LP1 and LP2: Dual-Target MOPr/DOPr Ligands as Drug Candidates for Persistent Pain Relief.

Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
Lorella PasquinucciRita Turnaturi

Abstract

Although persistent pain is estimated to affect about 20% of the adult population, current treatments have poor results. Polypharmacology, which is the administration of more than one drug targeting on two or more different sites of action, represents a prominent therapeutic approach for the clinical management of persistent pain. Thus, in the drug discovery process the "one-molecule-multiple targets" strategy nowadays is highly recognized. Indeed, multitarget ligands displaying a better antinociceptive activity with fewer side effects, combined with favorable pharmacokinetic and pharmacodynamic characteristics, have already been shown. Multitarget ligands possessing non-opioid/opioid and opioid/opioid mechanisms of action are considered as potential drug candidates for the management of various pain conditions. In particular, dual-target MOPr (mu opioid peptide receptor)/DOPr (delta opioid peptide receptor) ligands exhibit an improved antinociceptive profile associated with a reduced tolerance-inducing capability. The benzomorphan-based compounds LP1 and LP2 belong to this class of dual-target MOPr/DOPr ligands. In the present manuscript, the structure-activity relationships and the pharmacological fingerprint of LP1 and LP2 c...Continue Reading

References

Oct 1, 1986·Pain·J D LevineR McBryde
May 29, 1998·Brain Research. Molecular Brain Research·S RoyH H Loh
Jun 18, 2002·The Journal of Pharmacology and Experimental Therapeutics·Jean M BidlackMark P Wentland
Oct 15, 2003·The Journal of Pharmacology and Experimental Therapeutics·Glenn W StevensonS Stevens Negus
Apr 23, 2004·Drugs·Pamela S Davies, Bradley S Galer
Oct 14, 2005·Journal of Medicinal Chemistry·Richard Morphy, Zoran Rankovic
Jan 6, 2006·The Journal of Pharmacology and Experimental Therapeutics·Hirokazu MizoguchiShinobu Sakurada
Jun 10, 2006·Trends in Pharmacological Sciences·Juan A MicóAlain Eschalier
May 11, 2007·Journal of Medicinal Chemistry·Mark J FieldJacob B Schwarz
Nov 26, 2008·European Journal of Pharmacology·S Stevens NegusKenner C Rice
Oct 29, 2009·Pain Research & Management : the Journal of the Canadian Pain Society = Journal De La Société Canadienne Pour Le Traitement De La Douleur·Julia Ann Fleming, Bradley David O'Connor
Jul 6, 2010·Bioorganic & Medicinal Chemistry·Lorella PasquinucciGiuseppe Ronsisvalle
Jul 27, 2010·Journal of Perianesthesia Nursing : Official Journal of the American Society of PeriAnesthesia Nurses·Julie Golembiewski, Andrei M Rakic
Sep 17, 2010·American Journal of Therapeutics·Mary Hanna Bekhit
Nov 3, 2010·The Journal of Clinical Investigation·Gillian Burgess, Dic Williams
Aug 10, 2011·Journal of Opioid Management·Patricia RichardsUNKNOWN MoxDuo Study Team
Sep 16, 2011·Current Medical Research and Opinion·Charles Argoff
Nov 22, 2011·Life Sciences·Lorella PasquinucciGiuseppe Ronsisvalle
May 15, 2012·Life Sciences·Carmela ParentiLorella Pasquinucci
Jun 20, 2012·British Journal of Pharmacology·Amynah A PradhanChristopher J Evans
Mar 19, 2014·European Journal of Medicinal Chemistry·Maria Lorena AccollaLorella Pasquinucci
Jun 20, 2014·Journal of Medicinal Chemistry·Andrew AnighoroGiulio Rastelli
Dec 3, 2014·Behavioural Brain Research·Paul Chu Sin ChungBrigitte L Kieffer
Dec 15, 2015·European Journal of Medicinal Chemistry·Rita TurnaturiLorella Pasquinucci
May 29, 2016·Bioorganic & Medicinal Chemistry·Lorella PasquinucciSimone Ronsisvalle
Jun 28, 2016·Pharmacological Reviews·Louis GendronGraciela Pineyro
Oct 27, 2016·Neuroscience·Ana Vicente-SanchezAmynah A Pradhan
Oct 27, 2016·Current Medicinal Chemistry·Rita TurnaturiCarmela Parenti
Jul 25, 2017·Bioorganic & Medicinal Chemistry·Lorella PasquinucciCarmela Parenti
Feb 25, 2018·European Journal of Medicinal Chemistry·Rita TurnaturiLorella Pasquinucci
Mar 17, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Rita TurnaturiLorella Pasquinucci
Jun 17, 2018·European Journal of Medicinal Chemistry·Rita TurnaturiCarmela Parenti
Jan 10, 2019·Expert Opinion on Pharmacotherapy·Wojciech LeppertJerzy Wordliczek

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