Potent, selective tetrahydro-beta-carboline antagonists of the serotonin 2B (5HT2B) contractile receptor in the rat stomach fundus.
J Med Chem
; 39(14): 2773-80, 1996 Jul 05.
Article
em En
| MEDLINE
| ID: mdl-8709108
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.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Antagonistas da Serotonina
/
Carbolinas
/
Receptores de Serotonina
/
Músculo Liso
Limite:
Animals
Idioma:
En
Revista:
J Med Chem
Ano de publicação:
1996
Tipo de documento:
Article