A-796,260 Explained

A-796,260 is a drug developed by Abbott Laboratories that acts as a potent and selective cannabinoid CB₂ receptor agonist. Replacing the aromatic 3-benzoyl or 3-naphthoyl group found in most indole derived cannabinoids with the 3-tetramethylcyclopropylmethanone group, imparts significant selectivity for CB₂, and A-796,260 was found to be a highly selective CB₂ agonist with little affinity for CB₁, having a CB₂ K_i of 4.6 nM vs 945 nM at CB₁.^[1] It has potent analgesic and anti-inflammatory actions in animal models, being especially effective in models of neuropathic pain, but without producing cannabis-like behavioral effects.^[2]

Legal Status

As of October 2015 A-796,260 is a controlled substance in China.^[3]

See also

• A-834,735
• A-836,339
• BMS-F
• JWH-200
• UR-144
• XLR-11

Notes and References

1. Frost JM, Dart MJ, Tietje KR, Garrison TR, Grayson GK, Daza AV, El-Kouhen OF, Yao BB, Hsieh GC, Pai M, Zhu CZ, Chandran P, Meyer MD . 6 . Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity . Journal of Medicinal Chemistry . 53 . 1 . 295–315 . January 2010 . 19921781 . 10.1021/jm901214q .
2. Yao BB, Hsieh GC, Frost JM, Fan Y, Garrison TR, Daza AV, Grayson GK, Zhu CZ, Pai M, Chandran P, Salyers AK, Wensink EJ, Honore P, Sullivan JP, Dart MJ, Meyer MD . 6 . In vitro and in vivo characterization of A-796260: a selective cannabinoid CB2 receptor agonist exhibiting analgesic activity in rodent pain models . British Journal of Pharmacology . 153 . 2 . 390–401 . January 2008 . 17994110 . 2219533 . 10.1038/sj.bjp.0707568 .
3. Web site: 关于印发《非药用类麻醉药品和精神药品列管办法》的通知 . China Food and Drug Administration . 27 September 2015 . Chinese . 1 October 2015 . https://web.archive.org/web/20151001222554/http://www.sfda.gov.cn/WS01/CL0056/130753.html . 1 October 2015 . dead .