| Literature DB >> 19527931 |
Claudio Trapella1, Carmela Fischetti, Michela Pela', Ilaria Lazzari, Remo Guerrini, Girolamo Calo', Anna Rizzi, Valeria Camarda, David G Lambert, John McDonald, Domenico Regoli, Severo Salvadori.
Abstract
Twelve derivatives of the nociceptin/orphanin FQ (N/OFQ) receptor (NOP) antagonist 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4'-piperidin-1-yl]propyl} pyrrolidine-2-carboxamide (Comp 24) were synthesized and tested in binding experiments performed on CHO(hNOP) cell membranes. Among them, a novel interesting NOP receptor antagonist (compound 35) was identified by blending chemical moieties taken from different NOP receptor ligands. In vitro in various assays, Compound 35 consistently behaved as a pure, highly potent (pA(2) in the range 8.0-9.9), competitive and NOP selective antagonist. However compound 35 was found inactive when challenged against N/OFQ in vivo in the mouse tail withdrawal assay. Thus, the usefulness of the novel NOP ligand compound 35 is limited to in vitro investigations.Entities:
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Year: 2009 PMID： 19527931 DOI： 10.1016/j.bmc.2009.05.068
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641