Publication | Open Access
Activation of the G-Protein-Coupled Receptor 119: A Conformation-Based Hypothesis for Understanding Agonist Response
48
Citations
10
References
2011
Year
G-protein-coupled Receptor 119PharmacotherapyHeterocycle ChemistryMolecular PharmacologyMedicinal ChemistryHuman PharmacologyCell SignalingMolecular PhysiologyConformation-based HypothesisBiochemistryG Protein-coupled ReceptorReceptor (Biochemistry)Mechanism Of ActionConformational StudyGpr119 ReceptorPharmacologySignal TransductionFunctional SelectivityNatural SciencesAgonist ResponseAgonist PharmacologyMedicineDrug Discovery
The synthesis and properties of the bridged piperidine (oxaazabicyclo) compounds 8, 9, and 11 are described. A conformational analysis of these structures is compared with the representative GPR119 ligand 1. These results and the differences in agonist pharmacology are used to formulate a conformation-based hypothesis to understand activation of the GPR119 receptor. We also show for these structures that the agonist pharmacology in rat masks the important differences in human pharmacology.
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