YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
鎮痙薬の薬理学的研究(第1報)Diarylmethylene-5-methyl-transquinolizidinium Bromide類の鎮痙作用への選択性
久保 信治森川 宏二山崎 光雄笠松 貞夫越中 栄一加藤 日出男
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1981 年 101 巻 2 号 p. 174-181

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Pharmacological properties of 3-(di-2-thienylmethylene)-5-methyl-trans-quinolizidinium bromide (HSR-902), 2-(di-2-thienylmethylene)-5-methyl-trans-quinolizidinium bromide (HSR-911), 3-diphenylmethylene-5-methyl-trans-quinolizidinium bromide (HSR-405) and 2-diphenylmethylene-5-methyl-trans-quinolizidinium bromide (HSR-402), new antispasmodic agents, were compared with those of atropine and butylscopolamine bromide, and the following results were obtained. These antispasmodic agents shifted the dose-response curve of acetylcholine chloride (ACh) in parallel to the right without decreasing the maximal response in isolated guinea pig ileum, and the plots of Schild were found to be linear. The order of potency to antagonize the spontaneous motility of guinea pig ileum was as follows : HSR-911≒atropine>HSR-402>HSR-902»HSR-405> butylscopolamine bromide. The order of potency to antagonize the contraction of rat stomach induced by vagus nerve stimulation was as follows : HSR-911>HSR-402>HSR-902»HSR-405>atropine»butylscopolamine bromide. The order of potency to mydriatic activity of rat or mouse was as follows : atropine>HSR-911≒HSR-402»HSR-405>HSR-902>butylscopolamine bromide. The order of potency to inhibit pilocarpine induced salivation of guinea pig or mouse was as follows : atropine»HSR-911>HSR-402>HSR-902>HSR-405>butylscopolamine bromide. These results indicated that antagonisms of these antispasmodic agents against ACh were competitive, and the selectivity to antispasmodic activity of HSR-902 might be the highest among these antispasmodic agents including atropine and butylscopolamine bromide.

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