ArticleBritish journal of pharmacology2002
The antihistamine fexofenadine does not affect I(Kr) currents in a case report of drug-induced cardiac arrhythmia.
Article in British journal of pharmacology, 2002. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers, 1 of them a synthesis that pooled it.
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Who cites it
16 citing papers in PubMed, 1 synthesis or guideline pooled it, 56 citations in OpenAlex.
- Pharmacogenomic markers associated with drug-induced QT prolongation: a systematic review.PharmacogenomicsPooled it
- Metabolic-Hydroxy and Carboxy Functionalization of Alkyl Moieties in Drug Molecules: Prediction of Structure Influence and Pharmacologic Activity.Molecules (Basel, Switzerland) · 2020Review
- Second-Generation Histamine H1 Receptor Antagonists Suppress Delayed Rectifier KBioMed research international · 2019Article
- Comparative Study of Chemical Stability of Two HJournal of analytical methods in chemistry · 2019Article
- Modulation of Ether-à-Go-Go Related Gene (ERG) Current Governs Intrinsic Persistent Activity in Rodent Neocortical Pyramidal Cells.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2018Article
- Functional Coupling of Human Microphysiology Systems: Intestine, Liver, Kidney Proximal Tubule, Blood-Brain Barrier and Skeletal Muscle.Scientific reports · 2017Article
- Pro-arrhythmic potential of oral antihistamines (H1): combining adverse event reports with drug utilization data across Europe.PloS one · 2015Article
- Allocryptopine and benzyltetrahydropalmatine block hERG potassium channels expressed in HEK293 cells.Acta pharmacologica Sinica · 2013Article
- Modification of K+ channel-drug interactions by ancillary subunits.The Journal of physiology · 2008Review
- Blockade of HERG human K+ channels and IKr of guinea-pig cardiomyocytes by the antipsychotic drug clozapine.British journal of pharmacology · 2006Article
- Comparison of HERG channel blocking effects of various beta-blockers-- implication for clinical strategy.British journal of pharmacology · 2006Article
- Functional significance of KCNH2 (HERG) K897T polymorphism for cardiac repolarization assessed by analysis of T-wave morphology.Annals of noninvasive electrocardiology : the official journal of the International Society for Holter and Noninvasive Electrocardiology, Inc · 2006Article
- Blockade of HERG cardiac K+ current by antifungal drug miconazole.British journal of pharmacology · 2005Article
- Second-generation antihistamines: actions and efficacy in the management of allergic disorders.Drugs · 2005Review
- Inhibition of cloned HERG potassium channels by the antiestrogen tamoxifen.Naunyn-Schmiedeberg's archives of pharmacology · 2003Article
- KCNE2 and the K (+) channel: the tail wagging the dog.Channels (Austin, Tex.)Review
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. The human HERG gene encodes the cardiac repolarizing K(+) current I(Kr) and is genetically inactivated in inherited long QT syndrome 2 (LQTS2). The antihistamine terfenadine blocks HERG channels, and can cause QT prolongation and torsades de pointes, whereas its carboxylate fexofenadine lacks HERG blocking activity. 2. In the present study the ability of fexofenadine to block the K897T HERG channel variant was investigated. The underlying single nucleotide polymorphism (SNP) A2960C was identified in a patient reported to develop fexofenadine-associated LQTS. 3. K897T HERG channels produced wild-type-like currents in Xenopus oocytes. Even at a concentration of 100 micro M, fexofenadine did not inhibit wild-type or K897T HERG channels. Coexpression of wild-type and K897T HERG with the ss-subunit MiRP1, slightly changed current kinetics but did not change sensitivity to terfenadine and fexofenadine. 4. Western blot analysis and immunostaining of transiently transfected COS-7 cells demonstrated that overall expression level, glycosylation pattern and subcellular localization of K897T HERG is indistinguishable from wild-type HERG protein, and not altered in the presence of 1 micro M fexofenadine. 5. We provide the first functional characterization of the K897T HERG variant. We demonstrated that K897T HERG is similar to wild-type HERG, and is insensitive to fexofenadine. Although the polymorphism changes PKA and PKC phosphorylation sites, regulation of K897T HERG by these kinases is not altered. 6. Our results strongly indicate that QT lengthening and cardiac arrhythmia in the reported case of drug-induced LQT are not due to the K897T exchange or to an inhibitory effect of fexofenadine on cardiac I(Kr) currents. British Journal of
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