New high affinity H 3 receptor agonists without a basic side chain

R Kitbunnadaj, M Hoffmann, SA Fratantoni…

文献索引：Kitbunnadaj, Ruengwit; Hoffmann, Marcel; Fratantoni, Silvina A.; Bongers, Gerold; Bakker, Remko A.; Wieland, Kerstin; El Jilali, Ahmed; De Esch, Iwan J. P.; Menge, Wiro M. P. B.; Timmerman, Henk; Leurs, Rob Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 23 p. 6309 - 6323

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被引用次数: 13

摘要

In this study, we replaced the basic amine function of the known histamine H3 receptor agonists imbutamine or immepip with non-basic alcohol or hydrocarbon moieties. All compounds in this study show a moderate to high affinity for the cloned human H3 receptor and, unexpectedly, almost all of them act as potent agonists. Moreover, in the alcohol series, we consistently observed an increased selectivity for the human H3 receptor over the ...