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UFP-101, a peptide antagonist selective for the nociceptin/orphanin FQ receptor.
CNS Drug Rev. 2005 Summer; 11(2):97-112.CD

Abstract

Nociceptin/orphanin FQ modulates various biological functions at central and peripheral levels by selectively activating a G-protein coupled receptor named N/OFQ peptide (NOP) receptor. For extending our knowledge on the biological roles of the N/OFQ-NOP receptor system the identification of selective NOP ligands, especially antagonists, is mandatory. [Nphe1, Arg14, Lys15] N/OFQ-NH2 (UFP-101) is a novel NOP ligand that was designed by combining, in the same molecule, the [Nphe1] chemical modification which eliminates efficacy and the [Arg14, Lys15] substitution which increases ligand potency and duration of action in vivo. In the present article, we summarize the pharmacological features of UFP-101 as determined in a series of in vitro and in vivo assays. Moreover, some biological actions and possible therapeutic indications of NOP ligands are discussed on the basis of results obtained with UFP-101. Data obtained with this compound were compared with those generated using other NOP antagonists, especially J-113397 and [Nphe1]N/OFQ(1-13)-NH2, receptor or peptide knockout mice and other pharmacological tools useful for blocking N/OFQ - NOP receptor signaling. The analysis of the available data demonstrates that UFP-101 is a useful pharmacological tool for the investigation of the central and peripheral biological functions regulated by the N/OFQ-NOP receptor system and for defining the therapeutic potential of NOP receptor ligands.

Authors+Show Affiliations

Department Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Centre, University of Ferrara, via Fossato di Mortara, 19, 44100 Ferrara, Italy. g.calo@unife.itNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, P.H.S.
Review

Language

eng

PubMed ID

16007234

Citation

Calo, Girolamo, et al. "UFP-101, a Peptide Antagonist Selective for the Nociceptin/orphanin FQ Receptor." CNS Drug Reviews, vol. 11, no. 2, 2005, pp. 97-112.
Calo G, Guerrini R, Rizzi A, et al. UFP-101, a peptide antagonist selective for the nociceptin/orphanin FQ receptor. CNS Drug Rev. 2005;11(2):97-112.
Calo, G., Guerrini, R., Rizzi, A., Salvadori, S., Burmeister, M., Kapusta, D. R., Lambert, D. G., & Regoli, D. (2005). UFP-101, a peptide antagonist selective for the nociceptin/orphanin FQ receptor. CNS Drug Reviews, 11(2), 97-112.
Calo G, et al. UFP-101, a Peptide Antagonist Selective for the Nociceptin/orphanin FQ Receptor. CNS Drug Rev. 2005;11(2):97-112. PubMed PMID: 16007234.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - UFP-101, a peptide antagonist selective for the nociceptin/orphanin FQ receptor. AU - Calo,Girolamo, AU - Guerrini,Remo, AU - Rizzi,Anna, AU - Salvadori,Severo, AU - Burmeister,Melissa, AU - Kapusta,Daniel R, AU - Lambert,David G, AU - Regoli,Domenico, PY - 2005/7/12/pubmed PY - 2005/12/20/medline PY - 2005/7/12/entrez SP - 97 EP - 112 JF - CNS drug reviews JO - CNS Drug Rev VL - 11 IS - 2 N2 - Nociceptin/orphanin FQ modulates various biological functions at central and peripheral levels by selectively activating a G-protein coupled receptor named N/OFQ peptide (NOP) receptor. For extending our knowledge on the biological roles of the N/OFQ-NOP receptor system the identification of selective NOP ligands, especially antagonists, is mandatory. [Nphe1, Arg14, Lys15] N/OFQ-NH2 (UFP-101) is a novel NOP ligand that was designed by combining, in the same molecule, the [Nphe1] chemical modification which eliminates efficacy and the [Arg14, Lys15] substitution which increases ligand potency and duration of action in vivo. In the present article, we summarize the pharmacological features of UFP-101 as determined in a series of in vitro and in vivo assays. Moreover, some biological actions and possible therapeutic indications of NOP ligands are discussed on the basis of results obtained with UFP-101. Data obtained with this compound were compared with those generated using other NOP antagonists, especially J-113397 and [Nphe1]N/OFQ(1-13)-NH2, receptor or peptide knockout mice and other pharmacological tools useful for blocking N/OFQ - NOP receptor signaling. The analysis of the available data demonstrates that UFP-101 is a useful pharmacological tool for the investigation of the central and peripheral biological functions regulated by the N/OFQ-NOP receptor system and for defining the therapeutic potential of NOP receptor ligands. SN - 1080-563X UR - https://www.unboundmedicine.com/medline/citation/16007234/UFP_101_a_peptide_antagonist_selective_for_the_nociceptin/orphanin_FQ_receptor_ L2 - https://onlinelibrary.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=1080-563X&date=2005&volume=11&issue=2&spage=97 DB - PRIME DP - Unbound Medicine ER -