Indanyl piperazines as melatonergic MT2 selective agents.
Bioorg Med Chem Lett
; 13(6): 1199-202, 2003 Mar 24.
Article
en En
| MEDLINE
| ID: mdl-12643943
ABSTRACT
Optimization of a benzyl piperazine pharmacophore produced N-acyl-4-indanyl-piperazines that bind with high affinity to melatonergic MT(2) receptors. (R)-4-(2,3-dihydro-6-methoxy-1H-inden-1-yl)-N-ethyl-1-piperazine-carboxamide fumarate (13) is a water soluble, selective MT(2) agonist, which produces advances in circadian phase in rats at doses of 1-56 mg/kg that are no different from those of melatonin at 1 mg/kg. Unlike melatonin, 13 produced only weak contractile effects in rat tail artery.
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Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Piperazinas
/
Receptores Citoplasmáticos y Nucleares
/
Receptores de Superficie Celular
Límite:
Animals
/
Humans
/
Male
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2003
Tipo del documento:
Article
País de afiliación:
Estados Unidos