Maggi C A, Meli A
J Pharmacol Methods. 1984 Sep;12(2):91-6. doi: 10.1016/0160-5402(84)90026-3.
A new in vivo procedure suitable for testing the smooth muscle relaxant properties of a test substance is described. Topical eserine produced a long-lasting steady increase in tone of guinea pig distal colon and enhanced the atropine-sensitive phasic activity. Intravenously administered atropine, pirenzepine, and dicyclomine (which possess competitive antimuscarinic properties) produced a dose-related inhibition of eserine-induced muscle tone and suppressed phasic contractions. On the other hand, verapamil and octylonium bromide (which produce smooth muscle relaxation by interfering with Ca++ availability for contraction) did not suppress phasic contraction although they were fully effective in inhibiting eserine-induced tone. The eserine-induced contraction of guinea pig distal colon appears to be a suitable, quick, and inexpensive test for evaluating the effects of potential smooth muscle relaxants against background hypermotility produced by amplifying the neurogenic drive to the target organ.
描述了一种适用于测试受试物质平滑肌松弛特性的新的体内实验方法。局部应用毒扁豆碱可使豚鼠远端结肠张力持续稳定升高，并增强对阿托品敏感的相性活动。静脉注射阿托品、哌仑西平和双环维林（具有竞争性抗毒蕈碱特性）可产生与剂量相关的对毒扁豆碱诱导的肌张力的抑制作用，并抑制相性收缩。另一方面，维拉帕米和溴化奥替溴铵（通过干扰收缩所需的钙离子供应来产生平滑肌松弛）虽然能完全有效抑制毒扁豆碱诱导的张力，但并未抑制相性收缩。毒扁豆碱诱导的豚鼠远端结肠收缩似乎是一种合适、快速且廉价的测试方法，用于评估潜在平滑肌松弛剂对通过增强对靶器官的神经源性驱动而产生的背景性运动亢进的影响。
