Anti-analgesia of a selective NPFF2 agonist depends on opioid activity
Biochemical and Biophysical Research Communications. 2005-10-01; 336(1): 197-203
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1. Biochem Biophys Res Commun. 2005 Oct 14;336(1):197-203.
Anti-analgesia of a selective NPFF2 agonist depends on opioid activity.
Roussin A(1), Serre F, Gouardères C, Mazarguil H, Roumy M, Mollereau C, Zajac JM.
(1)Institut de Pharmacologie et de Biologie Structurale, CNRS UMR 5089, 205 Route
de Narbonne, 31077 Toulouse Cedex, France.
NPFF agonists designed to be selective NPFF(2) receptor probes were synthesized.
D.Asn-Pro-(N-Me)Ala-Phe-Leu-Phe-Gln-Pro-Gln-Arg-Phe-NH(2) (dNPA) displays a very
high affinity (0.027nM) for NPFF(2) receptors transfected in CHO cells, and a
very high selectivity with a discrimination ratio greater than 100 versus NPFF(1)
receptors. dNPA acts as a potent and selective agonist in [(35)S]GTPgammaS
binding experiments and inhibits intracellular cAMP production with the same
efficacy as NPA-NPFF. In SH-SY5Y cells expressing NPFF(2) receptors dNPA, in the
presence of carbachol, stimulates Ca(2+) release from the intracellular stores.
In vivo, after intracerebroventricular injection dNPA increases body temperature
in mice and reverses the morphine-induced analgesia. Also, dNPA displays
anti-opioid activity after systemic administration. So far, dNPA exhibits the
highest affinity and selectivity for NPFF(2) receptors and reveals that its
behavioral anti-opioid activity depends on the degree of opioid-induced
PMID: 16129413 [Indexed for MEDLINE]