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Papers of the Week


Papers: 27 Mar 2021 - 2 Apr 2021


Animal Studies, Pharmacology/Drug Development


2021 Mar 30


Gut

Agonist that activates the µ-opioid receptor in acidified microenvironments inhibits colitis pain without side effects.

Authors

Jiménez-Vargas N N, Yu Y, Jensen DD, Bok D D, Wisdom M, Latorre R, Lopez C, Jaramillo-Polanco JO, Degro C, Guzman-Rodriguez M, Tsang Q, Snow Z, Schmidt BL, Reed DE, Lomax A E, Margolis K G, Stein C, Bunnett NW, Vanner SJ
Gut. 2021 Mar 30.
PMID: 33785555.

Abstract

The effectiveness of µ-opioid receptor (MOPr) agonists for treatment of visceral pain is compromised by constipation, respiratory depression, sedation and addiction. We investigated whether a fentanyl analogue, (±)-N-(3-fluoro-1-phenethylpiperidine-4-yl)-N-phenyl propionamide (NFEPP), which preferentially activates MOPr in acidified diseased tissues, would inhibit pain in a preclinical model of inflammatory bowel disease (IBD) without side effects in healthy tissues.