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.

Trapella, C; Fischetti, C; Pela', M; Lazzari, I; Guerrini, R; Calo', G; Rizzi, A; Camarda, V; Lambert, Dg; Mcdonald, J; Regoli, D; Salvadori, S.

doi:10.1016/j.bmc.2009.05.068

CINECA IRIS Institutional Research Information System

IRIS è la soluzione IT che facilita la raccolta e la gestione dei dati relativi alle attività e ai prodotti della ricerca. Fornisce a ricercatori, amministratori e valutatori gli strumenti per monitorare i risultati della ricerca, aumentarne la visibilità e allocare in modo efficace le risorse disponibili.

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.

Scheda prodotto non validato

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo

Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11392/536232

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 interni:	TRAPELLA, Claudio FISCHETTI, Carmela PELA', Michela LAZZARI, Ilaria GUERRINI, Remo CALO', Girolamo RIZZI, Anna CAMARDA, Valeria REGOLI, Domenico SALVADORI, Severo
Data di pubblicazione:	2009
Rivista:	BIOORGANIC & MEDICINAL CHEMISTRY
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.
Handle:	http://hdl.handle.net/11392/536232
Appare nelle tipologie:	03.1 Articolo su rivista

File in questo prodotto:

Non ci sono file associati a questo prodotto.

Citazioni
ND
ND

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.