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

Autor:	Celestine T. O'Shaughnessy, Gerard Martin Paul Giblin, Brian Peter Slingsby, Carl Haslam, Alan Naylor, Andrew John Eatherton, Alex W. Wilson, and Andrew R. Wittington, Nick M. Clayton, Richard D. Green, Paul Goldsmith, William L. Mitchell, D. Anthony Rawlings, Andrew J. Brown, Iain P. Chessell
Rok vydání:	2007
Předmět:	Agonist Trifluoromethyl medicine.drug_class Stereochemistry Analgesic Partial agonist chemistry.chemical_compound chemistry Pyran Drug Discovery Neuropathic pain Hyperalgesia Cannabinoid receptor type 2 medicine Molecular Medicine lipids (amino acids peptides and proteins) medicine.symptom
Zdroj:	Journal of Medicinal Chemistry. 50:2597-2600
ISSN:	1520-4804 0022-2623
DOI:	10.1021/jm061195+
Popis:	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.
Databáze:	OpenAIRE
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