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EnglishTwelve 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.
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| Data di pubblicazione: | 2009 | |
| Titolo: | Structure-activity studies on the nociceptin/orphanin FQ receptor antagonist 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4'-piperidin-1-yl]propyl} pyrrolidine-2-carboxamide. | |
| Autori: | Trapella C; Fischetti C; Pela' M; Lazzari I; Guerrini R; Calo' G; Rizzi A; Camarda V; Lambert DG; McDonald J; Regoli D; Salvadori S. | |
| Rivista: | BIOORGANIC & MEDICINAL CHEMISTRY | |
| Parole Chiave: | SAR studies; NOP receptor antagonists; Receptor and [35S]GTPγS binding; Mouse vas deferens; Calcium mobilization; Tail withdrawal assay | |
| 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. | |
| Digital Object Identifier (DOI): | 10.1016/j.bmc.2009.05.068 | |
| Handle: | http://hdl.handle.net/11392/536232 | |
| Appare nelle tipologie: | 03.1 Articolo su rivista |
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