| Literature DB >> 8709108 |
J E Audia1, D A Evrard, G R Murdoch, J J Droste, J S Nissen, K W Schenck, P Fludzinski, V L Lucaites, D L Nelson, M L Cohen.
Abstract
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 KBS > 10.0 have been obtained). These high-affinity tetrahydro-beta-carboline antagonists are able to discriminate among the 5HT2 family of serotonin receptors, with members of the series showing selectivities of more than 100-fold versus both the 5HT2A and 5HT2C receptors based upon radioligand binding and functional assays. As the first compounds reported with such selectivity and enhanced receptor affinity, these tetrahydro-beta-carboline antagonists are useful tools for elucidating the role of serotonin acting at the 5HT2B receptor in normal and disease physiology.Entities:
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Year: 1996 PMID： 8709108 DOI： 10.1021/jm960062t
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446