Inhibitory Effect of Lomerizine, a Prophylactic Drug for Migraines, on Serotonin-Induced Contraction of the Basilar Artery
We examined the effects of lomerizine on serotonin (5-hydroxytryptamine, 5-HT)– induced contraction of the basilar artery and compared them with those of nifedipine. Although both lomerizine and nifedipine completely blocked K+-induced vasoconstriction, 5-HT–induced vasoconstriction was more strongl...
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2009-01-01
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| Series: | Journal of Pharmacological Sciences |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1347861319311223 |
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doaj-7cda07b15f9341658513e2961dc14f352020-11-25T02:06:26ZengElsevierJournal of Pharmacological Sciences1347-86132009-01-011112221225Inhibitory Effect of Lomerizine, a Prophylactic Drug for Migraines, on Serotonin-Induced Contraction of the Basilar ArteryMasakazu Ishii0Shunsuke Kobayashi1Masamichi Ohkura2Ryuichi Yamamoto3Shunichi Shimizu4Yuji Kiuchi5Department of Pathophysiology, School of Pharmacy, Showa University, Shinagawa-ku, Tokyo 142-8555, Japan; Corresponding author. masakazu@pharm.showa-u.ac.jpDepartment of Pathophysiology, School of Pharmacy, Showa University, Shinagawa-ku, Tokyo 142-8555, JapanDepartment of Cardiovascular Pharmacology, Yamagata University School of Medicine, Yamagata 990-9585, JapanFirst Department of Pharmacology, School of Pharmacological Sciences, Kyushu University of Health and Welfare, Yoshino, Nobeoka 882-8508, JapanDepartment of Pathophysiology, School of Pharmacy, Showa University, Shinagawa-ku, Tokyo 142-8555, JapanDepartment of Pathophysiology, School of Pharmacy, Showa University, Shinagawa-ku, Tokyo 142-8555, JapanWe examined the effects of lomerizine on serotonin (5-hydroxytryptamine, 5-HT)– induced contraction of the basilar artery and compared them with those of nifedipine. Although both lomerizine and nifedipine completely blocked K+-induced vasoconstriction, 5-HT–induced vasoconstriction was more strongly inhibited by lomerizine than nifedipine. A 5-HT2A antagonist inhibited the 5-HT–induced vasoconstriction, but a 5-HT1B antagonist did not. Lomerizine, but not nifedipine, suppressed 5-HT–induced Ca2+ release in 5-HT2A–expressing HEK293 cells. Moreover, neither antagonist affected ATP-induced Ca2+ release. These results suggest that lomerizine may inhibit not only voltage-dependent Ca2+ channels but also 5-HT2A receptors and so inhibit 5-HT–induced contraction in the basilar artery. Keywords:: lomerizine, serotonin (5-hydroxytryptamine), basilar arteryhttp://www.sciencedirect.com/science/article/pii/S1347861319311223 |
| collection |
DOAJ |
| language |
English |
| format |
Article |
| sources |
DOAJ |
| author |
Masakazu Ishii Shunsuke Kobayashi Masamichi Ohkura Ryuichi Yamamoto Shunichi Shimizu Yuji Kiuchi |
| spellingShingle |
Masakazu Ishii Shunsuke Kobayashi Masamichi Ohkura Ryuichi Yamamoto Shunichi Shimizu Yuji Kiuchi Inhibitory Effect of Lomerizine, a Prophylactic Drug for Migraines, on Serotonin-Induced Contraction of the Basilar Artery Journal of Pharmacological Sciences |
| author_facet |
Masakazu Ishii Shunsuke Kobayashi Masamichi Ohkura Ryuichi Yamamoto Shunichi Shimizu Yuji Kiuchi |
| author_sort |
Masakazu Ishii |
| title |
Inhibitory Effect of Lomerizine, a Prophylactic Drug for Migraines, on Serotonin-Induced Contraction of the Basilar Artery |
| title_short |
Inhibitory Effect of Lomerizine, a Prophylactic Drug for Migraines, on Serotonin-Induced Contraction of the Basilar Artery |
| title_full |
Inhibitory Effect of Lomerizine, a Prophylactic Drug for Migraines, on Serotonin-Induced Contraction of the Basilar Artery |
| title_fullStr |
Inhibitory Effect of Lomerizine, a Prophylactic Drug for Migraines, on Serotonin-Induced Contraction of the Basilar Artery |
| title_full_unstemmed |
Inhibitory Effect of Lomerizine, a Prophylactic Drug for Migraines, on Serotonin-Induced Contraction of the Basilar Artery |
| title_sort |
inhibitory effect of lomerizine, a prophylactic drug for migraines, on serotonin-induced contraction of the basilar artery |
| publisher |
Elsevier |
| series |
Journal of Pharmacological Sciences |
| issn |
1347-8613 |
| publishDate |
2009-01-01 |
| description |
We examined the effects of lomerizine on serotonin (5-hydroxytryptamine, 5-HT)– induced contraction of the basilar artery and compared them with those of nifedipine. Although both lomerizine and nifedipine completely blocked K+-induced vasoconstriction, 5-HT–induced vasoconstriction was more strongly inhibited by lomerizine than nifedipine. A 5-HT2A antagonist inhibited the 5-HT–induced vasoconstriction, but a 5-HT1B antagonist did not. Lomerizine, but not nifedipine, suppressed 5-HT–induced Ca2+ release in 5-HT2A–expressing HEK293 cells. Moreover, neither antagonist affected ATP-induced Ca2+ release. These results suggest that lomerizine may inhibit not only voltage-dependent Ca2+ channels but also 5-HT2A receptors and so inhibit 5-HT–induced contraction in the basilar artery. Keywords:: lomerizine, serotonin (5-hydroxytryptamine), basilar artery |
| url |
http://www.sciencedirect.com/science/article/pii/S1347861319311223 |
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