Synthesis and structure-activity relationships of a series of benzazepine derivatives as 5-HT2C receptor agonists.
Bioorg Med Chem
; 16(6): 3309-20, 2008 Mar 15.
Article
en En
| MEDLINE
| ID: mdl-18083579
ABSTRACT
To identify potent and selective 5-HT(2C) receptor agonists, a series of novel benzazepine derivatives were synthesized, and their structure-activity relationships examined. The compounds were evaluated for their 5-HT(2C), 5-HT(2A), and 5-HT(2B) receptor binding affinity and intrinsic activity for the 5-HT(2C) and 5-HT(2A) receptors. Among these compounds, 6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine (6) was effective in a rat penile erection model when administered po, which is a symptom of the serotonin syndrome reflecting 5-HT(2C) receptor activation. Moreover, compound 6 was characterized as a partial agonist of 5-HT(2A) receptors; therefore, it had little effect on the cardiovascular system.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Benzazepinas
/
Agonistas del Receptor de Serotonina 5-HT2
Límite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2008
Tipo del documento:
Article
País de afiliación:
Japón