666260-75-9 Usage
Description
GW 842166X is a pyrimidine ester-based compound that acts as a highly selective peripheral cannabinoid (CB2) receptor agonist. It is known for its high potency in treating inflammatory and neuropathic pain, with ED50 values of 91 nM in rats and 63 nM in humans. When administered orally to rats in the Freund's complete adjuvant (FCA) model of inflammatory pain, GW 842166X demonstrates full reversal of hyperalgesia at a dosage of 0.3 mg/kg.
Uses
Used in Pharmaceutical Industry:
GW 842166X is used as an analgesic agent for the treatment of inflammatory and neuropathic pain. Its high selectivity for the CB2 receptor makes it a promising candidate for pain management without the psychoactive side effects associated with CB1 receptor agonists.
Used in Immune System Regulation:
GW 842166X is used as an immune modulator, targeting the CB2 receptors predominantly found in immune cells, monocytes, and macrophages. This selective targeting allows for potential therapeutic applications in modulating immune responses and treating immune-related disorders.
Used in Neuropathic Pain Management:
GW 842166X is used as a neuroprotective agent for the treatment of neuropathic pain. Its ability to selectively activate CB2 receptors may provide a novel approach to managing neuropathic pain without the side effects of traditional opioids or other pain medications.
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
