丙咪嗪、奥昔布宁和黄酮哌酯对兔逼尿肌的体外比较效应

Comparative in vitro effects of imipramine, oxybutynin, and flavoxate on rabbit detrusor.

作者信息

Fredericks C M, Green R L, Anderson G F

出版信息

Urology. 1978 Oct;12(4):487-91. doi: 10.1016/0090-4295(78)90312-6.

Abstract

The ability of imipramine, oxybutynin, and flavoxate to antagonize carbamylcholine and barium chloride (BaCl2)-induced contractions of rabbit detrusor, and to block impulse conduction in desheathed frog sciatic nerves has been assessed in vitro. Impiramine exerts noncompetitive carbamylcholine and BaCl2 blockade by 10(-5) M and a local anesthetic effect equipotent with that of tetracaine. Oxybutynin exerts a strong competitive antagonism of carbamylcholine by 10(-8) M, a noncompetitive antagonism of BaCl2 equivalent to that of imipramine, and moderate local anesthetic activity. Flavoxate, under these experimental conditions exerts little anticholinergic, antispasmodis, or local anesthetic activity. Imipramine and oxybutynin thus demonstrate a number of smooth muscle effects by which their therapeutic actions may be exerted. The mechanisms of action of flavoxate remain obscure.

摘要

已在体外评估了丙咪嗪、奥昔布宁和黄酮哌酯拮抗氨甲酰胆碱和氯化钡（BaCl₂）诱导的兔逼尿肌收缩以及阻断去鞘青蛙坐骨神经冲动传导的能力。丙咪嗪通过10⁻⁵M发挥非竞争性氨甲酰胆碱和BaCl₂阻断作用，其局部麻醉作用与丁卡因相当。奥昔布宁通过10⁻⁸M对氨甲酰胆碱发挥强烈的竞争性拮抗作用，对BaCl₂的非竞争性拮抗作用与丙咪嗪相当，且具有中等程度的局部麻醉活性。在这些实验条件下，黄酮哌酯几乎不发挥抗胆碱能、解痉或局部麻醉活性。因此，丙咪嗪和奥昔布宁表现出多种平滑肌效应，它们可能通过这些效应发挥治疗作用。黄酮哌酯的作用机制仍不清楚。