GARRETT J, OSSWALD W, GONCALVES MOREIRA M
Br J Pharmacol Chemother. 1962 Feb;18(1):49-60. doi: 10.1111/j.1476-5381.1962.tb01149.x.
It has been suggested that heptaminol and methylheptaminol should be used as myocardial stimulants because they have cardiotonic actions similar to those of cardiac glycosides. However, as these aliphatic amines show definite sympathomimetic effects, the mechanism of their actions on the heart was investigated, in order to determine whether digitalis-like properties are involved in these effects. The pattern of pharmacological actions of heptaminol and methylheptaminol was compared with that of catechol amines, tyramine and k-strophanthin. The influence of atropine, hexamethonium, cocaine and reserpine was also investigated. The results show that both heptanolamines have a long-lasting cardiostimulant action which is abolished by cocaine and absent in reserpine pretreated animals. The pharmacological activity of these drugs may be entirely attributed to an indirect sympathomimetic action of the tyramine type, probably due to release of endogenous catechol amines. None of the experimental findings is consistent with the alleged digitalis-like action of these compounds.
有人提出,庚胺醇和甲基庚胺醇应用作心肌兴奋剂,因为它们具有与强心苷类似的强心作用。然而,由于这些脂肪族胺表现出明确的拟交感神经效应,因此对它们作用于心脏的机制进行了研究,以确定这些效应中是否涉及洋地黄样特性。将庚胺醇和甲基庚胺醇的药理作用模式与儿茶酚胺、酪胺和毒毛旋花子苷K的作用模式进行了比较。还研究了阿托品、六甲铵、可卡因和利血平的影响。结果表明,两种庚醇胺都有持久的心脏兴奋作用,这种作用可被可卡因消除,在利血平预处理的动物中则不存在。这些药物的药理活性可能完全归因于酪胺型的间接拟交感神经作用,可能是由于内源性儿茶酚胺的释放。没有任何实验结果与这些化合物所谓的洋地黄样作用一致。