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黄酮哌酯抗痉挛活性机制的体外比较研究。

Mechanism of flavoxate antispasmodic activity comparative in vitro studies.

作者信息

Cazzulani P, Panzarasa R, De Stefani C, Graziani G

出版信息

Arch Int Pharmacodyn Ther. 1985 Apr;274(2):189-200.

PMID:4026456
Abstract

In order to clarify the pharmacological activity of flavoxate, its effect on the tone and spontaneous activity of the guinea-pig isolated ureter and of the muscle strip from rat urinary bladder were studied. Flavoxate, as well as papaverine, reduced all three parameters considered on the guinea-pig isolated ureter, namely: peristaltic motility, endoluminal pressure and longitudinal muscle contractility. In the same test, verapamil (a calcium antagonist), emepronium and atropine (both anticholinergic drugs) were used for comparison. Using strips of rat urinary bladder depolarized by KCl, flavoxate, papaverine and verapamil displayed a relaxant activity, while anticholinergic compounds such as atropine, hyoscine and emepronium failed to relax this tissue. In another series of experiments the effects of flavoxate and anticholinergic drugs on the contraction elicited by vagal electrical stimulation of the guinea-pig isolated stomach in toto were assayed. The results obtained suggest that the action of flavoxate is due to direct smooth muscle relaxation and does not involve anticholinergic activity.

摘要

为阐明黄酮哌酯的药理活性,研究了其对豚鼠离体输尿管以及大鼠膀胱肌条的张力和自发活动的影响。黄酮哌酯与罂粟碱一样,降低了豚鼠离体输尿管所考察的三个参数,即:蠕动性、腔内压力和纵肌收缩性。在同一试验中,使用维拉帕米(一种钙拮抗剂)、依美溴铵和阿托品(两种抗胆碱能药物)作为对照。使用经氯化钾去极化的大鼠膀胱肌条,黄酮哌酯、罂粟碱和维拉帕米表现出舒张活性,而抗胆碱能化合物如阿托品、东莨菪碱和依美溴铵则不能使该组织舒张。在另一系列实验中,测定了黄酮哌酯和抗胆碱能药物对豚鼠离体全胃迷走神经电刺激所引起的收缩的影响。所得结果表明,黄酮哌酯的作用是由于直接使平滑肌舒张,而不涉及抗胆碱能活性。

相似文献

1
Mechanism of flavoxate antispasmodic activity comparative in vitro studies.黄酮哌酯抗痉挛活性机制的体外比较研究。
Arch Int Pharmacodyn Ther. 1985 Apr;274(2):189-200.
2
Pharmacological studies on the mode of action of flavoxate.黄酮哌酯作用方式的药理学研究。
Arch Int Pharmacodyn Ther. 1984 Apr;268(2):301-12.
3
Effects of terflavoxate on stimulated contractions of urinary bladder in vitro.
Arzneimittelforschung. 1993 Feb;43(2):122-8.
4
Effects of the anticholinergic drug prifinium bromide on urinary bladder contractions in rat in vivo and in guinea-pig in vitro.
Arzneimittelforschung. 1991 Apr;41(4):417-20.
5
Pharmacological activities of the main metabolite of flavoxate 3-methylflavone-8-carboxylic acid.黄酮哌酯主要代谢产物3-甲基黄酮-8-羧酸的药理活性。
Arzneimittelforschung. 1988 Mar;38(3):379-82.
6
Effects of propiverine hydrochloride on the spontaneous contractions of isolated guinea-pig urinary bladder strip and rhythmic urinary bladder contractions of anesthetized dog.
Arzneimittelforschung. 1992 Dec;42(12):1459-61.
7
Pharmacological characterisation of the smooth muscle antispasmodic agent tiropramide.平滑肌解痉剂替罗哌胺的药理学特性
Arzneimittelforschung. 1989 Sep;39(9):1114-9.
8
Pharmacological properties of tiropramide, an antispasmodic drug.
Gen Pharmacol. 1989;20(3):335-9. doi: 10.1016/0306-3623(89)90269-3.
9
The anticholinergic activity of agents indicated for urinary incontinence is an important property for effective control of bladder dysfunction.用于治疗尿失禁的药物的抗胆碱能活性是有效控制膀胱功能障碍的一项重要特性。
J Pharmacol Exp Ther. 1989 Nov;251(2):586-93.
10
Bladder muscle contractility. Comparative effects and mechanisms of action of atropine, propantheline, flavoxate, and imipramine.膀胱肌肉收缩力。阿托品、丙胺太林、黄酮哌酯及丙咪嗪的比较效应与作用机制。
Urology. 1977 Jan;9(1):31-5. doi: 10.1016/0090-4295(77)90279-5.

引用本文的文献

1
Flavoxate in urogynecology: an old drug revisited.黄酮哌酯在泌尿妇科中的应用:一种旧药的新审视。
Int Urogynecol J. 2015 Jul;26(7):959-66. doi: 10.1007/s00192-014-2585-5. Epub 2014 Dec 6.
2
Current concepts in the treatment of disorders of micturition.排尿障碍治疗的当前概念
Drugs. 1988 Apr;35(4):477-94. doi: 10.2165/00003495-198835040-00006.