Maria Antonietta De Luca, Graziella Tocco, Rafaela Mostallino, Antonio Laus, Francesca Caria, Aurora Musa, Nicholas Pintori, Marcos Ucha, Celia Poza, Emilio Ambrosio, Gaetano Di Chiara, M Paola Castelli
Recent trends of opioid abuse and related fatalities have highlighted the critical role of Novel Synthetic Opioids (NSOs). We studied the μ-opioid-like properties of isotonitazene (ITZ), metonitazene (MTZ), and piperidylthiambutene (PTB) using different approaches. In vitro studies showed that ITZ and MTZ displayed a higher potency in both rat membrane homogenates (EC50 :0.99 and 19.1 nM, respectively) and CHO-MOR (EC50 :0.71 and 10.0 nM, respectively) than [D-Ala2 , NMe-Phe4 , Gly-ol5 ]-enkephalin (DAMGO), with no difference in maximal efficacy (Emax) between DAMGO and NSOs...
December 15, 2022: Neuropharmacology