[咪唑类H2激动剂：2-氨基取代对药理活性的重要性]

[Imidazolic H2-agonists: importance of 2-amino substitution for pharmacological activity].

作者信息

Morini G, Chiavarini M, Bordi F, Plazzi P V, Vitali F, Impicciatore M

出版信息

Boll Soc Ital Biol Sper. 1984 Apr 30;60(4):789-95.

Abstract

The results of 2-aminohistamine (compound I) and 2-amino-5-methylhistamine (compound II) on cat acid secretion and on guinea pig gall-bladder motility are described and compared with those of Histamine or Dimaprit. The compound (I) showed a greater H2- than H1-receptor stimulating activity, while compound (II), inactive on H1, was effective on H2-receptors, being endowed with a less "potency" and "efficacy" than compound (I). The pharmacological activities of both compounds, related to their chemical structure, are discussed.

摘要

本文描述了2-氨基组胺（化合物I）和2-氨基-5-甲基组胺（化合物II）对猫胃酸分泌和豚鼠胆囊运动的影响，并与组胺或二甲双胍的作用进行了比较。化合物（I）显示出比H1受体刺激活性更强的H2受体刺激活性，而化合物（II）对H1无活性，但对H2受体有效，其“效力”和“功效”均低于化合物（I）。文中还讨论了这两种化合物的药理活性与其化学结构之间的关系。