Antitussive Activity of Narcotine Derivatives

概要

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Antitussive action and general pharmacological properties were comparatively examined in narcotine derivatives, especially the steric isomers, i.e., l-α-and l-β-narcotine, and their N-oxides. l-β-Narcotine showed better antitussive effect than l-α-narcotine by chemical and mechanical stimulation methods using guinea pigs. The N-oxides of both l-α-and l-β-narcotines had better action than thier original salts and the antitussive action of l-β-narcotine N-oxide was more effective than that of dihydrocodeine when tested by the mechanical stimulation method. Both l-α-and l-β-narcotines showed some activity in tests of anti-acetylcholine action on frog rectus abdominis muscle, respiration and blood pressure of rabbits, relaxation and histamine antagonizing action on guinea pig smooth muscle, and acute toxicity of mice. These compounds had no effect of increasing the analgesic action in combination with morphine, inhibition of intestinal propulsion in mice, or constipative action. N-oxides of both l-α- and l-β-narcotines had weak or entirely no effect in these tests, except for a marked antitussive action and relaxation of tracheal muscle in comparatively high dosage.
公益社団法人日本薬学会の論文
1964-05-25