Antiepileptic drug tiagabine does not directly target key cardiac ion channels Kv11.1, Nav1.5 and Cav1.2
| العنوان: | Antiepileptic drug tiagabine does not directly target key cardiac ion channels Kv11.1, Nav1.5 and Cav1.2 |
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| المؤلفون: | Łukasz Fijałkowski, Grzegorz Grześk, Jacek Nowaczyk, Magdalena Kowalska, Kinga Sałat, Monika Kubacka, Alicja Nowaczyk |
| المصدر: | Molecules Volume 26 Issue 12 Molecules, Vol 26, Iss 3522, p 3522 (2021) |
| سنة النشر: | 2021 |
| مصطلحات موضوعية: | Male, Tachycardia, ERG1 Potassium Channel, Tiagabine, Action Potentials, Pharmaceutical Science, Pharmacology, Nav1.5, NAV1.5 Voltage-Gated Sodium Channel, Analytical Chemistry, QD241-441, 0302 clinical medicine, Drug Discovery, cardiac voltage-gated ion channels, Medicine, media_common, 0303 health sciences, biology, Chronic pain, Heart, Molecular Docking Simulation, Chemistry (miscellaneous), Molecular Medicine, Anticonvulsants, medicine.symptom, ECG study, medicine.drug, Drug, Calcium Channels, L-Type, media_common.quotation_subject, Article, 03 medical and health sciences, In vivo, Animals, Humans, Repolarization, Computer Simulation, Rats, Wistar, Physical and Theoretical Chemistry, Adverse effect, 030304 developmental biology, Epilepsy, molecular modeling, business.industry, Organic Chemistry, medicine.disease, tiagabine, Rats, biology.protein, business, 030217 neurology & neurosurgery |
| الوصف: | Tiagabine is an antiepileptic drug used for the treatment of partial seizures in humans. Recently, this drug has been found useful in several non-epileptic conditions, including anxiety, chronic pain and sleep disorders. Since tachycardia—an impairment of cardiac rhythm due to cardiac ion channel dysfunction—is one of the most commonly reported non-neurological adverse effects of this drug, in the present paper we have undertaken pharmacological and numerical studies to assess a potential cardiovascular risk associated with the use of tiagabine. A chemical interaction of tiagabine with a model of human voltage-gated ion channels (VGICs) is described using the molecular docking method. The obtained in silico results imply that the adverse effects reported so far in the clinical cardiological of tiagabine could not be directly attributed to its interactions with VGICs. This is also confirmed by the results from the isolated organ studies (i.e., calcium entry blocking properties test) and in vivo (electrocardiogram study) assays of the present research. It was found that tachycardia and other tiagabine-induced cardiac complications are not due to a direct effect of this drug on ventricular depolarization and repolarization. |
| وصف الملف: | application/pdf |
| اللغة: | English |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca268406f0c506e14b10ad28b30d576d https://ruj.uj.edu.pl/xmlui/handle/item/285012 |
| Rights: | OPEN |
| رقم الانضمام: | edsair.doi.dedup.....ca268406f0c506e14b10ad28b30d576d |
| قاعدة البيانات: | OpenAIRE |
| الوصف غير متاح. |