N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist

…, A Yamatodani, G Coruzzi, H Timmerman…

文献索引：Kitbunnadaj, Ruengwit; Hashimoto, Takeshi; Poli, Enzo; Zuiderveld, Obbe P.; Menozzi, Alessandro; Hidaka, Ryoko; De Esch, Iwan J. P.; Bakker, Remko A.; Menge, Wiro M. P. B.; Yamatodani, Atsushi; Coruzzi, Gabriella; Timmerman, Henk; Leurs, Rob Journal of Medicinal Chemistry, 2005 , vol. 48, # 6 p. 2100 - 2107

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被引用次数: 42

摘要

In this study, we continue our efforts toward the development of potent and highly selective histamine H3 receptor agonists. We introduced various alkyl or aryl alkyl groups on the piperidine nitrogen of the known H3/H4 agonist immepip and its analogues (1-3a). We observed that N-methyl-substituted immepip (methimepip) exhibits high affinity and agonist activity at the human histamine H3 receptor (p K i= 9.0 and pEC50= 9.5) with a 2000-fold ...