IndraLab

Statements

(2S,4R)-ketoconazole inhibits KCNH2. 8 / 8
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"These properties are compared with four known HERG channel blockers including verapamil, cisapride, ketoconazole and dofetilide in the XREF_TABLE."
23313619
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"The much lower ketoconazole block of hERG at negative potentials indicates that ketoconazole binds less to hERG closed state than open and inactivated ones.In this study, we described the biophysical [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
19720020
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"The mechanism of hERG inhibition by ketoconazole remains controversial (14-16)."
19720020
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"For example, the antiarrhythmic agents ketoconazole and fluoxetine have been shown to reduce hERG density by at least 50% following 48 hours of treatment, XREF_BIBR - XREF_BIBR whereas pentamidine and probucol reduce cell-surface hERG without affecting ion conduction."
20156596
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"Ketoconazole directly blocked the hERG channel current and reduced the amount of hERG channel protein trafficked to the cell surface in a concentration dependent manner."
17965736
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"Recent studies demonstrated that ketoconazole prolonged the QT not only through direct blockade of the IKr, but also by reducing the density (number of) of HERG potassium channels in the cell membrane."
20676275
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"Several studies suggest that ketoconazole inhibits hERG preferentially in the closed state (14,16)."
19720020
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"For example, ketoconazole was initially suggested inhibit hERG without a requirement for prior channel activation (Dumaine et al., 1998), but more recently it has been found to bind with a dependency [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
18616963