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10.1124/jpet.120.000484 http://scihub22266oqcxt.onion/10.1124/jpet.120.000484 33674391!ä!33674391 Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 247.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 247.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       J+Pharmacol+Exp+Ther 2021 ; 377 (2): 265-272 Nephropedia Template TP {{tp|p=33674391|t=2021. COVID-19 Drugs Chloroquine and Hydroxychloroquine, but Not Azithromycin and Remdesivir, Block hERG Potassium Channels |pdf=|usr=}}{{33674391}} gab.com Text COVID-19 Drugs Chloroquine and Hydroxychloroquine, but Not Azithromycin and Remdesivir, Block hERG Potassium Channels JO: J Pharmacol Exp Ther http://www.kidney.de/pget.php?&tw=1&pmid=33674391 #FOAvip Drug-induced long QT syndrome (LQTS) is an established cardiac side effect of a wide range of medications and represents a significant concern for drug safety. The rapidly and slowly activating delayed rectifier K(+) currents, mediated by channels encoded by the human ether-a-go-go-related gene (hERG) and KCNQ1 + KCNE1, respectively, are two main currents responsible for ventricular repolarization. The common cause for drugs to induce LQTS is through impairing the hERG channel. For the recent emergence of COVID-19, caused by severe acute respiratory syndrome coronavirus 2, several drugs have been investigated as potential therapies; however, there are concerns about their QT prolongation risk. Here, we studied the effects of chloroquine, hydroxychloroquine, azithromycin, and remdesivir on hERG channels. Our results showed that although chloroquine acutely blocked hERG current (I(hERG)), with an IC(50) of 3.0 microM, hydroxychloroquine acutely blocked I(hERG) 8-fold less potently, with an IC(50) of 23.4 microM. Azithromycin and remdesivir did not acutely affect I(hERG) When these drugs were added at 10 microM to the cell culture medium for 24 hours, remdesivir increased I(hERG) by 2-fold, which was associated with an increased mature hERG channel expression. In addition, these four drugs did not acutely or chronically affect KCNQ1 + KCNE1 channels. Our data provide insight into COVID-19 drug-associated LQTS and cardiac safety concerns. SIGNIFICANCE STATEMENT: This work demonstrates that, among off-label potential COVID-19 treatment drugs chloroquine, hydroxychloroquine, azithromycin, and remdesivir, the former two drugs block hERG potassium channels, whereas the latter two drugs do not. All four drugs do not affect KCNQ1 + KCNE1. As hERG and KCNQ1 + KCNE1 are two main K(+) channels responsible for ventricular repolarization, and most drugs that induce long QT syndrome (LQTS) do so by impairing hERG channels, these data provide insight into COVID-19 drug-associated LQTS and cardiac safety concerns. Twit Text FOAVip COVID-19 Drugs Chloroquine and Hydroxychloroquine, but Not Azithromycin and Remdesivir, Block hERG Potassium Channels ????J Pharmacol Exp Ther http://www.kidney.de/pget.php?&tw=1&pmid=33674391 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=33674391 #FOAvip English Wikipedia <ref>{{Cite pmid|33674391}}</ref> COVID-19 Drugs Chloroquine and Hydroxychloroquine, but Not Azithromycin and Remdesivir, Block hERG Potassium Channels #MMPMID33674391 Szendrey M; Guo J; Li W; Yang T; Zhang S J Pharmacol Exp Ther 2021[May]; 377 (2): 265-272 PMID33674391show ga Drug-induced long QT syndrome (LQTS) is an established cardiac side effect of a wide range of medications and represents a significant concern for drug safety. The rapidly and slowly activating delayed rectifier K(+) currents, mediated by channels encoded by the human ether-a-go-go-related gene (hERG) and KCNQ1 + KCNE1, respectively, are two main currents responsible for ventricular repolarization. The common cause for drugs to induce LQTS is through impairing the hERG channel. For the recent emergence of COVID-19, caused by severe acute respiratory syndrome coronavirus 2, several drugs have been investigated as potential therapies; however, there are concerns about their QT prolongation risk. Here, we studied the effects of chloroquine, hydroxychloroquine, azithromycin, and remdesivir on hERG channels. Our results showed that although chloroquine acutely blocked hERG current (I(hERG)), with an IC(50) of 3.0 microM, hydroxychloroquine acutely blocked I(hERG) 8-fold less potently, with an IC(50) of 23.4 microM. Azithromycin and remdesivir did not acutely affect I(hERG) When these drugs were added at 10 microM to the cell culture medium for 24 hours, remdesivir increased I(hERG) by 2-fold, which was associated with an increased mature hERG channel expression. In addition, these four drugs did not acutely or chronically affect KCNQ1 + KCNE1 channels. Our data provide insight into COVID-19 drug-associated LQTS and cardiac safety concerns. SIGNIFICANCE STATEMENT: This work demonstrates that, among off-label potential COVID-19 treatment drugs chloroquine, hydroxychloroquine, azithromycin, and remdesivir, the former two drugs block hERG potassium channels, whereas the latter two drugs do not. All four drugs do not affect KCNQ1 + KCNE1. As hERG and KCNQ1 + KCNE1 are two main K(+) channels responsible for ventricular repolarization, and most drugs that induce long QT syndrome (LQTS) do so by impairing hERG channels, these data provide insight into COVID-19 drug-associated LQTS and cardiac safety concerns. |*COVID-19 Drug Treatment[MESH] |Adenosine Monophosphate/*analogs & derivatives/pharmacology/therapeutic use[MESH] |Alanine/*analogs & derivatives/pharmacology/therapeutic use[MESH] |Anti-Bacterial Agents/pharmacology/therapeutic use[MESH] |Antimalarials/pharmacology/therapeutic use[MESH] |Antiviral Agents/pharmacology/therapeutic use[MESH] |Azithromycin/*pharmacology/therapeutic use[MESH] |COVID-19/metabolism[MESH] |Chloroquine/*pharmacology/therapeutic use[MESH] |Dose-Response Relationship, Drug[MESH] |ERG1 Potassium Channel/*antagonists & inhibitors/metabolism[MESH] |HEK293 Cells[MESH] |Humans[MESH] |Hydroxychloroquine/*pharmacology/therapeutic use[MESH]COVID-19 Drugs Chloroquine and Hydroxychloroquine, but Not Azithromyci(epmc).pdf DeepDyve Pubget Overpricing