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奥昔布宁(得妥)对兔逼尿肌的抗胆碱能及解痉活性研究。

A study of the anticholinergic and antispasmodic activity of oxybutynin (Ditropan) on rabbit detrusor.

作者信息

Fredericks C M, Anderson G F, Kreulen D L

出版信息

Invest Urol. 1975 Jan;12(4):317-9.

PMID:235500
Abstract

Experiments have been conducted which show that while the tertiary amine oxybutynin has only moderate in vitro anticholinergic and antihistaminic activity, it is a potent inhibitor of barium chloride-induced spasms of rabbit detrusor muscle. Oxybutynin exerts 1/13 the anticholinergic activity of propantheline and 1/4 that of atropine, but produces approximately 2x the inhibition of barium chloride-induced spasm than propantheline and 10x the inhibition produced by atropine. In sum, oxybutynin possesses a notable antispasmodic activity distinct from its anticholinergic activity and stronger than that of atropine, propantheline, or methantheline, which may prove useful in the treatment of smooth muscle hypermotility.

摘要

已进行的实验表明,虽然叔胺奥昔布宁仅具有中等程度的体外抗胆碱能和抗组胺活性,但它是氯化钡诱导的兔逼尿肌痉挛的有效抑制剂。奥昔布宁的抗胆碱能活性仅为丙胺太林的1/13和阿托品的1/4,但对氯化钡诱导的痉挛的抑制作用约为丙胺太林的2倍,阿托品的10倍。总之,奥昔布宁具有明显的抗痉挛活性,与其抗胆碱能活性不同,且比阿托品、丙胺太林或美索曲明更强,这可能在治疗平滑肌运动亢进方面有用。

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