2. Academic Validation
  3. Discovery of a novel class of selective human CB1 inverse agonists

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

Affiliation

  • 1 Vernalis (R&D) Ltd, Granta Park, Abington, Cambridge CB21 6GB, UK. n.foloppe@vernalis.com
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.

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