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10.1038/sj.bjp.0706933 http://scihub22266oqcxt.onion/10.1038/sj.bjp.0706933 C2014691!2014691!17031385     free     free     free Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       Br+J+Pharmacol 2006 ; 149 (7): 880-7 Nephropedia Template TP {{tp|p=17031385|t=2006. Characterization of a selective and potent antagonist of human P2X7 receptors, AZ11645373 |pdf=|usr=}}{{17031385}} gab.com Text Characterization of a selective and potent antagonist of human P2X7 receptors, AZ11645373 JO: Br J Pharmacol http://www.kidney.de/pget.php?&tw=1&pmid=17031385 #FOAvip Background and purpose:: The ATP-gated P2X7 receptor has been shown to play a role in several inflammatory processes, making it an attractive target for anti-inflammatory drug discovery. We have recently identified a novel set of cyclic imide compounds that inhibited P2X7 receptor-mediated dye uptake in human macrophage THP-1 cells. In this study the actions and selectivity of one of these compounds, AZ11645373, were characterized. Experimental approach:: We measured membrane currents, calcium influx, and YOPRO-1 uptake from HEK cells expressing individual P2X receptors, and YOPRO1 uptake and interleukin-1? release from THP-1 cells in response to ATP and the ATP analogue benzoylbenzoyl ATP (BzATP). Key results:: AZ11645373 up to 10 ?M, had no agonist or antagonist actions on membrane currents due to P2X receptor activation at human P2X1, rat P2X2, human P2X3, rat P2X2/3, human P2X4, or human P2X5 receptors expressed in HEK cells. AZ11645373 inhibited human P2X7 receptor responses in HEK cells in a non-surmountable manner with KB values ranging from 5 - 20 nM, with mean values not significantly different between assays. KB values were not altered by removing extracellular calcium and magnesium. ATP-evoked IL-1? release from lipopolysaccharide-activated THP-1 cells was inhibited by AZ11645373, IC50 = 90 nM. AZ11645373 was > 500-fold less effective at inhibiting rat P2X7 receptor-mediated currents with less than 50% inhibition occurring at 10 ?M. Conclusions and implications:: AZ11645373 is a highly selective and potent antagonist at human but not rat P2X7 receptors and will have much practical value in studies of human cells. Twit Text FOAVip Characterization of a selective and potent antagonist of human P2X7 receptors, AZ11645373 ????Br J Pharmacol http://www.kidney.de/pget.php?&tw=1&pmid=17031385 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=17031385 #FOAvip English Wikipedia <ref>{{Cite pmid|17031385}}</ref> Characterization of a selective and potent antagonist of human P2X7 receptors, AZ11645373 #MMPMID17031385 Stokes L; Jiang LH; Alcaraz L; Bent J; Bowers K; Fagura M; Furber M; Mortimore M; Lawson M; Theaker J; Laurent C; Braddock M; Surprenant A Br J Pharmacol 2006[Nov]; 149 (7): 880-7 PMID17031385show ga Background and purpose:: The ATP-gated P2X7 receptor has been shown to play a role in several inflammatory processes, making it an attractive target for anti-inflammatory drug discovery. We have recently identified a novel set of cyclic imide compounds that inhibited P2X7 receptor-mediated dye uptake in human macrophage THP-1 cells. In this study the actions and selectivity of one of these compounds, AZ11645373, were characterized. Experimental approach:: We measured membrane currents, calcium influx, and YOPRO-1 uptake from HEK cells expressing individual P2X receptors, and YOPRO1 uptake and interleukin-1? release from THP-1 cells in response to ATP and the ATP analogue benzoylbenzoyl ATP (BzATP). Key results:: AZ11645373 up to 10 ?M, had no agonist or antagonist actions on membrane currents due to P2X receptor activation at human P2X1, rat P2X2, human P2X3, rat P2X2/3, human P2X4, or human P2X5 receptors expressed in HEK cells. AZ11645373 inhibited human P2X7 receptor responses in HEK cells in a non-surmountable manner with KB values ranging from 5 - 20 nM, with mean values not significantly different between assays. KB values were not altered by removing extracellular calcium and magnesium. ATP-evoked IL-1? release from lipopolysaccharide-activated THP-1 cells was inhibited by AZ11645373, IC50 = 90 nM. AZ11645373 was > 500-fold less effective at inhibiting rat P2X7 receptor-mediated currents with less than 50% inhibition occurring at 10 ?M. Conclusions and implications:: AZ11645373 is a highly selective and potent antagonist at human but not rat P2X7 receptors and will have much practical value in studies of human cells. äCharacterization of a selective and potent antagonist of human P2X7 re(epmc).pdf DeepDyve Pubget Overpricing