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Bioorg Med Chem Lett
; 18(20): 5689-93, 2008 Oct 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-18799310
RESUMEN
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.