666260-75-9 Usage
Description
The peripheral cannabinoid (CB2) receptor is a G protein-coupled receptor (GPCR) that is localized predominantly in immune cells, monocytes, macrophages, and in several peripheral organs and binds the active component of cannabis, Δ9-tetrahydrocannabinol, as well as anandamide, an endogenous CB receptor ligand. GW 842166X is a peripheral cannabinoid (CB2) receptor agonist with ED50 values of 91 and 63 nM in rat and human, respectively. When administered orally to rats in the Freund’s complete adjuvant (FCA) model of inflammatory pain, GW 842166X is highly potent with an ED50 value of 0.1 mg/kg and full reversal of hyperalgesia at 0.3 mg/kg.
Uses
GW-842166X is pyrimidine ester based compound that is known as a highly selective CB2 receptor agonist for the treatment of inflammatory and neuropathic pain.
Check Digit Verification of cas no
The CAS Registry Mumber 666260-75-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 6,6,6,2,6 and 0 respectively; the second part has 2 digits, 7 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 666260-75:
(8*6)+(7*6)+(6*6)+(5*2)+(4*6)+(3*0)+(2*7)+(1*5)=179
179 % 10 = 9
So 666260-75-9 is a valid CAS Registry Number.
InChI:InChI=1/C18H17Cl2F3N4O2/c19-11-1-2-14(13(20)7-11)26-17-25-9-12(15(27-17)18(21,22)23)16(28)24-8-10-3-5-29-6-4-10/h1-2,7,9-10H,3-6,8H2,(H,24,28)(H,25,26,27)
666260-75-9Relevant articles and documents
Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro-2H-pyran-4-yl) methyl]-4-(trifluoromethyl)-5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain
Giblin, Gerard M. P.,O'Shaughnessy, Celestine T.,Naylor, Alan,Mitchell, William L.,Eatherton, Andrew J.,Slingsby, Brian P.,Rawlings, D. Anthony,Goldsmith, Paul,Brown, Andrew J.,Haslam, Carl P.,Clayton, Nick M.,Wilson, Alex W.,Chessell, Iain P.,Wittington, Andrew R.,Green, Richard
, p. 2597 - 2600 (2008/02/03)
Selective CB2 receptor agonists are promising potential therapeutic agents for the treatment of inflammatory and neuropathic pain. A focused screen identified a pyrimidine ester as a partial agonist at the CB2 receptor with micromolar potency. Subsequent lead optimization identified 35, GW842166X, as the optimal compound in the series. 35 has an oral ED50 of 0.1 mg/kg in the rat FCA model of inflammatory pain and was selected as a clinical candidate for this indication.
PYRIMIDINE DERIVATIVES AND THEIR USE AS CB2 MODULATORS
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Page 41, (2010/02/06)
This relates to novel pyrimidine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in activity of
