The Identification of GPR52 Agonist HTL0041178, a Potential Therapy for Schizophrenia and Related Psychiatric Disorders
Simon Poulter, Nigel Austin, Rachel Armstrong, Matt Barnes, S.J. Bucknell, Alícia P. Higueruelo, Joydeep Banerjee, Andy Mead, Richard F. Mould, Cliona MacSweeney, Alistair O’Brien, Lisa A. Stott, Stephen P. Watson
Abstract
), a potent GPR52 agonist with a promising pharmacokinetic profile and exhibiting oral activity in preclinical models, has been identified. This molecule was the outcome of a judicious molecular property-based optimization approach, focusing on balancing potency against metabolic stability, solubility, permeability, and P-gp efflux.
Topics & Concepts
Metabolic stabilityAgonistSchizophrenia (object-oriented programming)PharmacokineticsPotencyPharmacologyMedicineEffluxPsychiatryBioinformaticsChemistryInternal medicineBiologyBiochemistryIn vitroReceptorReceptor Mechanisms and SignalingDrug Transport and Resistance MechanismsNeuropeptides and Animal Physiology