アルモトリプタン
安全性情報
- リスクと安全性に関する声明
- 危険有害性情報のコード(GHS)
| メーカー |
製品番号 |
製品説明 |
CAS番号 |
包装 |
価格 |
更新時間 |
購入 |
|
富士フイルム和光純薬株式会社(wako)
|
W01MAS091207 |
N,N-Dimethyl-2-(5-((pyrrolidin-1-ylsulfonyl)-methyl)-1H-indol-3-yl)ethanamine |
154323-57-6 |
1g |
￥713000 |
2024-03-01 |
購入 |
|
富士フイルム和光純薬株式会社(wako)
|
W01MAS091207 |
N,N-Dimethyl-2-(5-((pyrrolidin-1-ylsulfonyl)-methyl)-1H-indol-3-yl)ethanamine |
154323-57-6 |
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 |
154323-57-6 |
Y0002140 |
￥19700 |
2024-03-01 |
購入 |
アルモトリプタン 化学特性,用途語,生産方法
効能
抗片頭痛薬, セロトニン受容体作動薬
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-HT
1D/1B agonist with a 35 to
51-fold selectivity versus 5-HT
1A and 5-HT
7 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-HT
1B 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 EC
50 of 0.03 and 0.7 μM) compared to basilar (EC
50
= 3.5 μM) and pulmonary arteries (EC
50＞10μM) or rabbit mesenteric and renal arteries
(EC
50＞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.
使用
Serotonin 5HT1B /1D-receptor agonist
定義
ChEBI: An indole compound having a 2-(dimethylamino)ethyl group at the 3-position and a (pyrrolidin-1-ylsulfonyl)methyl group at the 5-position.
アルモトリプタン 上流と下流の製品情報
原材料
準備製品
アルモトリプタン 生産企業
Global( 108)Suppliers
154323-57-6(アルモトリプタン)キーワード:
- 154323-57-6
- LAS-31416-d6
- ALMOTRIPTAN(SUBJECTTOPATENETFREE)
- Almotriptan
- N,N-Dimethyl-2-[5-(pyrrolidin-1-ylsulfonylmethyl)-1H-indol-3-yl]-ethanamine
- dimethyl-[2-[5-(pyrrolidin-1-ylsulfonylmethyl)-1H-indol-3-yl]ethyl]amine
- AlMotriptan API
- N,N-dimethyl-5-[(1-pyrrolidinylsulfonyl)methyl]-1H-Indole-3-ethanamine
- ALMOTRIPTAN-D6
- 1-[[[2-(Dimethyl-amino)ethyl]-1H-indol-5-yl]methyl]sulfonyl]pyrrolidine
- 1-[[3-(2-dimethylaminoethyl)-5-indolyl]methanesulphonyl]pyrrolidine
- LAS-31416
- 1-[[[2-(Dimethyl-amino)ethyl]-1H-indol-5-yl]methyl]sulfonyl]pyrrolidine-d6
- 1-[[3-(2-dimethylaminoethyl)-5-indolyl]methanesulphonyl]pyrrolidine-d6
- 1H-Indole-3-ethanamine, N,N-dimethyl-5-[(1-pyrrolidinylsulfonyl)methyl]-
- AlmotriptanQ: What is
Almotriptan Q: What is the CAS Number of
Almotriptan Q: What is the storage condition of
Almotriptan Q: What are the applications of
Almotriptan
- アルモトリプタン