Discovery of a novel class of selective human CB1 inverse agonists.

Ligand-based virtual screening led to the discovery of a new class of potent inverse agonists of the human cannabinoid receptor 1, hCB 1 , which are selective versus hCB 2 . These CB 1 ligands present intriguing departures from a classical CB 1 antagonist pharmacophore. Elements of SAR are discussed in this context.