JWH 133

JWH 133 is a synthetic cannabinoid (CB) that is over 200-fold selective for the peripheral CB2 receptor (Ki = 3.4 nM) over the central CB1 receptor (Ki = 677 nM).1 It inhibits the growth of tumors in mice, increasing apoptosis and impairing angiogenesis.2,3 JWH 133 also suppresses inflammation in experimental colitis and pancreatitis in mice as well as in in vitro models.4,5,6

References

1. Huffman, J.W., Liddle, J., Yu, S., et al. 3-(1',1'-Dimethylbutyl)-1-deoxy-Δ8-THC and related compounds: synthesis of selective ligands for the CB2 receptor. Bioorganic & Medicinal Chemistry 7, 2905-2914 (1999).
2. Casanova, M.L., Blázquez, C., Martínez-Palacio, J., et al. Inhibition of skin tumor growth and angiogenesis in vivo by activation of cannabinoid receptors. Journal of Clinical Investigation 111(1), 43-50 (2003).
3. Blázquez, C., Casanova, M.L., Planas, A., et al. Inhibition of tumor angiogenesis by cannabinoids. The FASEB Journal 17, 529-531 (2003).
4. Kimball, E.S., Schneider, C.R., Wallace, N.H., et al. Agonists of cannabinoid receptor 1 and 2 inhibit experimental colitis induced by oil of mustard and by dextran sulfate sodium. American Journal of Physiology and Gastrointestinal Liver Physiology 291(2), G364-G371 (2006).
5. Michler, T., Storr, M., Kramer, J., et al. Activation of cannabinoid receptor 2 reduces inflammation in acute experimental pancreatitis via intra-acinar activation of p38 and MK2-dependent mechanisms. American Journal of Physiology and Gastrointestinal Liver Physiology 304(2), G181-G192 (2013).
6. Ramirez, S.H., Haskó, J., Skuba, A., et al. Activation of cannabinoid receptor 2 attenuates leukocyte-endothelial cell interactions and blood-brain barrier dysfunction under inflammatory conditions. Journal of Neuroscience 32(12), 4004-4016 (2012).