Pharmacological Properties of Quaternary Atropinium Derivatives

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  • 四級アンモニウム型アトロピン誘導体の薬理作用について
  • 4級アンモニウム型アトロピン誘導体の薬理作用について
  • 4キュウ アンモニウムガタ アトロピン ユウドウタイ ノ ヤクリ サヨウ ニ

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Description

In order to examine how quaternization of atropine changes its pharmacological profile, five atropinium compounds (1a-e) were synthesized and subjected to examination for acute toxicity, mydriatic activity and antispasmodic activity by using the isolated guinea pig ileum and in situ ileum. The five atropinium compounds (1a-e) had lower anticholinergic activity than parent atropine. Among the five compounds, those introduced less bulky hydroxyalkyl groups to their nitrogen atom showed higher anticholinergic activity or larger pA2 values than the others. It was of special interest that spasmolytic activity of the atropinium derivatives evaluated by use of in situ ileum was much higher than that expected from their anticholinergic activity obtained by the isolated ileum, and even close to that of atropine. Toxicity of the atropinium compounds was somewhat similar to that of atropine. These results are suggestive that the quaternization of atropine does not favor reduction of toxicity and enhancement of anticholinergic activity but seems to introduce ganglion blocking activity. This study also suggests us that spasmolytic activity of drugs should be evaluated on the basis of their activity of inhibiting in situ ileum motility.

Journal

  • YAKUGAKU ZASSHI

    YAKUGAKU ZASSHI 105 (2), 183-187, 1985

    The Pharmaceutical Society of Japan

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