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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。

相似文献

1
A study of the anticholinergic and antispasmodic activity of oxybutynin (Ditropan) on rabbit detrusor.奥昔布宁(得妥)对兔逼尿肌的抗胆碱能及解痉活性研究。
Invest Urol. 1975 Jan;12(4):317-9.
2
Characterization of the oxybutynin antagonism of drug-induced spasms in detrusor.奥昔布宁对逼尿肌药物诱导痉挛的拮抗作用特征
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Comparison of the antimuscarinic and antispasmodic actions of racemic oxybutynin and desethyloxybutynin and their enantiomers with those of racemic terodiline.消旋奥昔布宁、去乙基奥昔布宁及其对映体与消旋特罗地林的抗毒蕈碱和抗痉挛作用比较。
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引用本文的文献

1
Differences in the effects of urinary incontinence agents S-oxybutynin and terodiline on cardiac K(+) currents and action potentials.尿失禁药物S-奥昔布宁和特罗地林对心脏钾离子电流及动作电位影响的差异
Br J Pharmacol. 2000 Sep;131(2):245-54. doi: 10.1038/sj.bjp.0703595.
2
The use of oxybutynin in urological practice.奥昔布宁在泌尿外科实践中的应用。
Int Urol Nephrol. 1987;19(4):385-91. doi: 10.1007/BF02550355.
3
The pharmacokinetics of oxybutynin in man.奥昔布宁在人体中的药代动力学。
Eur J Clin Pharmacol. 1988;35(5):515-20. doi: 10.1007/BF00558247.