Etorphines: mu-opioid receptor-selective antinociception and low physical dependence capacity

European Journal of Pharmacology
Mario D AcetoE R Bowman

Abstract

Comparative analgesic studies revealed that dihydroetorphine was more potent than etorphine in the tail-flick and hot-plate tests, respectively and nearly equipotent in the phenylquinone assay. Both compounds were short acting. Studies with selective opioid receptor antagonists beta-funaltrexamine, nor-binaltorphimine and naltrindole revealed that both etorphines were mu-selective agonists. Presumptive evidence for competitive antagonism of these compounds with naloxone was provided by Schild regressions with slopes of near unity. In a suppression test in rhesus monkeys maximally dependent on morphine, dihydroetorphine and etorphine dose-dependently replaced morphine. Drug-naive simians chronically exposed to frequent, intermittent and escalating doses of dihydroetorphine for 42 days showed few withdrawal signs when challenged with large doses of naloxone or were abruptly withdrawn from this drug. The results suggest that these atypical opioids may be useful in the clinical treatment of pain and opiate drug abuse.

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Citations

May 22, 2002·European Journal of Pharmacology·Dauren BiyashevSándor Benyhe
Jan 14, 2000·European Journal of Pharmacology·M D AcetoZ Ji
Dec 26, 2001·Brain Research. Brain Research Reviews·J G Liu, K J Anand
Jan 8, 1999·Peptides·G A OlsonA J Kastin
Mar 4, 2009·Journal of Medicinal Chemistry·Gerta Cami-KobeciStephen M Husbands
Aug 11, 2004·Experimental and Clinical Psychopharmacology·Patrick M BeardsleyLouis S Harris
Feb 4, 2014·European Journal of Pharmacology·Mariana Martins Gomes PinheiroPatrícia Dias Fernandes
Feb 18, 2016·Life Sciences·Thais Biondino Sardella GiornoPatricia Dias Fernandes
Jan 13, 2010·Journal of Ethnopharmacology·Niele de Matos GomesPatricia Dias Fernandes
Oct 29, 2009·Journal of Ethnopharmacology·Mariana M G PinheiroPatrícia Dias Fernandes
Jul 16, 2014·Pharmaceutical Biology·Madhu Cholenahalli LingarajuSurendra Kumar Tandan
Aug 15, 2015·Evidence-based Complementary and Alternative Medicine : ECAM·Carolina Carvalho GuilhonPatricia Dias Fernandes
Feb 1, 2011·Journal of Ethnopharmacology·Larissa J R P RaymundoPatrícia D Fernandes
Oct 11, 2012·Pharmacology, Biochemistry, and Behavior·Gabriela S M FigueiredoPatricia D Fernandes
Oct 7, 2004·European Journal of Pharmacology·Ivy CarrollLouis S Harris
May 16, 2017·European Journal of Pharmacology·Ferenc ZádorMahmoud Al-Khrasani
Feb 1, 2005·Life Sciences·Wolfgang SadéeEdward J Bilsky
Mar 1, 2005·European Journal of Pharmacology·Stephen M HusbandsJohn R Traynor
Sep 24, 2004·The Journal of Pharmacology and Experimental Therapeutics·Susanna FürstHelmut Schmidhammer
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Sep 5, 2003·Journal of Medicinal Chemistry·Johannes SchützHelmut Schmidhammer
Jul 22, 2005·Journal of Medicinal Chemistry·Wayne W HardingThomas E Prisinzano

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