Tenner T E
Pharmacology. 1981;22(4):227-34. doi: 10.1159/000137494.
In an effort to compare the H2 receptors responsible for the chronotropic and vasorelaxant effects of histamine, rabbit right atria and aortae were studied using four H2 receptor agonists and the H2 receptor antagonist cimetidine. While the efficacies of the various agonists were not similar in the two tissues, the order of potency in both atria and aortae was impromidine greater than histamine greater than 4-methylhistamine greater than dimaprit. In addition, cimetidine, an H2 receptor antagonist, inhibited the chronotropic and relaxant effects of impromidine and histamine in a consistent fashion in both atria and aorta. The results obtained in the present study are consistent with the concept that the H2 receptors in rabbit atria and aortae represent one type of receptor and not two isoreceptors as is the case for beta-adrenergic receptors in these tissues.
为了比较介导组胺变时性和血管舒张作用的H2受体,使用四种H2受体激动剂和H2受体拮抗剂西咪替丁对兔右心房和主动脉进行了研究。虽然各种激动剂在两种组织中的效能不相似,但在心房和主动脉中,其效价顺序均为英普咪定大于组胺大于4-甲基组胺大于二甲双胍。此外,H2受体拮抗剂西咪替丁在心房和主动脉中均以一致的方式抑制英普咪定和组胺的变时性和舒张作用。本研究获得的结果与以下概念一致,即兔心房和主动脉中的H2受体代表一种受体类型,而不像这些组织中的β-肾上腺素能受体那样是两种异构受体。