Antinociceptive profile of LP1, a non-peptide multitarget opioid ligand

Life Sciences
Carmela ParentiLorella Pasquinucci

Abstract

Opioid drugs are the principal treatment option for moderate to severe pain and exert their biological effects through interactions with opioid receptors that are widely distributed throughout the CNS and peripheral tissues. Ligands capable of simultaneously targeting different receptors could be successful candidates for the treatment of chronic pain. Enhanced antinociception coupled with a low incidence of side effects has been demonstrated for ligands possessing mixed mu-opioid receptor (MOR) and delta-opioid receptor (DOR) activity. We previously reported that 3-[(2R,6R,11R)-8-hydroxy-6,11-dimethyl-1,4,5,6-tetrahydro-2,6-methano-3-benzazocin-3(2H)-yl]-N-phenylpropanamide (LP1) acted as a MOR-DOR ligand in in vitro functional assays and moreover this drug produced a valid antinociception that was longer lasting than that of morphine. The aim of this work was to determine whether the antinociceptive effect produced by LP1 was central or peripheral and to assess which opioid receptor subtypes are involved in its effects. We explored the effects of naloxone methiodide (NX-M), a quaternary opioid antagonist, administered either intracerebroventricularly (i.c.v.) or subcutaneously (s.c.), on LP1-mediated antinociception in male S...Continue Reading

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Citations

Oct 16, 2013·Peptides·Richard J Bodnar
Mar 19, 2014·European Journal of Medicinal Chemistry·Maria Lorena AccollaLorella Pasquinucci
Apr 6, 2017·British Journal of Pharmacology·Thomas GüntherStefan Schulz
Mar 17, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Rita TurnaturiLorella Pasquinucci
Oct 25, 2013·The Journal of Pharmacology and Experimental Therapeutics·Cristina Sánchez-FernándezEnrique José Cobos
Dec 1, 2017·Future Medicinal Chemistry·Emanuela ArenaOrazio Prezzavento
Dec 2, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Joanna Starnowska-Sokół, Barbara Przewłocka
Apr 24, 2020·Current Topics in Medicinal Chemistry·Wakako Fujita
Jul 25, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Lorella PasquinucciRita Turnaturi
May 22, 2020·ACS Medicinal Chemistry Letters·Lorella PasquinucciRita Turnaturi
Nov 28, 2017·Journal of Medicinal Chemistry·Emanuele AmataOrazio Prezzavento

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