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ゾルミトリプタン

ゾルミトリプタン 化学構造式
139264-17-8
CAS番号.
139264-17-8
化学名:
ゾルミトリプタン
别名:
ゾルミトリプタン;(S)-4-[[3-[2-(ジメチルアミノ)エチル]-1H-インドール-5-イル]メチル]-2-オキサゾリジノン;ゾルミトリプタン (JAN)
英語化学名:
Zolmitriptan
英語别名:
Zomi;Zomig;311c90;bw311c90;Zolmitrptan;zolmitripan;Zolmitriptan;ZOLMITRIPTANE;ZOLIMITRIPTAN;ZolMitriptan API
CBNumber:
CB3313219
化学式:
C16H21N3O2
分子量:
287.35684
MOL File:
139264-17-8.mol

ゾルミトリプタン 物理性質

融点 :
136-141°C
比旋光度 :
D22 -5.79° (c = 0.5 in methanol)
沸点 :
563.3±38.0 °C(Predicted)
比重(密度) :
1.217±0.06 g/cm3(Predicted)
貯蔵温度 :
Refrigerator
溶解性:
Soluble in DMSO at 5mg/ml
酸解離定数(Pka):
9.64(at 25℃)
外見 :
powder
色:
white to beige
光学活性 (optical activity):
[α]/D -3 to -8°, c = 1 in methanol
極大吸収波長 (λmax):
225nm(lit.)
Merck :
14,10189
InChIKey:
ULSDMUVEXKOYBU-ZDUSSCGKSA-N
CAS データベース:
139264-17-8(CAS DataBase Reference)
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)
主な危険性  Xi,Xn
Rフレーズ  36/37/38-22
Sフレーズ  26-36
WGK Germany  3
RTECS 番号 RQ2707000
HSコード  29349990
絵表示(GHS)
注意喚起語 Warning
危険有害性情報
コード 危険有害性情報 危険有害性クラス 区分 注意喚起語 シンボル P コード
H302 飲み込むと有害 急性毒性、経口 4 警告 P264, P270, P301+P312, P330, P501
注意書き
P264 取扱い後は皮膚をよく洗うこと。
P264 取扱い後は手や顔をよく洗うこと。
P270 この製品を使用する時に、飲食または喫煙をしないこ と。
P501 内容物/容器を...に廃棄すること。

ゾルミトリプタン 価格 もっと(14)

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) W01FLC036593
(S)-4-[3-(2-Dimethylamino-ethyl)-1H-indol-5-ylmethyl]-oxazolidin-2-one
139264-17-8 1g ¥41600 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01FLC036593
(S)-4-[3-(2-Dimethylamino-ethyl)-1H-indol-5-ylmethyl]-oxazolidin-2-one
139264-17-8 5g ¥206600 2018-12-26 購入
東京化成工業 Z0024 ゾルミトリプタン >98.0%(HPLC)(T)
Zolmitriptan >98.0%(HPLC)(T)
139264-17-8 200mg ¥5500 2018-12-04 購入
東京化成工業 Z0024 ゾルミトリプタン >98.0%(HPLC)(T)
Zolmitriptan >98.0%(HPLC)(T)
139264-17-8 1g ¥19400 2018-12-04 購入
Sigma-Aldrich Japan SML0248 ≥98% (HPLC)
Zolmitriptan ≥98% (HPLC)
139264-17-8 10mg ¥21800 2018-12-25 購入

ゾルミトリプタン 化学特性,用途語,生産方法

効能

抗片頭痛薬, 血管収縮薬, セロトニン受容体作動薬

商品名

ゾーミッグ (沢井製薬); ゾーミッグ (沢井製薬)

説明

Zolmitriptan is a selective serotonin receptor agonist of the 1B and 1D subtypes. It is mainly used in the acute treatment of migraine attacks with or without aura and cluster headaches. Zolmitriptan takes effect through binding to human 5-HT1Band 5-HT1Dreceptors, leading to cranial blood vessel constriction and the release of sensory neuropeptides through nerve endings in the trigeminal system. 

化学的特性

White Crystalline Powder

Originator

Zeneca (UK)

使用

A Serotonin 5HTID-receptor agonist

使用

adrenergic agonist, nasal decongestant

brand name

Zomig (AstraZeneca); Zomig (IPR).

