Bastiaans H M, Donetti A, Kramer K, Bietti G, Cereda E, Dubini D, Mondini M, Bast A, Timmerman H
Department of Pharmacochemistry, Faculty of Chemistry, Vrije Universiteit, Amsterdam, The Netherlands.
Agents Actions. 1990 Apr;30(1-2):166-8. doi: 10.1007/BF01969028.
It has been hypothesized that bidentate hydrogen bonding plays an important role in the interaction of imidazolylphenylformamidines with the H2-receptor. The present study, in which the degree of pseudo-irreversible H2-antagonism of the four isomeric butyl substituted mifentidine analogues was determined on the spontaneously beating right atrium of the male guinea-pig, lends further support to this hypothesis. In solution the EE/EZ ratio is different for the four isomeric butylated mifentidine analogues. The rank order of the percentage of E,E conformation, which favors a bidentate interaction, of the formamidine moiety parallels the rank order of pseudo-irreversible H2-antagonism.
据推测，双齿氢键在咪唑基苯基甲脒与H2受体的相互作用中起重要作用。本研究测定了四种异构丁基取代米芬替丁类似物在雄性豚鼠自发性搏动右心房上的拟不可逆H2拮抗程度，为这一假说提供了进一步支持。在溶液中，四种异构丁基化米芬替丁类似物的EE/EZ比率不同。有利于双齿相互作用的甲脒部分的E,E构象百分比的排序与拟不可逆H2拮抗作用的排序平行。
