Design, Structural Optimization, and Characterization of the First Selective Macrocyclic Neurotensin Receptor Type 2 Non-opioid Analgesic
Magali Chartier, Michael Desgagné, Marc Sousbie, Jérôme Côté, Jean‐Michel Longpré, Éric Marsault, Philippe Sarret
Abstract
produces potent analgesia in three distinct rodent pain models, without causing the undesired effects associated with NTS1 activation. We further provide evidence of its non-opioid antinociceptive activity, therefore highlighting the strong therapeutic potential of NTS2-selective analogs for the management of acute and chronic pain.
Topics & Concepts
NeurotensinChemistryNeurotensin receptorIn vivoReceptorOpioidChemical synthesisStereochemistryPharmacologyCombinatorial chemistryIn vitroNeuropeptideBiochemistryMedicineBiologyBiotechnologyNeuropeptides and Animal PhysiologyReceptor Mechanisms and SignalingPain Mechanisms and Treatments