1.
J Med Chem
; 47(3): 519-29, 2004 Jan 29.
Artículo
en Inglés
| MEDLINE
| ID: mdl-14736234
RESUMEN
We have previously described a series of antagonists that showed high potency and selectivity for the NK(1) receptor. However, these compounds also had the undesirable property of existing as a mixture of interconverting rotational isomers. Here we show that alteration of the 2-naphthyl substituent can modulate the rate of isomer exchange. Comparisons of the NK(1) receptor affinity for the various conformational forms has facilitated the development of a detailed NK(1) pharmacophore model.