IndraLab

Statements

Desipramine inhibits KCNH2. 12 / 14
2 | 10
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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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"Moreover, desipramine produced acute blockage of the hERG channel at the binding sites of Y652 and F656 [XREF_BIBR]."
27690007
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"We found that desipramine reduced hERG currents by binding to a receptor site inside the channel pore."
21120454
ctd
No evidence text available
24052561
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"The IC (50) for desipramine needed to block the hERG current in Xenopus oocytes decreased progressively relative to the degree of depolarization."
20211602
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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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"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
ctd
No evidence text available
20211602
reach
"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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"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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"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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"XREF_BIBR Like probucol, desipramine accelerates degradation of mature hERG in HEK293 cells without interfering with Hsp90 and Hsp70 chaperones."
33763655