Discovery of a novel class of selective human CB1 inverse agonists

Nicolas Foloppe, Nicola H Allen, Carol H Bentley, Teresa D Brooks, Guy Kennett, Antony R Knight, Stefania Leonardi, Anil Misra, Nathaniel J T Monck, Daniel M Sellwood
Bioorganic & Medicinal Chemistry Letters 2008 February 1, 18 (3): 1199-206
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.

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