3-(β-氨乙基)-1,2,4-三唑衍生物对组胺H1和H2受体的作用。

Effect of derivatives of 3-(beta-aminoethyl)-1,2,4-triazole on the histamine H1- and H2-receptors.

作者信息

Grechishkin L L, Gavrovskaya L K, Goldfarb V L

出版信息

Pharmacology. 1977;15(6):512-8. doi: 10.1159/000136729.

Abstract

Derivatives of 3-(beta-aminoethyl)-1,2,4-triazole similar to histamine have been resynthesized and studied. Four well-known effects of histamine have been considered (the contractions of an isolated guinea pig terminal ileum, dog gastric acid secretion, contractile frequency of an isolated guinea pig right atrium, blood pressure lowering effect in cats). Newly synthesized compounds IEM-813 and IEM-759 exerted some selective effects of H1 and H2-receptors: IEM-813 showed greater affinity for gut-isolated H1-receptors than for stomach and atrium H2-receptors, while IEM-759 mainly influenced H2-receptors. Accordingly, the influence of 1,2,4-triazole analogues on H1- and H2-receptors is subject to structural demands.

摘要

已重新合成并研究了与组胺类似的3-(β-氨乙基)-1,2,4-三唑衍生物。考察了组胺的四种已知效应（豚鼠离体终末回肠收缩、犬胃酸分泌、豚鼠离体右心房收缩频率、猫血压降低效应）。新合成的化合物IEM-813和IEM-759对H1和H2受体发挥了一些选择性作用：IEM-813对肠道分离的H1受体的亲和力高于对胃和心房H2受体的亲和力，而IEM-759主要影响H2受体。因此，1,2,4-三唑类似物对H1和H2受体的影响取决于结构要求。