Identification and SAR around N-{2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide, a selective alpha2C adrenergic receptor antagonist.
Bioorg Med Chem Lett
; 18(20): 5689-93, 2008 Oct 15.
Article
em En
| MEDLINE
| ID: mdl-18799310
ABSTRACT
The discovery of the CNS-penetrant and selective alpha(2C) adrenergic receptor antagonist N-{2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide, 13 is described. Structure-activity studies demonstrate the structural requirements for binding affinity, functional activity, and selectivity over other alpha(2)-AR subtypes.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Azepinas
/
Niacinamida
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Antagonistas de Receptores Adrenérgicos alfa 2
Tipo de estudo:
Diagnostic_studies
Limite:
Animals
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Humans
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Male
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article