IndraLab

Statements


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"Probucol induced hERG channel reduction can be rescued by matrine and oxymatrine in vitro."

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"XREF_BIBR, XREF_BIBR Our data show that probucol (30, 50, and 100 muM) treatment decreases the mature 155 kDa band of hERG, but does not reduce the intracellular forms of the immature hERG 135 kDa band (XREF_FIG), suggesting that probucol may not block hERG forward trafficking."

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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."

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"XREF_BIBR By decreasing hERG channel-membrane density, probucol can cause LQTS and torsades de pointes arrhythmia in patients and sudden cardiac death in experimental animals."

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"Therefore, we speculate that maybe LDL cholesterol could also protect QTc interval from prolongation in schizophrenia patients treated with antipsychotics just through such a similar mechanism as preventing probucol-induced reduction of the hERG current."

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"Probucol also disrupted hERG trafficking and did not block hERG channels expressed in human embryonic kidney 293 cells."

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"Our data demonstrate that probucol accelerated the degradation of mature hERG channels, which associated with caveolin-1 (Cav1) in hERG expressing HEK cells."