UFP-112 a potent and long-lasting agonist selective for the Nociceptin/Orphanin FQ receptor.
Nociceptin/orphanin FQ (N/OFQ) controls several biological functions via selective activation of the N/OFQ peptide receptor (NOP). [(pF)Phe(4) Aib(7) Arg(14) Lys(15) ]N/OFQ-NH(2) (UFP-112) is an NOP receptor ligand designed using a combination of several chemical modifications in the same peptide sequence that increase NOP receptor affinity/potency and/or reduce susceptibility to enzymatic degradation. In the present review article, we summarize data from the literature and present original findings on the in vitro and in vivo pharmacological features of UFP-112. Moreover, important biological actions and possible therapeutic indications of NOP receptor agonists are discussed based on the results obtained with UFP-112 and compared with other peptide and nonpeptide NOP receptor ligands.
Calo'
Girolamo
G
Department Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Center, University of Ferrara, and National Institute of Neuroscience, Ferrara, Italy. g.calo@unife.it
Rizzi
Anna
A
Cifani
Carlo
C
Micioni Di Bonaventura
Maria Vittoria
MV
Regoli
Domenico
D
Massi
Maurizio
M
Salvadori
Severo
S
Lambert
David G
DG
Guerrini
Remo
R
D000818:Animals; D015195:Drug Design; D006801:Humans; D008024:Ligands; D018847:Opioid Peptides / Q000737:chemistry / Q000494:pharmacology*; D010146:Pain / Q000188:drug therapy / Q000503:physiopathology; D010455:Peptides / Q000494:pharmacology; D011957:Receptors, Opioid / Q000819:agonists*; D009435:Synaptic Transmission / Q000187:drug effects; D000094942:Nociceptin Receptor
D008024:Ligands; D018847:Opioid Peptides; D010455:Peptides; D011957:Receptors, Opioid; C525846:nociceptin-amide, Nphe(1)-(pF)Phe(4)-Aib(7)-Arg(14)-Lys(15)-; D000094942:Nociceptin Receptor; C000722283:OPRL1 protein, human