A-836,339

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A-836,339
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Systematic (IUPAC) name
N-[3-(2-methoxyethyl)-4,5-dimethyl-1,3-thiazol-2-ylidene]-2,2,3,3-tetramethylcyclopropane-1-carboxamide
Identifiers
PubChem CID 17754357
Chemical data
Formula C16H26N2O2S
Molar mass 310.454 g/mol[[Script error: No such module "String".]]
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A-836,339 is a drug developed by Abbott Laboratories which acts as a potent cannabinoid receptor full agonist. It is selective for CB2, with Ki values of 0.64nM at CB2 vs 270nM 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]

References

  1. ↑ McGaraughty, S.; Chu, K.; Dart, M.; Yao, B.; Meyer, M. (2009). "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): 1652–1661. doi:10.1016/j.neuroscience.2008.11.015. PMID 19063946.  edit
  2. ↑ Yao, B.; Hsieh, G.; Daza, A.; Fan, Y.; Grayson, G.; Garrison, T.; El Kouhen, O.; Hooker, B.; Pai, M. (2009). "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): 141–151. doi:10.1124/jpet.108.145011. PMID 18931146.  edit
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