IndraLab

Statements

Astemizole inhibits KCNH2. 64 / 64
7 17 1 | 33 6
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"This is possibly a hypomorphic mutation that may be rescued by low incubation temperature or a hERG blocker such as astemizole."
19668779
dgi
No evidence text available
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"Astemizole rescued pentamidine and caused hERG trafficking inhibition via competitive interaction with F656 residue [XREF_BIBR]."
27690007
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"As shown in XREF_FIG A, the user will find that astemizole inhibits the activities of the human hERG channel, which was stably expressed on HEK 293 cells, with an IC50 value of 0.0013 muM."
21586548
ctd
No evidence text available
10828461
ctd
No evidence text available
11082114
ctd
No evidence text available
12388285
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"At the end of the light triggered depolarization to -20 mV we observed a clear hyperpolarization before return to the resting membrane potential, which was abolished by the hERG blocker astemizole (30muM)."
29348631
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"In fact, whole-cell voltage-clamp experiments revealed that the IC (50) for astemizole induced hERG blockade is about 300-fold lower than that for the inhibition of high K (+)-induced [3H] NE release."
11705456
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"Desmethylastemizole and astemizole blocked HERG current with similar concentration dependence (half-maximal block of 1.0 and 0.9 nM, respectively) and block was use dependent."
10376921
ctd
No evidence text available
19139152
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"Both terfenadine and astemizole mediated HERG blockade depended significantly on the voltage."
8641472
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"Several other potent hERG channel blockers, such as astemizole and cisapride, were later reported to rescue the trafficking of LQT2 associated hERG channels harboring the G601S mutation."
24747662
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"Fig. 2A shows an original trace : both terfenadine and astemizole blocked HERG channels at submicromolar concentrations."
8641472
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"50 nM astemizole blocked HERG tail currents by 54.5 2.9% (n = 6) and 84.5 1.5% (n = 6), after prior depolar- terfenadine control 200 ms IRK1 control terfenadine -, w,."
8641472
sparser
"In order to verify whether I HERG inhibition by astemizole might correlate with the ability of the second-generation H 1 receptor blocker to prevent high [K + ] e -induced [ 3 H]NE release from SH-S[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
11705456
reach
"On the other hand, terfenadine and astemizole effectively blocked HERG K+ channels with nanomolar affinities (the estimated IC50 values were 330 and 480 nM, respectively), whereas loratadine was approximately 300-fold less potent (IC50 approximately 100 microM)."
9658196
ctd
No evidence text available
10376921
ctd
No evidence text available
11741928
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"HERG blockade by terfenadine and astemizole occurred much faster at higher activation frequencies."
8641472
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"For this purpose, the hERG blocker astemizole (AST), an anti-histamine drug withdrawn from the market because of its cardiotoxic effect (Zhou etal, 1999; Chiu etal, 2004), was added to WT hiPSC-CMs (Fig XREF_FIG)."
27470144
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"We calculated that HERG channels are blocked by astemizole with an IC 50 value of 0.735 +/-0.223 nM and a Hill coefficient of 0.461 +/-0.041 (n = 4)."
10828461
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"Further, the user will also find that astemizole inhibits activities of the human hERG channel transiently expressed in the Xenopus oocyte with an IC50 value of 0.0484 muM (XREF_FIG B)."
21586548
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"In fact, both terfenadine and astemizole have been shown to block HERG K+ channels in a concentration range similar to that found in the plasma of subjects with cardiotoxic manifestations."
10444235
ctd
No evidence text available
15671647
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"Incubation at lower temperature for R752W or with the hERG blocker astemizole for G601S dissociates channel-chaperone complexes and restores trafficking."
12775586
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"Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole."
10376921
sparser
"The fact that the ic 50 for astemizole-induced blockade of I HERG was about 300-fold lower than that calculated for its inhibition of depolarization-induced [ 3 H]NE relea[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
11705456
sparser
"Another crucial point that should be underlined and which favors the hypothesis of SOC inhibition as a primary mechanism for [ 3 H]NE release inhibition by H 1 receptor antagonists is the existence o[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
11705456
tas
No evidence text available
12747773
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"In contrast to the K+ conductances described above, terfenadine (3 pM) and astemizole (1 1tM) almost completely abolished HERG channel tail currents."
