Potent, selective tetrahydro-β-carboline antagonists of the serotonin 2B (5HT2B) contractile receptor in the rat stomach fundus

…, KW Schenck, P Fludzinski, VL Lucaites…

文献索引：Audia, James E.; Evrard, Deborah A.; Murdoch, Gwyn R.; Droste, James J.; Nissen, Jeffrey S.; Schenck, Kathy W.; Fludzinski, Pawel; Lucaites, Virginia L.; Nelson, David L.; Cohen, Marlene L. Journal of Medicinal Chemistry, 1996 , vol. 39, # 14 p. 2773 - 2780

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被引用次数: 128

摘要

A series of potent, selective 5HT2B receptor antagonists has been identified based upon yohimbine, with SAR studies resulting in a 1000-fold increase in 5HT2B receptor affinity relative to the starting structure (-log K Bs> 10.0 have been obtained). These high-affinity tetrahydro-β-carboline antagonists are able to discriminate among the 5HT2 family of serotonin receptors, with members of the series showing selectivities of more than 100- ...