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Design And Synthesis Of Novel Cannabinoid Receptor Modulators, Mary Paige Thrash

Honors Theses

Cannabinoid (CB) receptors are validated drug targets in the endocannabinoid signaling system associated with a number of human pathologies, and the development of novel and selective small molecule CB ligands is warranted. A lead molecule HL-010, a member of the 4H-thieno[3,2-b]pyrrole-5-carboxamide class of compounds, was previously identified through CB homology modeling and virtual screening protocols as a potential high affinity ligand for cannabinoid receptors. Validation of the in silico data was realized with the evaluation of both CB1 and CB2 receptor binding and functional activity assessment: HL-010 was found to be a potent (~10 nM) and selective CB2 receptor agonist …