The Effect of Lamotrigine on Nav1.4 Voltage-Gated Sodium Channels
Lamotrigine (LTG) is an anticonvulsant drug used in the treatment of epilepsy and bipolar disorder and it has been known that LTG targets voltage-dependent sodium channels (VGSCs). In this study, we investigated the effect of LTG on the Nav1.4 Na+ current using HEK293 cells expressing mouse Nav1.4 V...
| Main Authors: | , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2013-01-01
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| Series: | Journal of Pharmacological Sciences |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1347861319302725 |
| _version_ | 1828866276403970048 |
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| author | Yoshihiko Nakatani Haruka Masuko Taku Amano |
| author_facet | Yoshihiko Nakatani Haruka Masuko Taku Amano |
| author_sort | Yoshihiko Nakatani |
| collection | DOAJ |
| description | Lamotrigine (LTG) is an anticonvulsant drug used in the treatment of epilepsy and bipolar disorder and it has been known that LTG targets voltage-dependent sodium channels (VGSCs). In this study, we investigated the effect of LTG on the Nav1.4 Na+ current using HEK293 cells expressing mouse Nav1.4 VGSCs. By the treatment of LTG, Nav1.4 Na+ current was inhibited in a dose-dependent manner. Moreover, 100 μM LTG decreased Nav1.4 Na+ current around 40% and shifted the V1/2 of the inactivation curve to the hyperpolarization side by 20.96 mV. These findings suggest that LTG inhibits Nav1.4 Na+ current and modifies the kinetics of the inactivated state. Keywords:: lamotrigine, Nav1.4, voltage-clamp |
| first_indexed | 2024-12-13T04:47:36Z |
| format | Article |
| id | doaj.art-eb6c65f1480c450cbebc45aed6f79c08 |
| institution | Directory Open Access Journal |
| issn | 1347-8613 |
| language | English |
| last_indexed | 2024-12-13T04:47:36Z |
| publishDate | 2013-01-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Journal of Pharmacological Sciences |
| spelling | doaj.art-eb6c65f1480c450cbebc45aed6f79c082022-12-21T23:59:07ZengElsevierJournal of Pharmacological Sciences1347-86132013-01-011232203206The Effect of Lamotrigine on Nav1.4 Voltage-Gated Sodium ChannelsYoshihiko Nakatani0Haruka Masuko1Taku Amano2Department of Pharmacotherapeutics, School of Pharmacy, International University of Health and Welfare, 2600-1 Kitakanemaru, Ohtawara, Tochigi 324-8501, JapanDepartment of Pharmacotherapeutics, School of Pharmacy, International University of Health and Welfare, 2600-1 Kitakanemaru, Ohtawara, Tochigi 324-8501, JapanDepartment of Pharmacotherapeutics, School of Pharmacy, International University of Health and Welfare, 2600-1 Kitakanemaru, Ohtawara, Tochigi 324-8501, Japan; Corresponding author. amano-t@iuhw.ac.jpLamotrigine (LTG) is an anticonvulsant drug used in the treatment of epilepsy and bipolar disorder and it has been known that LTG targets voltage-dependent sodium channels (VGSCs). In this study, we investigated the effect of LTG on the Nav1.4 Na+ current using HEK293 cells expressing mouse Nav1.4 VGSCs. By the treatment of LTG, Nav1.4 Na+ current was inhibited in a dose-dependent manner. Moreover, 100 μM LTG decreased Nav1.4 Na+ current around 40% and shifted the V1/2 of the inactivation curve to the hyperpolarization side by 20.96 mV. These findings suggest that LTG inhibits Nav1.4 Na+ current and modifies the kinetics of the inactivated state. Keywords:: lamotrigine, Nav1.4, voltage-clamphttp://www.sciencedirect.com/science/article/pii/S1347861319302725 |
| spellingShingle | Yoshihiko Nakatani Haruka Masuko Taku Amano The Effect of Lamotrigine on Nav1.4 Voltage-Gated Sodium Channels Journal of Pharmacological Sciences |
| title | The Effect of Lamotrigine on Nav1.4 Voltage-Gated Sodium Channels |
| title_full | The Effect of Lamotrigine on Nav1.4 Voltage-Gated Sodium Channels |
| title_fullStr | The Effect of Lamotrigine on Nav1.4 Voltage-Gated Sodium Channels |
| title_full_unstemmed | The Effect of Lamotrigine on Nav1.4 Voltage-Gated Sodium Channels |
| title_short | The Effect of Lamotrigine on Nav1.4 Voltage-Gated Sodium Channels |
| title_sort | effect of lamotrigine on nav1 4 voltage gated sodium channels |
| url | http://www.sciencedirect.com/science/article/pii/S1347861319302725 |
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