Effects of cariprazine on hERG 1A and hERG 1A/3.1 potassium channels
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چکیده
منابع مشابه
Voltage-Dependent Gating of hERG Potassium Channels
The mechanisms by which voltage-gated channels sense changes in membrane voltage and energetically couple this with opening of the ion conducting pore has been the source of significant interest. In voltage-gated potassium (Kv) channels, much of our knowledge in this area comes from Shaker-type channels, for which voltage-dependent gating is quite rapid. In these channels, activation and deacti...
متن کاملAntiarrhythmic drug carvedilol inhibits HERG potassium channels.
OBJECTIVE The aryloxypropanolamine carvedilol is a multiple action cardiovascular drug with blocking effects on alpha-receptors, beta-receptors, Ca(2+)-channels, Na(+)-channels and various native cardiac K(+) channels, thereby prolonging the cardiac action potential. In a number of clinical trials with patients suffering from congestive heart failure, carvedilol appeared to be superior to other...
متن کاملCardiac IKr channels minimally comprise hERG 1a and 1b subunits.
Previous studies suggest native cardiac IKr channels are composed of alpha subunits encoded solely by the 1a transcript of the ERG1 gene. Using isoform-specific ERG1 antibodies, we have new evidence that subunits encoded by an alternate transcript, ERG1b, are also expressed in rat, canine, and human heart. The ERG1a and -1b subunits associate in vivo where they localize to the T tubules of vent...
متن کاملNa+ Permeation and Block of hERG Potassium Channels
The inactivation gating of hERG channels is important for the channel function and drug-channel interaction. Whereas hERG channels are highly selective for K+, we have found that inactivated hERG channels allow Na+ to permeate in the absence of K+. This provides a new way to directly monitor and investigate hERG inactivation. By using whole cell patch clamp method with an internal solution cont...
متن کاملInhibition of hERG Potassium Channels by Celecoxib and Its Mechanism
BACKGROUND Celecoxib (Celebrex), a widely prescribed selective inhibitor of cyclooxygenase-2, can modulate ion channels independently of cyclooxygenase inhibition. Clinically relevant concentrations of celecoxib can affect ionic currents and alter functioning of neurons and myocytes. In particular, inhibition of Kv2.1 channels by celecoxib leads to arrhythmic beating of Drosophila heart and of ...
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ژورنال
عنوان ژورنال: European Journal of Pharmacology
سال: 2019
ISSN: 0014-2999
DOI: 10.1016/j.ejphar.2019.04.006