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

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.