IndraLab

Statements

Desipramine inhibits KCNH2. 16 / 20
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"To further assess pro apoptotic effects of hERG antagonism, we applied the antidepressant drug desipramine that has previously been shown to reduce hERG currents and prevent hERG protein trafficking to the plasma membrane XREF_BIBR."
24516604
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"Pentamidine and desipramine were reported to suppress hERG forward trafficking to the cell surface, and the aromatic amino F656 mediated the effects of pentamidine [XREF_BIBR, XREF_BIBR]."
27690007
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"XREF_BIBR Like probucol, desipramine accelerates degradation of mature hERG in HEK293 cells without interfering with Hsp90 and Hsp70 chaperones."
33763655
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"The antidepressant drug desipramine that blocks hERG protein trafficking to the plasma membrane XREF_BIBR exhibited pro apoptotic effects similar to doxazosin (XREF_FIG)."
24516604
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"This indicates that the hERG channels were only slightly blocked by desipramine while remaining at the holding potential."
20211602
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"In order to address the question as to whether the hERG channels are also blocked by desipramine in its inactivated state, a long test pulse to +80 mV (4 s) was applied to inactivate the channels, whi[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
20211602
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"Overall, desipramine inhibits the hERG channels mainly in the open and inactivated state rather than in the closed state.Previous studies reported that two aromatic residues, Tyr-652 and Phe-656, whic[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
20211602
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"The potency of a channel block for the wild type and two mutant hERG channels (Y652A and F656A) were compared in order to determine if these key residues are also important in the desipramine-induced [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
20211602
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"It was shown that desipramine inhibits the major component of I Kr , hERG, which suggests that desipramine-induced cardiac arrhythmia may also result from hERG inhibition."
20211602
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"In this regard, the serotonin selective reuptake inhibitor fluoxetine, its metabolite norfluoxetine, and the tricyclic antidepressant desipramine disrupt ER processing of HERG, an effect thought to underlie drug induced (acquired) long QT syndrome [XREF_BIBR, XREF_BIBR]."
24530489
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"We found that desipramine reduced hERG currents by binding to a receptor site inside the channel pore."
21120454
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"The manner by which drugs can influence the number of hERG channels in the plasma membrane recently took on a further level of complexity with the demonstration that desipramine can inhibit the forwar[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
23538024
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"In rescue experiments, we found that they exert no reverse effect on pentamidine- or desipramine induced hERG trafficking defect, although quinidine has been reported to rescue trafficking deficient pore mutation hERG G601S based on the interaction with F656."
27690007
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"Desipramine, known to be an antidepressant drug, was demonstrated to suppress hERG K channels [39,40]."
35740340
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"Pentamidine and desipramine were reported to suppress hERG forward trafficking from the endoplasmic reticulum, and the aromatic amino F656 in S6 domain mediated the effects of pentamidine [XREF_BIBR, XREF_BIBR]."
27690007
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"Moreover, desipramine produced acute blockage of the hERG channel at the binding sites of Y652 and F656 [XREF_BIBR]."
27690007