Dénes B, Greeff K, Tawfik H
Arzneimittelforschung. 1982;32(3):201-7.
The effect of (+)- and (-)-tranylcypromine (TCP), (-)-deprenyl and pargyline was tested and the interaction of these MAO inhibitors with tyramine and noradrenaline was compared on the circulation of the cat and on the isolated guinea-pig atria. 1. Anesthetised cats: An i.v. injection of 1 mg/kg of (+)- as well as (-)-TCP leads to an increase in the blood pressure and dp/dtmax. This effect is getting weaker on repeated doses. (-)-Deprenyl and pargyline decrease blood pressure and dp/dtmax. After a preadministration of (+)-TCP or pargyline the effect of tyramine on the blood pressure and contractility is prolonged. (-)-TCP prolongs slightly the cardiac effect of tyramine and is less effective than (+)-TCP. (-)-Deprenyl does not influence the effect of tyramine. The noradrenaline effect is not affected by the MAO-inhibitors. 2. Conscious cats: An i.v. injection of (+)- as well as (-)-TCP increases the blood pressure and decreases the heart rate. Desipramine (DMI) blocks this effect. Preadministration of (+)- as well as (-)-TCP and pargyline, but not (-)-deprenyl, potentiates the effect of tyramine on the blood pressure. According to this activity one can arrange these MAO-inhibitors as follows: (+)-TCP greater than (-)-TCP greater than pargyline. 3. Atrial preparations of guinea pigs: (+)- and (-)-TCP have a positive inotropic effect at concentrations from 10(-6) to 10(-5) mol/l, which is blocked by bupranolol and DMI. A pretreatment with reserpine prevents the effect of (-)- and weakens that of (+)-TCP. (+)-TCP, pargyline and (-)-deprenyl potentiate the effect of tyramine, while that of noradrenaline is potentiated by (+)- as well as (-)-TCP and (-)-deprenyl.
测试了(+)-和(-)-反苯环丙胺(TCP)、(-)-司来吉兰和帕吉林的作用,并比较了这些单胺氧化酶(MAO)抑制剂与酪胺和去甲肾上腺素在猫的循环系统以及离体豚鼠心房上的相互作用。1. 麻醉猫:静脉注射1mg/kg的(+)-以及(-)-TCP会导致血压和dp/dtmax升高。重复给药后这种效应会减弱。(-)-司来吉兰和帕吉林会降低血压和dp/dtmax。预先给予(+)-TCP或帕吉林后,酪胺对血压和收缩性的作用会延长。(-)-TCP会轻微延长酪胺的心脏效应,且效果不如(+)-TCP。(-)-司来吉兰不影响酪胺的作用。去甲肾上腺素的作用不受MAO抑制剂影响。2. 清醒猫:静脉注射(+)-以及(-)-TCP会升高血压并降低心率。地昔帕明(DMI)会阻断这种效应。预先给予(+)-以及(-)-TCP和帕吉林,但不包括(-)-司来吉兰,会增强酪胺对血压的作用。根据这种活性,可以将这些MAO抑制剂排列如下:(+)-TCP>(-)-TCP>帕吉林。3. 豚鼠心房制备物:(+)-和(-)-TCP在浓度为10(-6)至10(-5)mol/l时具有正性肌力作用,这被布普洛尔和DMI阻断。用利血平预处理可防止(-)-TCP 的作用并减弱(+)-TCP的作用。(+)-TCP、帕吉林和(-)-司来吉兰会增强酪胺的作用,而去甲肾上腺素的作用则被(+)-以及(-)-TCP和(-)-司来吉兰增强。