ArticleActa pharmacologica Sinica2010
State-dependent blockade of human ether-a-go-go-related gene (hERG) K(+) channels by changrolin in stably transfected HEK293 cells.
Article in Acta pharmacologica Sinica, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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4 citing papers in PubMed, 11 citations in OpenAlex.
- Characterization of Preclinical Pharmacokinetic Properties and Prediction of Human PK Using a Physiologically Based Pharmacokinetic Model for a Novel Anti-Arrhythmic Agent Sulcardine Sulfate.Pharmaceutical research · 2021Article
- Interleukin-6 inhibition of hERG underlies risk for acquired long QT in cardiac and systemic inflammation.PloS one · 2018Article
- Natural products modulating the hERG channel: heartaches and hope.Natural product reports · 2017Review
- Oral Bioavailability and Mass Balance Studies of a Novel Anti-arrhythmic Agent Sulcardine Sulfate in Sprague-Dawley Rats and Beagle Dogs.European journal of drug metabolism and pharmacokinetics · 2017Article
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Authors and funding
5 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimTo study the effect of changrolin on the K(+) channels encoded by the human ether-a-go-go-related gene (hERG).
methodshERG channels were heterologously stably expressed in human embryonic kidney 293 cells, and the hERG K(+) currents were recorded using a standard whole-cell patch-clamp technique.
resultsChangrolin inhibited hERG channels in a concentration-dependent and reversible manner (IC(50)=18.23 mumol/L, 95% CI: 9.27-35.9 mumol/L; Hill coefficient=-0.9446). In addition, changrolin shifted the activation curve of hERG channels by 14.3+/-1.5 mV to more negative potentials (P<0.01, n=9) but did not significantly affect the steady-state inactivation of hERG (n=5, P>0.05). The relative block of hERG channels by changrolin was close to zero at the time point of channel opening by the depolarizing voltage step and quickly increased afterwards. The maximal block was achieved in the inactivated state, with no further development of the open channel block. In the "envelope of tails" experiments, the time constants of activation were found to be 287.8+/-46.2 ms and 174.2+/-18.4 ms, respectively, for the absence and presence of 30 mumol/L changrolin (P<0.05, n=7). The onset of inactivation was accelerated significantly by changrolin between -40 mV and +60 mV (P<0.05, n=7).
conclusionThe results demonstrate that changrolin is a potent hERG blocker that preferentially binds to hERG channels in the open and inactivated states.
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