Dimaprit, (S-[3-(N,N-dimethylamino)propyl]isothiourea). A highly specific histamine H2-receptor agonist. Part 2. Structure-activity considerations.
作者： G. J. Durant , C. R. Ganellin , M. E. Parsons
DOI: 10.1007/BF01964879
关键词: Dimaprit 、 Imidazole 、 Tautomer 、 Stereochemistry 、 Receptor 、 Agonist 、 Chemistry 、 Structure–activity relationship 、 Histamine H2 receptor 、 Histamine
摘要: Dimaprit, S-[3-(N,N-dimethylamino)propyl]isothiourea, appears to be a highly specific histamine H2-receptor agonist. Further indications of specificity are obtained from chemical considerations. Dimaprit has two basic centres (pKa values respectively 8.23 and 9.23, at 40°.) pH 7.4 about 5% the molecules will present as monocation analogous monocation. Chemical comparison suggests that −N+HMe2 group corresponds −N+H3 histamine, isothiourea dimaprit (which can undergo 1,3-prototropic tautomerism) may simulate imidazole ring function proton transfer agent H2 receptors.
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