Holiday Notification: Cayman Chemical will be closed Monday, May 28, 2012, in observance of the Memorial Day holiday.
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The peripheral cannabinoid (CB2) receptor is a G protein-coupled receptor (GPCR) that is localized predominantly in immune cells, monocytes, macrophages, and in several peripheral organs and binds the active component of cannabis, Δ9-tetrahydrocannabinol, as well as anandamide, an endogenous CB receptor ligand.1 GW 842166X is a CB2 receptor agonist with ED50 values of 91 and 63 nM in rat and human, respectively.2 When administered orally to rats in the Freund’s complete adjuvant (FCA) model of inflammatory pain, GW 842166X is highly potent with an ED50 value of 0.1 mg/kg and full reversal of hyperalgesia at 0.3 mg/kg.2
1
Khanolkar, A.D., Lu, D., Ibrahim, M., et al. Cannabilactones: A novel class of CB2 selective agonists with peripheral analgesic activity. J Med Chem506493-6500(2007).
2
Giblin, G.M.P., O'Shaughnessy, C.T., Naylor, A., et al. Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro-2H-pyran-4-yl)methyl]-4-(trifluoromethyl)-5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain. J Med Chem50(11)2597-2600(2007).
Khanolkar, A.D., Lu, D., Ibrahim, M., et al. Cannabilactones: A novel class of CB2 selective agonists with peripheral analgesic activity. J Med Chem506493-6500(2007).
Giblin, G.M.P., O'Shaughnessy, C.T., Naylor, A., et al. Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro-2H-pyran-4-yl)methyl]-4-(trifluoromethyl)-5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain. J Med Chem50(11)2597-2600(2007).
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