Allosteric Modulation of the Cannabinoid CB1 Receptor

  title={Allosteric Modulation of the Cannabinoid CB1 Receptor},
  author={Martin R. Price and Gemma L. Baillie and Adèle Thomas and Lesley A. Stevenson and Morag A. M. Easson and Richard Goodwin and Ad{\`e}le McLean and Lorraine McIntosh and G. Goodwin and Glenn Walker and Paul Westwood and Julia Marrs and Fiona J. Thomson and Phillip M. Cowley and Arthur Christopoulos and Roger G. Pertwee and Ruth Alexandra Ross},
  journal={Molecular Pharmacology},
  pages={1484 - 1495}
We investigated the pharmacology of three novel compounds, Org 27569 (5-chloro-3-ethyl-1H-indole-2-carboxylic acid [2-(4-piperidin-1-yl-phenyl)-ethyl]-amide), Org 27759 (3-ethyl-5-fluoro-1H-indole-2-carboxylic acid [2-94-dimethylamino-phenyl)-ethyl]-amide), and Org 29647 (5-chloro-3-ethyl-1H-indole-2-carboxylic acid (1-benzyl-pyrrolidin-3-yl)-amide, 2-enedioic acid salt), at the cannabinoid CB1 receptor. In equilibrium binding assays, the Org compounds significantly increased the binding of the… 

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