Synthesis and pharmacological evaluation of 1,2-dihydrospiro[isoquinoline-4(3H),4'-piperidin]-3-ones as nociceptin receptor agonists.
J Med Chem
; 51(4): 1058-62, 2008 Feb 28.
Article
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| MEDLINE
| ID: mdl-18232652
ABSTRACT
Some synthesized 1,2-dihydrospiro[isoquinoline-4(3 H),4'-piperidin]-3-ones were evaluated as ligands for nociceptin receptor (NOP receptor). Their affinity was established by binding studies, and efficacy was investigated by GTP binding experiments. Selectivity toward DOP, KOP, and MOP receptors was assessed, and structural requirements affecting affinity and selectivity were remarked. Most notably, compound 6d displayed nanomolar NOP receptor affinity and showed more than 800-fold selectivity. The new structures exerted full or partial agonistic activity.
Texto completo:
1
Base de datos:
MEDLINE
Asunto principal:
Piperidinas
/
Compuestos de Espiro
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Receptores Opioides
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Ciclohexanos
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Isoquinolinas
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
2008
Tipo del documento:
Article