Hexocyclium derivatives with a high selectivity for smooth muscle muscarinic receptors

R Micheletti  1 , A Schiavone, E Cereda, A Donetti
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Hexocyclium derivatives with a high selectivity for smooth muscle muscarinic receptors

R Micheletti et al. Br J Pharmacol. 1990 May.

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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