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Cariprazine inhibits KCNH2. 9 / 9
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"In the present study, the concentration at which cariprazine inhibited hERG 1A currents was 55–75-fold higher than the therapeutic plasma concentration."
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"Cariprazine blocked hERG 1A/3.1 at concentrations much higher than the therapeutic plasma concentration ( IC 50 of 12.2 μM)."
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"Thus, the potential clinical relevance of our findings remains to be confirmed.In conclusion, cariprazine inhibited hERG 1A and hERG 1A/3.1 currents in a concentration-dependent manner."
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"At substantially supratherapeutic concentrations, cariprazine blocked hERG 1A currents by preferentially interacting with the open state of hERG 1A channels."
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"Cariprazine inhibits hERG 1 A and hERG 1 A/3.1 currents in a concentration-dependent manner without affecting the membrane trafficking of these channels [105]."
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"Cariprazine inhibited the amplitude of hERG 1A currents at all membrane potentials between −50 and + 60 mV."
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"Cariprazine inhibited the hERG 1A currents by 16.6 ± 1.6% at the end of the depolarizing pulse to +60 mV, which increased to 36.0 ± 1.2% ( n = 10, P < 0.05) during the repolarization to −40 mV."
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"As shown in Fig. 5 , cariprazine more potently blocked hERG 1A currents during repolarization (in open state) than at the end of depolarization (in inactivated state), which suggests a preferential in[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Therefore, these results indicate that cariprazine blocks hERG 1A currents by preferentially binding to the open states of the channels."
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