Identification of an N -acylated- D Arg-Leu-NH 2 Dipeptide as a Highly Selective Neuropeptide FF1 Receptor Antagonist That Potently Prevents Opioid-Induced Hyperalgesia

• Published in: Journal of medicinal chemistry Vol. 64; no. 11; pp. 7555 - 7564
• Main Authors: Quillet, Raphaëlle, Schneider, Séverine, Utard, Valérie, Drieu la Rochelle, Armand, Elhabazi, Khadija, Henningsen, Jo Beldring, Gizzi, Patrick, Schmitt, Martine, Kugler, Valérie, Simonneaux, Valérie, Ilien, Brigitte, Simonin, Frédéric, Bihel, Frédéric
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 10.06.2021
• Subjects: Biochemistry, Molecular Biology; Life Sciences

RFamide-related peptide-3 (RFRP-3) and neuropeptide FF (NPFF) target two different receptor subtypes called neuropeptide FF1 (NPFF1R) and neuropeptide FF2 (NPFF2R) that modulate several functions. However, the study of their respective role is severely limited by the absence of selective blockers. W...