PMID: 7932576Oct 14, 1994Paper

Structure-activity study of neuropeptide FF: contribution of N-terminal regions to affinity and activity

Journal of Medicinal Chemistry
S GicquelJ M Zajac

Abstract

Twenty neuropeptide FF (NPFF) analogs having various lengths were synthesized by solid-phase peptide synthesis to gain more information on the role of N-terminal residues for the NPFF receptor affinity. The affinities were evaluated in the rat spinal cord membrane preparations, and the biological activities were measured on morphine analgesia in the mouse tail-flick test. Shortening of the NPFF sequence from the N-terminal produced only a moderate decrease in affinity until NPFF (4-8) was reached. In the same way, NPFF(3-8) significantly decreased morphine analgesia, while NPFF(4-8) had no significant effect at a dose of 22 nmol. The introduction in the N-terminal part of NPFF of a D-enantiomer at positions 2 and 1 or the presence of an N-methyl group on position 3 did not modify affinity and activity. Substitution of proline5 by the D-isomer decreased the affinity of NPFF analogs whatever their length, and [Tyr1,D-Pro5]NPFF(1-8) was 2.5-fold less potent than [Tyr1]NPFF(1-8) in reversing morphine-induced analgesia. In contrast, the presence of a glycine residue in position 5 did not influence the affinity toward NPFF receptors. Data provide evidence that the N-terminal segment of neuropeptide FF is responsible for high-affinity...Continue Reading

Citations

Jun 13, 1996·European Journal of Pharmacology·M Roumy, J M Zajac
Mar 1, 1996·Progress in Neurobiology·P PanulaK Wasowicz
Dec 29, 1999·Brain Research·P PanulaA Pertovaara
Aug 7, 2002·European Journal of Pharmacology·Isabelle QuelvenJean-Marie Zajac
May 21, 1998·European Journal of Pharmacology·M Roumy, J M Zajac
Sep 23, 1997·Pharmacology, Biochemistry, and Behavior·C Desprat, J M Zajac
Jun 20, 2012·Future Medicinal Chemistry·Jessica V Mankus, Christopher R McCurdy
Aug 18, 2009·Neurochemistry International·Franck TalmontCatherine Mollereau
Sep 15, 2007·Neuropeptides·Hsiu-Ying T YangMichael J Iadarola
Jul 21, 2010·Journal of Peptide Science : an Official Publication of the European Peptide Society·Brad R GreenGrzegorz Bulaj
Feb 1, 2005·European Journal of Pharmacology·Isabelle QuelvenJean-marie Zajac
Jul 21, 2012·Peptides·Honoré MazarguilJean-Marie Zajac
Jul 25, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Benjamin LefrancJérôme Leprince
Oct 1, 2014·Journal of Medicinal Chemistry·V Blair JourniganChristopher R McCurdy
Jul 17, 2020·Journal of Medicinal Chemistry·Thuy NguyenYanan Zhang
May 4, 2001·Journal of Medicinal Chemistry·L ProkaiJ R Rocca

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