Antinociception by a peripherally administered novel endomorphin-1 analogue containing beta-proline

European Journal of Pharmacology
Santi SpampinatoGiuliana Cardillo

Abstract

We previously described a novel endomorphin-1 analogue (Tyr-L-beta-Pro-Trp-Phe-NH(2); Endo1-beta-Pro) more resistant to enzymatic hydrolysis than endomorphin-1 that acts as a mu-opioid receptor agonist. In this study we report that Endo1-beta-Pro, s.c. injected in the mouse, is an effective antinociceptive agent in the tail flick (ED(50)=9.2 mg/kg) and acetic acid-induced abdominal constriction (ED(50)=1.2 mg/kg) tests. Moreover, s.c. Endo1-beta-Pro significantly decreases, in the mouse, the gastrointestinal propulsion measured as transit of an orally administered charcoal meal (ED(50)=10.0 mg/kg). Subcutaneous beta-funaltrexamine or a high dose of the mu(1)-opioid receptor-selective antagonist naloxonazine (50 mg/kg) prevents the antinociceptive and antitransit action of Endo1-beta-Pro; moreover, these effects are partially blocked by i.c.v. naloxone or by i.p. naloxone methiodide, this latter does not readily cross the blood-brain barrier. On the contrary, the kappa-opioid receptor antagonist nor-binaltorphimine or the delta-opioid receptor antagonist naltrindole are ineffective Thus, Endo1-beta-Pro may act, preferentially, through central and peripheral mu(2)-opioid receptors to produce antinociception and to inhibit gastroi...Continue Reading

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Citations

Jan 19, 2010·Acta Anaesthesiologica Scandinavica·C C Apfel, L Jalota
Apr 12, 2011·Neuropeptides·Luciana Malavolta, Francisco Romero Cabral
Mar 21, 2007·Chemistry & Biodiversity·Zhi-Hao ShiLi Yu
May 22, 2010·ChemMedChem·Attila KeresztesGéza Tóth
Mar 3, 2007·Pharmacological Reviews·Jakub FichnaJean-Claude Do Rego
Sep 25, 2017·The Journal of Pain : Official Journal of the American Pain Society·Amy K FeehanJames E Zadina
Aug 23, 2008·Peptides·Anna JaneckaJakub Fichna

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