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Immethridine is a potent histamine H3 receptor agonist (Ki = 0.85 nM).1 It is selective for histamine H3 over histamine H4 receptors (Ki = 245 nM). Immethridine inhibits cAMP-stimulated β-galactosidase transcription in SK-N-MC cells expressing human H3 receptors (EC50 = 0.18 nM) and induces a concentration-dependent decrease of the electrically induced twitch contraction in isolated guinea pig ileum. In vivo, immethridine (30 mg/kg, s.c.) inhibits hydrochloric acid-induced formation of gastric lesions in rats.2
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1. Identification of 4-
2. Histamine H3 receptors are involved in the protective effect of ghrelin against HCl-