Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists

…, R Loeffler, GW Gullikson, C Moummi…

文献索引：Becker, Daniel P.; Flynn, Daniel L.; Moormann, Alan E.; Nosal, Roger; Villamil, Clara I.; Loeffler, Richard; Gullikson, Gary W.; Moummi, Chafiq; Yang, Dai-C. Journal of Medicinal Chemistry, 2006 , vol. 49, # 3 p. 1125 - 1139

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被引用次数: 35

摘要

A series of pyrrolizidine esters, amides, and ureas was prepared and tested for 5-HT4 and 5- HT3 receptor binding, 5-HT4 receptor agonism in the rat tunica muscularis mucosae (TMM) assay, and for 5-HT3 receptor-mediated functional antagonism in the Bezold-Jarisch reflex assay. Several pyrrolizidine derivatives were identified with high affinity for the 5-HT4 receptor, including benzamide 12a (SC-53116), a potent and selective 5-HT4 partial ...