PMID: 11311733Apr 20, 2001Paper

(125)I]EYF: a new high affinity radioligand to neuropeptide FF receptors

Peptides
C GouarderesJ-M Zajac

Abstract

[(125)I]EYF ([(125)I]EYWSLAAPQRFamide), a new radioiodinated probe derived from a peptide present in the rat Neuropeptide FF precursor (EFWSLAAPQRFamide, EFW-NPSF) was synthesized and its binding characteristics investigated on sections of the rat spinal cord and on membranes of mouse olfactory bulb. In both tissues, [(125)I]EYF binding was saturable and revealed a very high affinity interaction with a single class of binding sites in rat and mouse (K(D) = 0.041 and 0.019 nM, respectively). Competition studies showed that [(125)I]EYF bound to one class of binding sites exhibiting a high affinity for all the different peptides the precursor could generate (NPA-NPFF, SPA-NPFF, NPFF, EFW-NPSF, QFW-NPSF) with the exception of NPSF which displayed a low affinity. Autoradiographic studies demonstrated that [(125)I]EYF binding sites were fully inhibited by a synthetic Neuropeptide FF agonist (1DMe) in all areas of the rat brain. The density of [(125)I]EYF binding sites was high in the intralaminar thalamic nuclei, the parafascicular thalamic nucleus and in the superficial layers of the dorsal horn. Non specific binding reached 5-10% of the total binding in all brain areas. Similarly, in mouse brain experiments, the non-specific bindin...Continue Reading

References

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Citations

Aug 7, 2002·European Journal of Pharmacology·Isabelle QuelvenJean-Marie Zajac
Apr 28, 2001·British Journal of Pharmacology·M KotaniM Parmentier
Dec 19, 2009·Analytical Biochemistry·Frank TalmontJean-Marie Zajac
Dec 1, 2009·Peptides·Franck TalmontCatherine Mollereau
Jul 17, 2020·Journal of Medicinal Chemistry·Thuy NguyenYanan Zhang
Aug 18, 2009·Neurochemistry International·Franck TalmontCatherine Mollereau

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