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10.1124/mol.110.066928 http://scihub22266oqcxt.onion/10.1124/mol.110.066928 20926757!3014278!20926757     free     free     free Deprecated: Implicit conversion from float 229.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 229.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 229.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 229.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 229.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 229.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 229.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 229.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       Mol+Pharmacol 2011 ; 79 (1): 42-50 Nephropedia Template TP {{tp|p=20926757|t=2011. Development of a selective small-molecule inhibitor of Kir1 1, the renal outer medullary potassium channel |pdf=|usr=}}{{20926757}} gab.com Text Development of a selective small-molecule inhibitor of Kir1 1, the renal outer medullary potassium channel JO: Mol Pharmacol http://www.kidney.de/pget.php?&tw=1&pmid=20926757 #FOAvip The renal outer medullary potassium (K+) channel, ROMK (Kir1.1), is a putative drug target for a novel class of loop diuretic that would lower blood volume and pressure without causing hypokalemia. However, the lack of selective ROMK inhibitors has hindered efforts to assess its therapeutic potential. In a high-throughput screen for small-molecule modulators of ROMK, we previously identified a potent and moderately selective ROMK antagonist, 7,13-bis(4-nitrobenzyl)-1,4,10-trioxa-7,13-diazacyclopentadecane (VU590), that also inhibits Kir7.1. Because ROMK and Kir7.1 are coexpressed in the nephron, VU590 is not a good probe of ROMK function in the kidney. Here we describe the development of the structurally related inhibitor 2,2'-oxybis(methylene)bis(5-nitro-1H-benzo[d]imidazole) (VU591), which is as potent as VU590 but is selective for ROMK over Kir7.1 and more than 65 other potential off-targets. VU591 seems to block the intracellular pore of the channel. The development of VU591 may enable studies to explore the viability of ROMK as a diuretic target. Twit Text FOAVip Development of a selective small-molecule inhibitor of Kir1 1, the renal outer medullary potassium channel ????Mol Pharmacol http://www.kidney.de/pget.php?&tw=1&pmid=20926757 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=20926757 #FOAvip English Wikipedia <ref>{{Cite pmid|20926757}}</ref> Development of a selective small-molecule inhibitor of Kir1 1, the renal outer medullary potassium channel #MMPMID20926757 Bhave G; Chauder BA; Liu W; Dawson ES; Kadakia R; Nguyen TT; Lewis LM; Meiler J; Weaver CD; Satlin LM; Lindsley CW; Denton JS Mol Pharmacol 2011[Jan]; 79 (1): 42-50 PMID20926757show ga The renal outer medullary potassium (K+) channel, ROMK (Kir1.1), is a putative drug target for a novel class of loop diuretic that would lower blood volume and pressure without causing hypokalemia. However, the lack of selective ROMK inhibitors has hindered efforts to assess its therapeutic potential. In a high-throughput screen for small-molecule modulators of ROMK, we previously identified a potent and moderately selective ROMK antagonist, 7,13-bis(4-nitrobenzyl)-1,4,10-trioxa-7,13-diazacyclopentadecane (VU590), that also inhibits Kir7.1. Because ROMK and Kir7.1 are coexpressed in the nephron, VU590 is not a good probe of ROMK function in the kidney. Here we describe the development of the structurally related inhibitor 2,2'-oxybis(methylene)bis(5-nitro-1H-benzo[d]imidazole) (VU591), which is as potent as VU590 but is selective for ROMK over Kir7.1 and more than 65 other potential off-targets. VU591 seems to block the intracellular pore of the channel. The development of VU591 may enable studies to explore the viability of ROMK as a diuretic target. |Animals[MESH] |Benzimidazoles/*chemical synthesis/*metabolism[MESH] |Cricetinae[MESH] |Female[MESH] |HEK293 Cells[MESH] |Humans[MESH] |Kidney Medulla/*metabolism[MESH] |Mice[MESH] |Potassium Channel Blockers/*chemical synthesis/*metabolism[MESH] |Potassium Channels, Inwardly Rectifying/*antagonists & inhibitors/*metabolism[MESH] |Potassium Channels/chemistry/metabolism[MESH] |Protein Binding/drug effects/physiology[MESH] |Rats[MESH]Development of a selective small-molecule inhibitor of Kir1 1, the ren(epmc).pdf DeepDyve Pubget Overpricing