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Autoimmune disease

Inflammatory bowel disease (IBD)

Cannabinoid CB2 receptor (CNR2)

In vitro and mouse studies identified selective CNR2 agonists that could help treat IBD. Radioligand displacement assays identified 4-oxo-1,4-dihydropyridines that were potent and selective inhibitors of human CNR2 over CNR1. In a mouse model of chemical-induced colitis, intraperitoneal treatment with the agonists decreased bowel thickening and ulceration compared with vehicle treatment and had an effect comparable to that of the positive control Pentasa mesalamine. Next steps could include optimizing the compounds for metabolic stability.
At least six companies have CNR2 agonists in clinical and preclinical development to treat various conditions.
Shire plc markets Pentasa to treat IBD.

SciBX 5(41); doi:10.1038/scibx.2012.1075
Published online Oct. 18, 2012

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El Bakali, J. et al. J. Med. Chem.; published online Sept. 28, 2012;
Contact: Régis Millet, University of Lille North of France, Lille, France