The anomalous pharmacology of fentanyl

Autor: Norah Alhosan, Katy J. Sutcliffe, Graeme Henderson, Damiana Cavallo, Eamonn Kelly, Nokomis Ramos-Gonzalez

Publikováno v: British Journal of Pharmacology. 180:797-812

Fentanyl is a key therapeutic, used in anaesthesia and pain management. It is also increasingly used illicitly and is responsible for a large and growing number of opioid overdose deaths, especially in North America. A number of factors have been sug

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d3b59aed1adff5b032df7f7b999f5a8f
https://doi.org/10.1111/bph.15573

Interaction With the Lipid Membrane Influences Fentanyl Pharmacology

Autor: Katy J. Sutcliffe, Robin A Corey, Norah Alhosan, Damiana Cavallo, Sam Groom, Marina Santiago, Chris Bailey, Steven J. Charlton, Richard B. Sessions, Graeme Henderson, Eamonn Kelly

Publikováno v: Sutcliffe, K J, Corey, R A, Alhosan, N, Cavallo, D, Groom, S, Santiago, M, Bailey, C, Charlton, S J, Sessions, R B, Henderson, G & Kelly, E 2022, ' Interaction With the Lipid Membrane Influences Fentanyl Pharmacology ', Advances in drug and alcohol research, vol. 2, 10280 . https://doi.org/10.3389/adar.2022.10280

Overdose deaths from fentanyl have reached epidemic proportions in the USA and are increasing worldwide. Fentanyl is a potent opioid agonist that is less well reversed by naloxone than morphine. Due to fentanyl’s high lipophilicity and elongated st

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::333656ded7415d571fa1ae68f2a11c89
https://doi.org/10.3389/adar.2022.10280

A tetrapeptide class of biased analgesics from an Australian fungus targets the µ-opioid receptor

Autor: Paul F. Alewood, Eamonn Kelly, Katy J. Sutcliffe, Christophe Mallet, Andrew M. Piggott, Alexander Gillis, Paramjit Singh, Ranjala Ratnayake, Sarasa A. Mohammadi, Ernest Lacey, MacDonald J. Christie, Frank Fontaine, Richard B. Sessions, Meritxell Canals, Yan P. Du, Anna M. Wang, Setareh Sianati, Robert J. Capon, Zoltan Dekan, Arsalan Yousuf, Ai-Hua Jin, Michael Stewart

Publikováno v: Proceedings of the National Academy of Sciences of the United States of America
Dekan, Z, Sianati, S, Yousuf, A, Sutcliffe, K, Gillis, A, Mallet, C, Singh, P, Jin, A, Wang, A, Mohammadi, S, Stewart, M, Ratnayake, R, Fontaine, F, Lacey, E, Piggott, A, Du, Y, Canals, M, Sessions, R B, Kelly, E P, Capon, R, Alewood, P & Christie, M J 2019, ' A tetrapeptide class of biased analgesics from an Australian fungus targets the μ-opioid receptor ', Proceedings of the National Academy of Sciences of the United States of America, vol. 116, no. 44, pp. 22353-22358 . https://doi.org/10.1073/pnas.1908662116

Significance Agonists of the μ-opioid receptor (MOPr) are currently the gold standard for pain treatment. However, their therapeutic usage is greatly limited by side effects including respiratory depression, constipation, tolerance, and dependence.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e7d4d03fed007f2a4d12033bcdb9f177
http://europepmc.org/articles/PMC6825270

The novel μ-opioid receptor agonist PZM21 depresses respiration and induces tolerance to antinociception

Autor: Katy J. Sutcliffe, Christopher P Bailey, Alex E Conibear, William L. Dewey, Eamonn Kelly, Graeme Henderson, Alex Disney, Stephen M. Husbands, Rob Hill

Publikováno v: British Journal of Pharmacology. 175:2653-2661

BACKGROUND AND PURPOSE PZM21 is a novel μ-opioid receptor ligand that has been reported to induce minimal arrestin recruitment and be devoid of the respiratory depressant effects characteristic of classical μ receptor ligands such as morphine. We h

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::05d491e04060df723b52d0f6e87855f8
https://doi.org/10.1111/bph.14224