Discovery of a novel class of selective human CB1 inverse agonists

  • Bioorg Med Chem Lett. 2008 Feb 1;18(3):1199-206. doi: 10.1016/j.bmcl.2007.11.133.
Nicolas Foloppe  1 ,  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
Affiliations
  • 1. Vernalis (R&D) Ltd, Granta Park, Abington, Cambridge CB21 6GB, UK. [email protected]
PMID: 18083560 DOI: 10.1016/j.bmcl.2007.11.133
Abstract

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.