Opioid receptor binding and in vivo antinociceptive activity of position 3-substituted morphiceptin analogs

Biochemical and Biophysical Research Communications
Jakub FichnaAnna Janecka

Abstract

Analogs of morphiceptin (Tyr-Pro-Phe-Pro-NH2), a mu-selective opioid receptor ligand, with position 3-modifications, including altered size, lipophilicity, and electronic character, while maintaining aromaticity were synthesized. The activity of the new analogs in in vitro assays and in in vivo hot-plate test of analgesia was compared and the results were consistent. [D-1-Nal3]Morphiceptin was the most potent analog of this series with a 26-fold increase in mu-opioid receptor affinity, a 15-fold potency increase in the GPI assay, and a significant potency increase in the hot-plate analgesic test, as compared with morphiceptin. [d-Qal3]Morphiceptin was found to be a weak antagonist in the GPI assay.

References

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Feb 3, 2004·Current Topics in Medicinal Chemistry·Anna JaneckaTomasz Janecki

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Citations

Mar 23, 2005·Bioorganic & Medicinal Chemistry Letters·Yanfeng GaoRui Wang
Jul 11, 2006·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Jakub FichnaJean-Claude do Rego
Oct 10, 2009·Pharmacological Reports : PR·Monika LukowiakAndrzej W Lipkowski
Apr 9, 2005·The Journal of Peptide Research : Official Journal of the American Peptide Society·J FichnaA Janecka
Aug 9, 2005·The Journal of Peptide Research : Official Journal of the American Peptide Society·R KruszynskiA Janecka
Mar 29, 2014·Chemical Biology & Drug Design·Oliwia FrączakAleksandra Olma
May 9, 2006·Biochemical and Biophysical Research Communications·Jakub FichnaAnna Janecka
Mar 31, 2016·Journal of Peptide Science : an Official Publication of the European Peptide Society·Oliwia FrączakAleksandra Olma
Nov 18, 2005·Biochemical Pharmacology·Anna JaneckaJean-Claude do-Rego
Jul 26, 2005·Peptides·Richard J Bodnar, Gad E Klein
Mar 11, 2015·Journal of Peptide Science : an Official Publication of the European Peptide Society·Krzysztof BańkowskiJan Izdebski
Jan 6, 2015·Journal of Peptide Science : an Official Publication of the European Peptide Society·Anika LasotaAleksandra Olma
Sep 11, 2012·Regulatory Peptides·Meixing LiShouliang Dong
Jul 23, 2016·Journal of Peptide Science : an Official Publication of the European Peptide Society·Maciej MaciejczykAleksandra Olma
Mar 21, 2007·Chemistry & Biodiversity·Zhi-Hao ShiLi Yu
Feb 25, 2006·The Journal of Pharmacology and Experimental Therapeutics·Jakub FichnaAnna Janecka

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