Chemicopharmacological Studies on Antispasmodic Action. XII. Structure-Activity Relationship of Aralkylamines.

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Abstract
1. Fifty-eight aralkylamines were tested for atropine-like activity against acetylcholine-stimulated ileal strips of mice. 2. Papaverine-like activity of the aralkylamines was tested against excess acetylcholine-stimulated ileal strips of mice. 3. The relationship between chemical structure and pharmacological activity has been discussed. In almost all the compounds tested here, atropine-like activities change somewhat parallel with the papaverine-like activities of the compounds. The effect of quaternization of tertiary amines is the only exception, where the quaternary ammonium compounds have stronger atropine-like and weaker papaverine-like action than the corresponding tertiary amines. It is suggested that some physicochemical properties such as lipoid solubility would influence the papaverine-like activity and also participate even in intensifying the atropine-like antiacetylcholine activity.

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