潜在的组胺H2受体拮抗剂。2. N-α-胍基组胺。
Potential histamine H2-receptor antagonists. 2. N-alpha-Guanylhistamine.
作者信息
Durant G J, Parsons M E, Black J W
出版信息
J Med Chem. 1975 Aug;18(8):830-3. doi: 10.1021/jm00242a014.
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.
激动剂分子组胺已被用作设计潜在H2受体拮抗剂的起点。将侧链氨基转化为胍基得到了首个组胺H2受体拮抗剂，Nα-胍基组胺。在高剂量水平（静脉注射时约ID50为800 μmol/kg）下，通过抑制大鼠组胺刺激的胃酸分泌，以及通过抑制豚鼠右心房组胺刺激的心动过速（pA2等于3.9），证实了H2受体拮抗作用。胍基组胺在组胺H2受体上表现为部分激动剂。
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