Journal of Medicinal Chemistry · 2019 · 60 citations · 41 references
PharmacyMedicinal ChemistryPharmacologyDrug DiscoveryMolecular PharmacologyStructure-activity RelationshipsAllosteric Drug DesignAllosteric ModulationAllosteric Modulator DesignCannabinoid PharmacologyLigand BindingPotency OptimizationAqueous Solubility ImprovementCannabinoid AgonistsCannabinoid AnalgesicsCannabinoid Receptor PharmacologyCannabinoid Structure-activity RelationshipsGlaucoma ModelsOptimization Of Drug-like PropertiesPositive Allosteric Modulators
), exhibited moderate ago-PAM potency and improved aqueous solubility with therapeutic reduction of intraocular pressure in murine glaucoma models. The SAR findings and the enhanced allosteric activity in this class of allosteric modulators were accounted for in our recently developed computational model for CB1R allosteric activation and positive allosteric modulation.
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