Literature DB >> 20579878

Structure-activity relationships and in vivo activity of (1H-pyrazol-4-yl)acetamide antagonists of the P2X(7) receptor.

Paul J Beswick1, 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.   

Abstract

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]. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20579878     DOI: 10.1016/j.bmcl.2010.05.107

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

Review 1.  Molecular and functional properties of P2X receptors--recent progress and persisting challenges.

Authors:  Karina Kaczmarek-Hájek; Eva Lörinczi; Ralf Hausmann; Annette Nicke
Journal:  Purinergic Signal       Date:  2012-05-01       Impact factor: 3.765

Review 2.  Purinergic signalling in the musculoskeletal system.

Authors:  Geoffrey Burnstock; Timothy R Arnett; Isabel R Orriss
Journal:  Purinergic Signal       Date:  2013-08-14       Impact factor: 3.765

Review 3.  Purinergic Signalling: Therapeutic Developments.

Authors:  Geoffrey Burnstock
Journal:  Front Pharmacol       Date:  2017-09-25       Impact factor: 5.810

4.  Synthesis, SAR, and Pharmacological Characterization of Brain Penetrant P2X7 Receptor Antagonists.

Authors:  Brad M Savall; Duncan Wu; Meri De Angelis; Nicholas I Carruthers; Hong Ao; Qi Wang; Brian Lord; Anindya Bhattacharya; Michael A Letavic
Journal:  ACS Med Chem Lett       Date:  2015-04-24       Impact factor: 4.345

Review 5.  Recent Advances in CNS P2X7 Physiology and Pharmacology: Focus on Neuropsychiatric Disorders.

Authors:  Anindya Bhattacharya
Journal:  Front Pharmacol       Date:  2018-02-01       Impact factor: 5.810

Review 6.  The potential of P2X7 receptors as a therapeutic target, including inflammation and tumour progression.

Authors:  Geoffrey Burnstock; Gillian E Knight
Journal:  Purinergic Signal       Date:  2017-11-21       Impact factor: 3.765

  6 in total

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