IndraLab

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"Indeed, moxifloxacin (40), fluvoxamine (41), and, recently, doxepin (42) have been reported to inhibit hERG with a mixed state-dependence of inhibition (with components of both closed- and open-channe[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"Milnes et al. [XREF_BIBR] reported that fluvoxamine inhibits HERG potassium channels with rapid onset and its inhibition is only partially reduced in F656A mutant channels, which are known to profoundly attenuate the inhibition of HERG channels by many known QT prolonging drugs."

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"Vesnarinone does not require Tyr-652 [16] , and fluvoxamine can block hERG when there are mutations in Phe-656 or Tyr-652 [17] ."

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"Also worth noting is the exclusion from Pred-hERG AD of 11 hERG blockers including namely clarithromycin, digoxin, epinastine, erythromycin, furosemide, fluvoxamine, mexiletine, perhexiline, procainam[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"The rapid onset of HERG channel block by fluvoxamine seemed to be consistent with binding to an extracellular site on the HERG channel, possibly at the outer mouth of the channel where erg-specific to[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"However, some exceptions have been found, vesnarinone does not require Y652 ( Kamiya et al., 2001 ) and fluvoxamine and dronedarone, which can block HERG when F656 and Y652 are mutated ( Milnes et al.[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"