8641472
ctd
No evidence text available
10422790
ctd
No evidence text available
11040061
ctd
No evidence text available
16723379
ctd
No evidence text available
9658196
tas
No evidence text available
21185626
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"On the other hand, terfenadine and astemizole blocked HERG channels in a concentration dependent manner with IC 50 of 431 nM and 69 nM, respectively, which are compatible with the recorded plasma leve[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
10422790
sparser
"Astemizole, an anti-histamine, is able to inhibit both Kv10.1 and Kv11.1 channels, contributing to inhibition of cancer cell proliferation in vitro and in vivo [ xref , xref , xref ]."
26010603
ctd
No evidence text available
15272206
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"The results of these studies have elegantly shown that both terfenadine [52] and astemizole [53] blocked HERG K + channels in a concentration range similar to that found in the plasma of subjects with[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
9714291
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"Use- dependent HERG channel blockade by 0.3 wM terfenadine (A) or 0.1 1tM astemizole (B)."
8641472
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"Desmethylastemizole and astemizole cause equipotent block of HERG channels, and these are among the most potent HERG channel antagonists yet studied."
10376921
ctd
No evidence text available
11705456
tas
No evidence text available
24900814
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"In this preparation, terfenadine and astemizole blocked the HERG channels expressed in Xenopus oocytes, whereas epinastine had little effect on that current (Chachin et al., 1998)."
10478629
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"Astemizole, terfenadine and quinidine inhibited hERG currents with IC (50) values of 159nM, 224nM and 2muM, respectively (n = 51, 10 and 18)."
23103595
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"On the other hand terfenadine and astemizole effectively blocked HERG K+ channels with nanomolar affinities (330 and 480 nmol/L, respectively), whereas loratadine was about 300-fold less potent."
11575008
tas
No evidence text available
15324906
ctd
No evidence text available
24052561
ctd
No evidence text available
15740727
sparser
"Thus, the simultaneous inhibition of Kv10.1 and Kv11.1 by astemizole in AML cell types expressing both channels might be advantageous."
35207698
tas
No evidence text available
25133923
sparser
"Here, terfenadine and astemizole both inhibited the human ether-a-go-go related gene (HERG) encoded channels expressed in Xenopus oocytes at nanomolar concentrations in a use- and voltage-dependent fa[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
8641472
ctd
No evidence text available
8641472
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"The data obtained demonstrated that, under depolarizing conditions, the inhibition of hERG K + channels by astemizole was unable to modify SH-SY5Y membrane potential, and therefore that the pharmacolo[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
11705456
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"HERG channel blockers, such as E4031, fexofenadine and astemizole, facilitated maturation of hERG proteins by acting as chemical chaperones XREF_BIBR; however, these agents can not be used clinically for enhancing hERG channel currents, because they acutely block the rapidly activating delayed-rectifier K + channel current (I Kr)."
28607619
tas
No evidence text available
27017549
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"The extreme use dependence of terfenadine and astemizole suggests that drug binding can only occur to the open or inactivated state of HERG channels."
8641472
ctd
No evidence text available
14678746
reach
"This result illustrates the importance of the inactivated state in high-affinity block of HERG by astemizole and terfenadine as well as dofetilide, a drug requiring channel opening for block to occur."
10828461
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"Terfenadine and astemizole suppressed the HERG current with IC50 of 431 nM and 69 nM, respectively."
10422790
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"HERG blockade by terfenadine and astemizole was also analyzed for its voltage dependence."
8641472
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"For astemizole, overall decreased potency was observed at higher temperature, with the greatest degree of block observed with a non-state selective protocol, suggesting that astemizole is able to block multiple states of hERG (Yao et al. 2005)."
35103080
tas
No evidence text available
15911273