アルモトリプタン
- ¥19700 - ¥713000
- 化學(xué)名: アルモトリプタン
- 英語名: Almotriptan
- 別名:アルモトリプタン
- CAS番號: 154323-57-6
- 分子式: C17H25N3O2S
- 分子量: 335.46
- EINECS:1312995-182-4
- MDL Number:MFCD00927104
3物価
選択條件:
ブランド
- 富士フイルム和光純薬株式會社(wako)
- Sigma-Aldrich Japan
パッケージ
- Y0002140
- 250mg
- 1g
- 生産者富士フイルム和光純薬株式會社(wako)
- 製品番號W01MAS091207
- 製品説明
- 英語製品説明N,N-Dimethyl-2-(5-((pyrrolidin-1-ylsulfonyl)-methyl)-1H-indol-3-yl)ethanamine
- 包裝単位1g
- 価格¥713000
- 更新しました2024-03-01
- 購入
- 生産者富士フイルム和光純薬株式會社(wako)
- 製品番號W01MAS091207
- 製品説明
- 英語製品説明N,N-Dimethyl-2-(5-((pyrrolidin-1-ylsulfonyl)-methyl)-1H-indol-3-yl)ethanamine
- 包裝単位250mg
- 価格¥79100
- 更新しました2023-06-01
- 購入
- 生産者Sigma-Aldrich Japan
- 製品番號Y0002140
- 製品説明システム適合性用アルモトリプタン CRS, European Pharmacopoeia (EP) Reference Standard
- 英語製品説明 CRS, European Pharmacopoeia (EP) Reference Standard
- 包裝単位Y0002140
- 価格¥19700
- 更新しました2024-03-01
- 購入
生産者 | 製品番號 | 製品説明 | 包裝単位 | 価格 | 更新時(shí)間 | 購入 |
---|---|---|---|---|---|---|
富士フイルム和光純薬株式會社(wako) | W01MAS091207 | N,N-Dimethyl-2-(5-((pyrrolidin-1-ylsulfonyl)-methyl)-1H-indol-3-yl)ethanamine |
1g | ¥713000 | 2024-03-01 | 購入 |
富士フイルム和光純薬株式會社(wako) | W01MAS091207 | N,N-Dimethyl-2-(5-((pyrrolidin-1-ylsulfonyl)-methyl)-1H-indol-3-yl)ethanamine |
250mg | ¥79100 | 2023-06-01 | 購入 |
Sigma-Aldrich Japan | Y0002140 | システム適合性用アルモトリプタン CRS, European Pharmacopoeia (EP) Reference Standard CRS, European Pharmacopoeia (EP) Reference Standard |
Y0002140 | ¥19700 | 2024-03-01 | 購入 |
プロパティ
沸點(diǎn) :538.7±60.0 °C(Predicted)
比重(密度) :1.27±0.1 g/cm3(Predicted)
酸解離定數(shù)(Pka) :16.92±0.30(Predicted)
外見 :Solid
色 :White to off-white
CAS データベース :154323-57-6(CAS DataBase Reference)
比重(密度) :1.27±0.1 g/cm3(Predicted)
酸解離定數(shù)(Pka) :16.92±0.30(Predicted)
外見 :Solid
色 :White to off-white
CAS データベース :154323-57-6(CAS DataBase Reference)
安全情報(bào)
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注意喚起語: | Warning | ||||||||||||||||||||||||||||||||||||||||||||||||
危険有害性情報(bào): |
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注意書き: |
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説明
Almotriptan was first marketed in Spain as a new medicine against acute attacks of migraine. It is the fifth agent belonging to the “triptan” class to be launched after sumatriptan, naratriptan, zolmitriptan and rizatriptan. This close structural analog of sumatriptan can be prepared in six steps from 4-nitrobenzylsulfonyl chloride with a Fischer indole synthesis as the key step. Almotriptan acts as a dual 5-HT1D/1B agonist with a 35 to 51-fold selectivity versus 5-HT1A and 5-HT7 receptors respectively as well as having insignificant affinity for the most relevant nonserotonergic receptors (K1>1μM). Its agonistic effect on 5-HT,n receptors of trigeminal sensory neurons turns off neurogenic inflammation by inhibiting the release of neuropeptides such as calcitonin gene-related peptide, neurokinin A and substance P. Concomitantly, its action on the 5-HT1B receptors in meningeal arteries relieves the vasodilatation of these vessels associated with migraine attacks. Almotriptan causes selective concentration-dependent vasoconstriction of human meningeal and temporal arteries (with EC50 of 0.03 and 0.7 μM) compared to basilar (EC50 = 3.5 μM) and pulmonary arteries (EC50>10μM) or rabbit mesenteric and renal arteries (EC50>100 μM). Although it is predominantly cleared by the kidneys as unchanged drug (45%) or transformed into inactive metabolites by monoamine oxidase A (MAO-A) and CYP3A4 enzymes in the liver, almotriptan has the highest oral bioavailability (70%) of the triptans and has a half-life of 3.5 h. The therapeutic dose of 12.5 mg is well tolerated, shows a rapid onset of action (30 min) and low recurrence rate compared to sumatriptan.関連商品価格
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