Functional characterization of a human receptor for neuropeptide FF and related peptides

British Journal of Pharmacology
M KotaniM Parmentier

Abstract

1. Neuropeptides FF (NPFF) and AF (NPAF) are involved in pain modulation and opioid tolerance. These peptides were known to act through uncharacterized G protein-coupled receptors (GPCR). We describe here, using an aequorin-based assay as screening tool, that an orphan GPCR, previously designated HLWAR77, is a functional high affinity receptor for NPFF and related peptides. This receptor is further designated as NPFFR. 2. Binding experiments were performed with a new radioiodinated probe, [(125)I]-EYF, derived from the EFW-NPSF sequence of the rat NPFF precursor. Chinese hamster ovary (CHO) cell membranes expressing NPFFR bound [(125)I]-EYF with a K(d) of 0.06 nM. Various NPFF analogues and related peptides inhibited [(125)I]-EYF specific binding with the following rank order (K(i)): human NPAF (0.22 nM), SQA-NPFF (0.29 nM), NPFF (0.30 nM), 1DMe (0.31 nM), EYW-NPSF (0.32 nM), QFW-NPSF (0.35 nM), 3D (1.12 nM), Met-enk-RF-NH(2) (3.25 nM), FMRF-NH(2) (10.5 nM) and NPSF (12.1 nM). 3. The stimulatory activity of the same set of peptides was measured by a functional assay based on the co-expression of NPFFR, G(alpha 16) and apoaequorin. The rank order of potency was consistent with the results of the binding assay. 4. Membranes from ...Continue Reading

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Citations

Apr 16, 2003·Analytical Biochemistry·Cecilia JiangYinghe Hu
Aug 7, 2002·European Journal of Pharmacology·Isabelle QuelvenJean-Marie Zajac
May 30, 2002·Progress in Neurobiology·Mark J Millan
Nov 15, 2003·Matrix Biology : Journal of the International Society for Matrix Biology·Satyajit K KarnikDean Y Li
Apr 12, 2003·Current Opinion in Pharmacology·Anthony P Davenport
Oct 2, 2003·European Journal of Biochemistry·Elisabeth BonnardJean-Marie Zajac
Oct 2, 2002·Journal of Neurochemistry·Johanna M NystedtPertti Panula
Oct 8, 2003·The Journal of Experimental Medicine·Valérie WittamerDavid Communi
Apr 20, 2004·Assay and Drug Development Technologies·Janine N BresnickGeorge McAllister
May 7, 2010·The AAPS Journal·Akihiko OzawaWesley K Kroeze
Oct 18, 2011·Pharmacological Reports : PR·Catherine MollereauJean-Marie Zajac
Jun 18, 2010·Neuropeptides·Lionel MoulédousJean-Marie Zajac
Dec 1, 2009·Peptides·Franck TalmontCatherine Mollereau
Sep 15, 2007·Neuropeptides·Hsiu-Ying T YangMichael J Iadarola
Mar 6, 2007·Neuroscience Research·Christine Gouardères, Jean-Marie Zajac
Aug 31, 2010·BioFactors·Lionel MoulédousJean-Marie Zajac
Feb 1, 2005·European Journal of Pharmacology·Isabelle QuelvenJean-marie Zajac

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