Design, Synthesis, and Biological Activity of New CB2 Receptor Ligands: from Orthosteric and Allosteric Modulators to Dualsteric/Bitopic Ligands
Francesca Gado, Rebecca Ferrisi, Beatrice Polini, Kawthar A. Mohamed, Caterina Ricardi, Elena Lucarini, Sara Carpi, Federica Domenichini, Lesley Stevenson, Simona Rapposelli, Giuseppe Saccomanni, Paola Nieri, Gabriella Ortore, Roger G. Pertwee, Carla Ghelardini, Lorenzo Di Cesare Mannelli, Grazia Chiellini, Robert B. Laprairie, Clementina Manera
Abstract
in an experimental mouse model of neuropathic pain. Finally, computational studies clarified the binding mode of these compounds inside the CB2R, further confirming their bitopic nature.
Topics & Concepts
ChemistryAllosteric regulationG protein-coupled receptorFunctional selectivityReceptorLigand (biochemistry)Allosteric modulatorStereochemistryPharmacologyBiochemistryBiologyPharmacological Receptor Mechanisms and EffectsReceptor Mechanisms and SignalingComputational Drug Discovery Methods