A-796,260

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A-796,260
A-796260 structure.png
Systematic (IUPAC) name
1-(2-morpholin-4-ylethyl)-1H-indol-3-yl]-(2,2,3,3-tetramethylcyclopropyl)methanone
Clinical data
Legal status
?
Identifiers
CAS number 895155-26-7 N
ATC code ?
PubChem CID 11584525
ChemSpider 9759290 YesY
ChEMBL CHEMBL262865 YesY
Chemical data
Formula C22H30N2O2 
Mol. mass 354.485 g/mol
 N (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]

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.  edit
  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 2219533. PMID 17994110.