Isothiourea analogues of histamine as potent agonists or antagonists of the histamine H 3-receptor

H Van der Goot, MJP Schepers, GJ Sterk…

文献索引：Van der Goot; Schepers; Sterk; Timmerman European Journal of Medicinal Chemistry, 1992 , vol. 27, # 5 p. 511 - 517

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被引用次数: 142

摘要

Abstract The synthesis and H 3-activity of a series of isothiourea analogues of histamine have been described. It has been shown that S-[2-(4 (5)-imidazolyl) ethylisothiourea (VUF 8325) is a potent H 3-agonist measured as the electrically evoked contraction of the guinea- pig ileum. Upon methylation of the imidazole system or the isothiourea moiety a decrease in affinity was observed leading to potent H 3-antagonists. Particularly the 4-chlorobenzyl ...