Anti-analgesia of a selective NPFF2 agonist depends on opioid activity
Biochemical and Biophysical Research Communications. 2005-10-01; 336(1): 197-203
DOI: 10.1016/j.bbrc.2005.08.060
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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.
Author information:
(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
analgesia.
DOI: 10.1016/j.bbrc.2005.08.060
PMID: 16129413 [Indexed for MEDLINE]