English T A, Gristwood R W, Owen D A, Wallwork J
Br J Pharmacol. 1986 Oct;89(2):335-40. doi: 10.1111/j.1476-5381.1986.tb10265.x.
The inotropic effects of impromidine have been studied and compared with those of histamine on human isolated left ventricular preparations stimulated at 1 Hz. Both drugs caused concentration-related increases in force of contraction and were of similar potency, although the maximum response to impromidine was markedly and significantly less than that to histamine. The positive inotropic responses of impromidine were inhibited by cimetidine 1 X 10(-5) M, consistent with histamine H2-receptor involvement. Impromidine 1 X 10(-4) M inhibited maximal responses to histamine to a level equal to the maximal impromidine response; however, impromidine did not inhibit responses to isoprenaline. Positive inotropic activity and inhibition of maximal responses to histamine occurred over a similar impromidine concentration-range. Impromidine displaced histamine concentration-response curves to the right, whereas mepyramine had no effect on responses to histamine. It is concluded that impromidine has positive inotropic activity on the human ventricle, that the response is mediated via histamine H2-receptors, and that impromidine is a partial agonist compared with histamine.
已对英普咪定的变力作用进行了研究,并将其与组胺对以1Hz频率刺激的人离体左心室标本的变力作用进行了比较。两种药物均引起与浓度相关的收缩力增加,且效力相似,尽管英普咪定的最大反应明显且显著低于组胺的最大反应。1×10⁻⁵M的西咪替丁可抑制英普咪定的正性变力反应,这与组胺H₂受体参与一致。1×10⁻⁴M的英普咪定可将组胺的最大反应抑制至与英普咪定最大反应相等的水平;然而,英普咪定并不抑制对异丙肾上腺素的反应。正性变力活性和对组胺最大反应的抑制作用在相似的英普咪定浓度范围内出现。英普咪定使组胺浓度-反应曲线右移,而美吡拉敏对组胺反应无影响。结论是,英普咪定对人心室具有正性变力活性,该反应通过组胺H₂受体介导,并且与组胺相比,英普咪定是一种部分激动剂。