一般的な説明

Zolmitriptan, the second triptan marketed (approved in1997), has a much better bioavailability (40%–48%) thansumatriptan. It is rapidly absorbed after oral or nasal sprayadministration. It also has an orally disintegrating tablet formulation(Zomig ZMT), which can be taken without water.Zolmitriptan undergoes rapid N-demethylation via CYP1A2to a more potent, active metabolite, N-desmethylzolmitriptan,which is 2 to 6 times more potent than the parentdrug. This active metabolite was detected 5 minutesafter dosing and accounts for about two thirds of the plasmaconcentration of the administered dose of the parent drug.284Thus, it is reasonable to assume that the therapeutic effectsand especially the CNS side effects of zolmitriptan must bein part attributed to the plasma levels of this active metabolite,at least until it is further degraded by hepatic MAO-Ato its inactive indole acetic acid derivatives.

臨床応用

Zomig was launched in Germany, Denmark, Sweden and the UK for use as an antimigraine agent (with and without aura). It can be prepared by three related routes of 5 to 7 steps starting from L-4-nitrophenylalanine. Zomig is a 5-HT1D/1B receptor agonist (10 fold ratio) with modest (< 100x) affinity for 5-HT1A and 5-HT1F receptors. It has no affinity for other serotonin receptors or receptors of other neurotransmitters. It has a novel dual action mechanism: centrally it acts on the trigeminal nucleus caudalis and peripherally is acts on the trigeminovascular system. Zomig was effective in treating headaches and nonheadache (photophobia, phonophobia and nausea) symptoms. It was 2-3 times more potent than sumatriptan and is metabolized to three compounds, one of which is 2-8 times more active than the parent. It caused a 40-50% decrease in headache after 1 h and a 73-77% after 4 h. There was a 30% reoccurance of headache but 90% effective treatment with a second dose. It blocks neurogenic inflammation by inhibiting release of peptides, causes vasoconstriction, and inhibits neuronal depolarization at peripheral sites in the cranium. It is 40% bioavailable and a 10 time theraputic dose showed no safety concerns.

参考文献

https://www.drugbank.ca/drugs/DB00315
Rothner, A. D., et al. "Zolmitriptan oral tablet in migraine treatment: high placebo responses in adolescents." Headache the Journal of Head & Face Pain 46.1(2006):101.
Hedlund, C, et al. "Zolmitriptan nasal spray in the acute treatment of cluster headache: a meta-analysis of two studies. " Neurology49.9(2009):1315–1323.

ゾルミトリプタン 上流と下流の製品情報

原材料

準備製品


ゾルミトリプタン 生産企業

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139264-17-8(ゾルミトリプタン)キーワード:


  • 139264-17-8
  • (s)-2-oxazolidinon
  • (s)-4-((3-(2-(dimethylamino)ethyl)-1h-indol-5-yl)methyl)-2-oxazolidinone
  • 311c90
  • bw311c90
  • Zolmitrptan
  • (4S)-4-[[3-[2-(Dimethylamino)ethyl]-1H-indol-5-yl]methyl-2-oxazolidinone
  • ZOLMITRIPTANE
  • (4r)-4-[[3-(2-dimethylaminoethyl)-1h-indol-5-yl]methyl]oxazolidin-2-one
  • Zomi
  • (S)-4-[3-(2-DIMETHYLAMINO-ETHYL)-1H-INDOL-5-YLMETHYL]-OXAZOLIDIN-2-ONE
  • (S)-4-(4-hydrazinobenzyl)-2-oxazolidinone(S)-4-(4-aminobenzyl)-2-oxazolidinone4-(2-Dimethylamino) butyaldehyde diethyl acetal
  • Zomig
  • (S)-4-[3-(2-Dimethylamino-ethyl)-1H-indol-5-
  • zolmitripan
  • Zolmitriptan
  • Assists Mi Qu Pu Tanzania
  • Zolmitriptan (150 mg)
  • (4R)-4-({3-[2-(diMethylaMino)ethyl]-1H-indol-5-yl}Methyl)-1,3-oxazolidin-2-one
  • ZolMitriptan(ZoMig)
  • ZolMitriptan API
  • ZOLIMITRIPTAN
  • (R)-4-((3-(2-(diMethylaMino)ethyl)-1H-indol-5-yl)Methyl)oxazolidin-2-one
  • Zolmitriptan (4R)-4-[[3-(2-Dimethylaminoethyl)-1H-indol-5-yl]methyl]oxazolidin-2-one
  • (S)-4-((3-(2-(Dimethylamino)ethyl)indol-5-yl)methyl)-2-oxazolidinone
  • Zolmitriptan, 98%, a selective 5-HT1B/1D/1F receptor agonist
  • ゾルミトリプタン
  • (S)-4-[[3-[2-(ジメチルアミノ)エチル]-1H-インドール-5-イル]メチル]-2-オキサゾリジノン
  • ゾルミトリプタン (JAN)
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