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Structure–activity relationships and in vivo activity of (1H-pyrazol-4-yl)acetamide antagonists of the P2X7 receptor

✍ Scribed by Paul J. Beswick; Andy Billinton; Laura J. Chambers; David K. Dean; Elena Fonfria; Robert J. Gleave; Stephen J. Medhurst; Anton D. Michel; Andrew P. Moses; Sadhana Patel; Shilina A. Roman; Sue Roomans; Stefan Senger; Alexander J. Stevens; Daryl S. Walter

Publisher
Elsevier Science
Year
2010
Tongue
English
Weight
381 KB
Volume
20
Category
Article
ISSN
0960-894X

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✦ Synopsis

Structure-activity relationships (SAR) of analogues of lead compound 1 were investigated and compound 16 was selected for further study in animal models of pain. Compound 16 was shown to be a potent antihyperalgesic agent in both the rat acute complete Freund's adjuvant (CFA) model of inflammatory pain [Iadarola, M. J.; Douglass, J.; Civelli, O.; Naranjo, J. R. rain Res.1988, 455, 205] and the knee joint model of chronic inflammatory pain [Wilson, A. W.; Medhurst, S. J.; Dixon, C. I.; Bontoft, N. C.; Winyard, L. A.; Brackenborough, K. T.; De Alba, J.; Clarke, C. J.; Gunthorpe, M. J.; Hicks, G. A.; Bountra, C.; McQueen, D. S.; Chessell, I. P. Eur. J. Pain2006, 10, 537].

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