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  • Title: Potential histamine H2-receptor antagonists. 2. N-alpha-Guanylhistamine.
    Author: Durant GJ, Parsons ME, Black JW.
    Journal: J Med Chem; 1975 Aug; 18(8):830-3. PubMed ID: 240023.
    Abstract:
    The agonist molecule, histamine, has been used as a starting point for the design of potential H2-receptor antagonists. Converting the side-chain amino group into a guanidine yielded the first histamine H2-receptor antagonist, Nalpha-guanylhistamine. Antagonism of H2 receptors was demonstrated by the inhibition of histamine-stimulated gastric acid secretion in the rat at high dose levels (approximate ID50 800 MUmol/kg, iv) and by the inhibition of histamine-stimulated tachycardia of guinea-pig right atrium (pA2 equals 3.9). Guanylhistamine behaves as a partial agonist at histamine H2 receptors.
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