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盐酸双环胺对豚鼠和家兔膀胱尿道平滑肌解痉作用的体外研究

In vitro study of antispasmodic effects of dicyclomine hydrochloride on vesicourethral smooth muscle of guinea pig and rabbit.

作者信息

Khanna O P, DiGregorio G J, Barbieri E J, McMichael R, Ruch E

出版信息

Urology. 1979 Apr;13(4):457-62. doi: 10.1016/0090-4295(79)90360-1.

Abstract

Dicyclomine inhibition of acetylcholine-induced and barium chloride-induced isotonic contractions of the smooth muscle from three segments of the lower urinary tract (bladder body, bladder base, and proximal urethra) of the guinea pig and the rabbit was studied in vitro. In the guinea pig dicyclomine caused competitive inhibition of acetylcholine-induced contraction of the bladder body (1 x 10(-7) M to 1 x 10(-5) M) and the bladder base (1 x 10(-6) M, 1 X 10(-5) M) and was less potent than atropine and propantheline. In the rabbit significant blockade of acetylcholine-induced contractions occurred at dicyclomine concentrations of 5 x 10(-6) M to 3 x 10(-5) M in the bladder body and at 1 x 10(-5) M and 3 x 10(-5) M in the bladder base. In both species dicyclomine inhibitory effects were most marked in the bladder body, moderate in the bladder base, and minimal in the proximal urethra. Dicyclomine failed to cause inhibition of the barium chloride-induced contractions in the guinea pig vesicourethral smooth muscle. In rabbits, however, significant antagonism P less than 0.01) of barium chloride-induced muscle contraction was observed with dicyclomine at concentration 1 x 10(-5) M in both bladder body and the bladder base. The clinical implication of such properties of dicyclomine are discussed.

摘要

研究了双环维林对豚鼠和家兔下尿路三个节段(膀胱体、膀胱底部和近端尿道)平滑肌由乙酰胆碱诱导和氯化钡诱导的等张收缩的抑制作用。在豚鼠中,双环维林对乙酰胆碱诱导的膀胱体(1×10⁻⁷M至1×10⁻⁵M)和膀胱底部(1×10⁻⁶M、1×10⁻⁵M)收缩产生竞争性抑制,且效力低于阿托品和丙胺太林。在家兔中,双环维林浓度为5×10⁻⁶M至3×10⁻⁵M时,对膀胱体乙酰胆碱诱导的收缩有显著阻断作用,在膀胱底部,浓度为1×10⁻⁵M和3×10⁻⁵M时有显著阻断作用。在两个物种中,双环维林的抑制作用在膀胱体最明显,在膀胱底部中等,在近端尿道最小。双环维林未能抑制豚鼠膀胱尿道平滑肌中氯化钡诱导的收缩。然而,在家兔中,在膀胱体和膀胱底部,浓度为1×10⁻⁵M的双环维林对氯化钡诱导的肌肉收缩有显著拮抗作用(P<0.01)。讨论了双环维林这些特性的临床意义。

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