A-796,260: Difference between revisions

{{Drugbox| verifiedrevid = 438395181

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|IUPAC_name = 1-(2-morpholin-4-ylethyl)-1H-indol-3-yl]-(2,2,3,3-tetramethylcyclopropyl)methanone

| CAS_number=

| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}

| StdInChI_Ref = {{stdinchicite|correct|chemspider}}

| molecular_weight = 354.485 g/mol

'''A-796,260''' is a drug developed by [[Abbott Laboratories]] which acts as a potent and selective [[cannabinoid]] [[Cannabinoid receptor 2|CB₂]] [[Receptor (biochemistry)|receptor]] [[agonist]]. Replacing the aromatic 3-[[benzoyl]] or 3-[[naphthoyl]] group found in most [[indole]] derived cannabinoids with the 3-[[methyl|tetramethyl]][[cyclopropyl]][[methanone]] 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 [[Dissociation constant#Protein-ligand binding|K_i]] of 0.77nM vs 2,100nM at CB₁.<ref>{{Cite doi|10.1038/sj.bjp.0707567}}</ref><ref>{{Cite doi|10.1021/jm901214q}}</ref> 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.<ref name="pmid17994110">{{cite journal |author=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 |title=In vitro and in vivo characterization of A-796260: a selective cannabinoid CB2 receptor agonist exhibiting analgesic activity in rodent pain models |journal=British Journal of Pharmacology |volume=153 |issue=2 |pages=390–401 |year=2008 |month=January |pmid=17994110 |pmc=2219533 |doi=10.1038/sj.bjp.0707568 |url=}}</ref>

==See also==

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