Literature DB >> 18438986

Structure-activity relationship studies on N'-aryl carbohydrazide P2X7 antagonists.

Derek W Nelson1, Kathy Sarris, Douglas M Kalvin, Marian T Namovic, George Grayson, Diana L Donnelly-Roberts, Richard Harris, Prisca Honore, Michael F Jarvis, Connie R Faltynek, William A Carroll.   

Abstract

N'-aryl acyl hydrazides were identified as P2X7 receptor antagonists. Structure-activity relationship (SAR) studies evaluated functional activity by monitoring calcium flux inhibition in cell lines expressing recombinant human and rat P2X7 receptors. Selected analogs were assayed in vitro for their capacity to inhibit release of cytokine IL-1beta. Compounds with potent antagonist function were evaluated in vivo using the zymosan-induced peritonitis model. A representative compound effectively attenuated mechanical allodynia in a rat model of neuropathic pain.

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Year:  2008        PMID： 18438986     DOI： 10.1021/jm701516f

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  11 in total

1.  P2X(7) Receptors in Neurological and Cardiovascular Disorders.

Authors:  Stephen D Skaper; Patrizia Debetto; Pietro Giusti
Journal:  Cardiovasc Psychiatry Neurol       Date:  2009-06-24

2.  Flow Synthesis and Biological Studies of an Analgesic Adamantane Derivative That Inhibits P2X7-Evoked Glutamate Release.

Authors:  Claudio Battilocchio; Lucie Guetzoyan; Chiara Cervetto; Lorenzo Di Cesare Mannelli; Daniela Frattaroli; Ian R Baxendale; Guido Maura; Antonietta Rossi; Lidia Sautebin; Mariangela Biava; Carla Ghelardini; Manuela Marcoli; Steven V Ley
Journal:  ACS Med Chem Lett       Date:  2013-05-22       Impact factor: 4.345

3.  Effects of extracellular ATP on bovine lung endothelial and epithelial cell monolayer morphologies, apoptoses, and permeabilities.

Authors:  David McClenahan; Kati Hillenbrand; Arvinder Kapur; David Carlton; Charles Czuprynski
Journal:  Clin Vaccine Immunol       Date:  2008-11-05

4.  Mitochondrial superoxide generation enhances P2X7R-mediated loss of cell surface CD62L on naive human CD4+ T lymphocytes.

Authors:  John G Foster; Edward Carter; Iain Kilty; Amanda B MacKenzie; Stephen G Ward
Journal:  J Immunol       Date:  2013-01-14       Impact factor: 5.422

Review 5.  Recent patents on novel P2X(7) receptor antagonists and their potential for reducing central nervous system inflammation.

Authors:  Scott A Friedle; Marjorie A Curet; Jyoti J Watters
Journal:  Recent Pat CNS Drug Discov       Date:  2010-01

6.  Natural compounds with P2X7 receptor-modulating properties.

Authors:  Wolfgang Fischer; Nicole Urban; Kerstin Immig; Heike Franke; Michael Schaefer
Journal:  Purinergic Signal       Date:  2013-10-27       Impact factor: 3.765

7.  Current and emerging "at-site" pain medications: a review.

Authors:  Praveen Pn Rao; Tarek Mohamed
Journal:  J Pain Res       Date:  2011-09-08       Impact factor: 3.133

8.  P2X7 receptor-deficient mice are susceptible to bone cancer pain.

Authors:  Rikke Rie Hansen; Christian K Nielsen; Arafat Nasser; Stine I M Thomsen; Laura F Eghorn; Yen Pham; Cecilia Schulenburg; Susanne Syberg; Ming Ding; Stanko S Stojilkovic; Niklas R Jorgensen; Anne-Marie Heegaard
Journal:  Pain       Date:  2011-05-11       Impact factor: 7.926

9.  Adamantyl analogues of paracetamol as potent analgesic drugs via inhibition of TRPA1.

Authors:  Nieves Fresno; Ruth Pérez-Fernández; Carlos Goicoechea; Ibon Alkorta; Asia Fernández-Carvajal; Roberto de la Torre-Martínez; Susana Quirce; Antonio Ferrer-Montiel; M Isabel Martín; Pilar Goya; José Elguero
Journal:  PLoS One       Date:  2014-12-01       Impact factor: 3.240

10.  Selective P2X(7) receptor antagonists for chronic inflammation and pain.

Authors:  William A Carroll; Diana Donnelly-Roberts; Michael F Jarvis
Journal:  Purinergic Signal       Date:  2008-06-21       Impact factor: 3.765
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