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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Main Authors: Masakazu Ishii (Author), Shunsuke Kobayashi (Author), Masamichi Ohkura (Author), Ryuichi Yamamoto (Author), Shunichi Shimizu (Author), Yuji Kiuchi (Author)
Format: Book
Published: Elsevier, 2009-01-01T00:00:00Z.
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Summary: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
Item Description:1347-8613
10.1254/jphs.09205SC