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Eletriptan

依來曲普坦
Mechanism of action:
Eletriptan 是一種血清素 5-HT₁B/5-HT₁D 受體促效劑(serotonin receptor agonist),屬於翠普登類(triptan)。Eletriptan 的作用集中於顱內三叉神經與週遭血管系統(trigeminovascular system),刺激顱內(特別是硬腦膜)血管平滑肌上的 5-HT₁B 受體,使顱內血管張力上調並引發血管收縮反應;在三叉神經末梢刺激 5-HT₁D 受體,減少抑鈣基因相關胜肽(calcitonin gene-related peptide)、P 物質(substance P)等促發炎與致痛神經胜肽的釋放,減少神經性發炎與疼痛傳導。
Reference(s):
1. Napier C et al. (1999). Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [³H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. Eur J Pharmacol.
2. van den Broek RW et al. (2000). Pharmacological analysis of contractile effects of eletriptan and sumatriptan on human isolated blood vessels. Eur J Pharmacol.
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