A-836,339 Explained

A-836,339 is a drug developed by Abbott Laboratories that acts as a potent cannabinoid receptor full agonist. It is selective for CB₂, with K_i values of 0.64 nM at CB₂ vs 270 nM at the psychoactive CB₁ receptor, but while it exhibits selective analgesic, anti-inflammatory and anti-hyperalgesic effects at low doses,^[1] its high efficacy at both targets results in typical cannabis-like effects appearing at higher doses, despite its low binding affinity for CB₁.^[2] In 2012 A-836,339 was detected via X-ray crystallography in a "dubious product" sold in Japan, though the product was described as a white powder, not herbal incense, it was suggested to be for human consumption.^[3]

References

1. McGaraughty S, Chu KL, Dart MJ, Yao BB, Meyer MD . A CB(2) receptor agonist, A-836339, modulates wide dynamic range neuronal activity in neuropathic rats: contributions of spinal and peripheral CB(2) receptors . Neuroscience . 158 . 4 . 1652–61 . February 2009 . 19063946 . 10.1016/j.neuroscience.2008.11.015 . 207244894 .
2. Yao BB, Hsieh G, Daza AV, Fan Y, Grayson GK, Garrison TR, El Kouhen O, Hooker BA, Pai M, Wensink EJ, Salyers AK, Chandran P, Zhu CZ, Zhong C, Ryther K, Gallagher ME, Chin CL, Tovcimak AE, Hradil VP, Fox GB, Dart MJ, Honore P, Meyer MD . 46602629 . 6 . Characterization of a cannabinoid CB2 receptor-selective agonist, A-836339 [2,2,3,3-tetramethyl-cyclopropanecarboxylic acid [3-(2-methoxy-ethyl)-4,5-dimethyl-3H-thiazol-(2Z)-ylidene]-amide], using in vitro pharmacological assays, in vivo pain models, and pharmacological magnetic resonance imaging . The Journal of Pharmacology and Experimental Therapeutics . 328 . 1 . 141–51 . January 2009 . 18931146 . 10.1124/jpet.108.145011 .
3. Uemura N, Fukaya H, Kanai C, Yoshida M, Nakajima JI, Takahashi M, Suzuki J, Moriyasu T, Nakae D . 6 . Identification of a synthetic cannabinoid A-836339 as a novel compound found in a product. Forensic Toxicology . 2013 . 10.1007/s11419-013-0201-x . 32 . 45–50 . 24846364 .