• Corpus ID: 2064637

SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.

  title={SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.},
  author={Murielle Rinaldi-Carmona and Francis Barth and Joseph Millan and Jean Marie Derocq and Pierre Casellas and Christian Congy and Didier Oustric and Martine Sarran and Monsif Bouaboula and Bernard Calandra and Marielle Portier and David Shire and Jean Claude Breliere and Gérard Le Fur},
  journal={The Journal of pharmacology and experimental therapeutics},
  volume={284 2},
Based on both binding and functional data, this study introduces SR 144528 as the first, highly potent, selective and orally active antagonist for the CB2 receptor. This compound which displays subnanomolar affinity (Ki = 0.6 nM) for both the rat spleen and cloned human CB2 receptors has a 700-fold lower affinity (Ki = 400 nM) for both the rat brain and cloned human CB1 receptors. Furthermore it shows no affinity for any of the more than 70 receptors, ion channels or enzymes investigated (IC50… 

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