A-796,260

From Wikipedia, the free encyclopedia
Jump to: navigation, search
A-796,260
A-796260 structure.png
Identifiers
CAS Number
PubChem CID
ChemSpider
ChEMBL
ECHA InfoCard 100.233.198
Chemical and physical data
Formula C22H30N2O2
Molar mass 354.485 g/mol
3D model (Jmol)
 NYesY (what is this?)  (verify)

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 Ki 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[edit]

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

See also[edit]

References[edit]

  1. ^ Frost, J. M.; et al. (2010). "Indol-3-ylcycloalkyl Ketones: Effects of N1 Substituted Indole Side Chain Variations on CB2 Cannabinoid Receptor Activity". Journal of Medicinal Chemistry. 53 (1): 295–315. doi:10.1021/jm901214q. PMID 19921781. 
  2. ^ Yao BB; et al. (January 2008). "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. doi:10.1038/sj.bjp.0707568. PMC 2219533Freely accessible. PMID 17994110. 
  3. ^ "关于印发《非药用类麻醉药品和精神药品列管办法》的通知" (in Chinese). China Food and Drug Administration. 27 September 2015. Retrieved 1 October 2015.