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J Med Chem. 2008 Feb 28;51(4):1058-62. doi: 10.1021/jm7009606. Epub 2008 Jan 31.

Synthesis and pharmacological evaluation of 1,2-dihydrospiro[isoquinoline-4(3H),4'-piperidin]-3-ones as nociceptin receptor agonists.

Author information

1
Dipartimento del Farmaco, Istituto Superiore di Sanità, Viale Regina Elena 299, 00161 Roma, Italy. carlo.mustazza@iss.it

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.

PMID:
18232652
DOI:
10.1021/jm7009606
[Indexed for MEDLINE]

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