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Papers of the Week
A pH-sensitive opioid does not exhibit analgesic tolerance in a mouse model of colonic inflammation.
Authors
Degro CE, Jiménez-Vargas NN, Guzman-Rodriguez M, Schincariol H, Tsang Q, Reed DE, Lomax AE, Bunnett NW, Stein C, Vanner SJAbstract
Tolerance to the analgesic effects of opioids and resultant dose escalation is associated with worsening of side effects and greater addiction risk. Here, we compare the development of tolerance to the conventional opioid fentanyl with a novel pH-sensitive μ-opioid receptor (MOR) agonist, (±)-N-(3-fluoro-1-phenethylpiperidine-4-yl)-N-phenyl propionamide (NFEPP) that is active only in acidic inflammatory microenvironments.