دورية أكاديمية
Lidocaine increases the number of beta-adrenoceptors in neonatal rat cardiocytes in culture.
| العنوان: | Lidocaine increases the number of beta-adrenoceptors in neonatal rat cardiocytes in culture. |
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| المؤلفون: | Mizuki T; Second Department of Medicine University of Occupational and Environmental Health, School of Medicine, Kitakyushu, Japan., Kobayashi H, Nakashima Y, Kuroiwa A, Izumi F |
| المصدر: | Naunyn-Schmiedeberg's archives of pharmacology [Naunyn Schmiedebergs Arch Pharmacol] 1994 Feb; Vol. 349 (2), pp. 170-4. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Springer Verlag Country of Publication: Germany NLM ID: 0326264 Publication Model: Print Cited Medium: Print ISSN: 0028-1298 (Print) Linking ISSN: 00281298 NLM ISO Abbreviation: Naunyn Schmiedebergs Arch Pharmacol Subsets: MEDLINE |
| أسماء مطبوعة: | Original Publication: Berlin, New York, Springer Verlag. |
| مواضيع طبية MeSH: | Animals, Newborn/*metabolism , Lidocaine/*pharmacology , Myocardium/*metabolism , Receptors, Adrenergic, beta/*metabolism, Adenylyl Cyclases/metabolism ; Animals ; Anti-Arrhythmia Agents/pharmacology ; Cell Membrane/drug effects ; Cell Membrane/enzymology ; Cell Membrane/metabolism ; Cells, Cultured ; Female ; Heart/drug effects ; Iodocyanopindolol ; Male ; Myocardium/enzymology ; Pindolol/analogs & derivatives ; Pindolol/pharmacokinetics ; Rats ; Rats, Wistar ; Receptors, Adrenergic, beta/drug effects ; Up-Regulation/drug effects |
| مستخلص: | Some physiological functions of the heart are modulated through cardiac beta-adrenoceptors. In acute myocardial infarction, ventricular arrhythmias occur frequently and class I antiarrhythmic drugs such as lidocaine are often administered continuously over long period. The aim of this study was to investigate the effects of long-term treatment with lidocaine on cardiac beta-adrenoceptors. Ventricular cardiocytes from 2-day-old Wistar rat were cultured in the presence or absence of lidocaine, and beta-adrenoceptors of the membrane fraction of the cells were measured with a binding assay using [125I]-iodocyanopindolol ([125I]CYP) as a radioligand. When the cells were cultured in the presence of lidocaine at clinical or toxic concentrations, the binding of [125I]CYP to the cells increased in a concentration (10(-5) mol/l-10(-3) mol/l)--and time (12-72 h)--dependent manner. The effect was due to an increase in maximum binding and was not due to a change in the dissociation constant for the ligand. The stimulation of adenylyl cyclase activity in the cell membrane by 1 mumol/l isoproterenol increased in lidocaine-treated cells. The increased number of receptors returned to the control level when the cells were cultured without lidocaine for a further 24 h. These results indicate that lidocaine up-regulates cardiac beta-adrenoceptors at both clinical or toxic doses during the period of treatment. Other antiarrhythmic drugs such as disopyramide (Ia), mexiletine (Ib) and flecainide (Ic) also increased the number of beta-receptors.(ABSTRACT TRUNCATED AT 250 WORDS) |
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| المشرفين على المادة: | 0 (Anti-Arrhythmia Agents) 0 (Receptors, Adrenergic, beta) 83498-72-0 (Iodocyanopindolol) 98PI200987 (Lidocaine) BJ4HF6IU1D (Pindolol) EC 4.6.1.1 (Adenylyl Cyclases) |
| تواريخ الأحداث: | Date Created: 19940201 Date Completed: 19940527 Latest Revision: 20190725 |
| رمز التحديث: | 20231215 |
| DOI: | 10.1007/BF00169833 |
| PMID: | 8170500 |
| قاعدة البيانات: | MEDLINE |
Find this article in full text from Springer Verlag. 
Full Text Finder | تدمد: | 0028-1298 |
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| DOI: | 10.1007/BF00169833 |