Zolmitriptan
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Zolmitriptan 속성
- 녹는점
- 136-141°C
- 알파
- D22 -5.79° (c = 0.5 in methanol)
- 끓는 점
- 563.3±38.0 °C(Predicted)
- 밀도
- 1.217±0.06 g/cm3(Predicted)
- 저장 조건
- 15-25°C
- 용해도
- 5mg/ml의 DMSO에 용해됨
- 산도 계수 (pKa)
- 9.64(at 25℃)
- 물리적 상태
- 가루
- 색상
- 흰색에서 베이지색
- optical activity
- [α]/D -3 to -8°, c = 1 in methanol
- 최대 파장(λmax)
- 225nm(lit.)
- Merck
- 14,10189
- 안정성
- 제공된 대로 구매일로부터 2년 동안 안정적입니다. DMSO 용액은 -20°C에서 최대 3개월 동안 보관할 수 있습니다.
- InChIKey
- ULSDMUVEXKOYBU-ZDUSSCGKSA-N
- CAS 데이터베이스
- 139264-17-8(CAS DataBase Reference)
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
위험품 표기 | Xi,Xn | ||
---|---|---|---|
위험 카페고리 넘버 | 36/37/38-22 | ||
안전지침서 | 26-36 | ||
WGK 독일 | 3 | ||
RTECS 번호 | RQ2707000 | ||
HS 번호 | 29349990 | ||
독성 | women,TDLo,oral,6mg/kg/43W-I (6mg/kg),BEHAVIORAL: HEADACHE,Lancet. Vol. 353, Pg. 378, 1999. |
Zolmitriptan C화학적 특성, 용도, 생산
개요
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.화학적 성질
White Crystalline Powder용도
Zolmitriptan is a serotonin 5HTID-receptor agonist and used to treat migraine (1,2,3).일반 설명
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.Clinical Use
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.참고 문헌
https://www.drugbank.ca/drugs/DB00315Rothner, 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.
Zolmitriptan 준비 용품 및 원자재
원자재
준비 용품
Zolmitriptan 공급 업체
글로벌( 510)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
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Shandong Hengshannuode Pharmaceutical Technology Co., Ltd. | +8615065888978 |
admin@hsnordpharma.com | China | 92 | 58 |
Hebei Yanxi Chemical Co., Ltd. | +86-17531190177; +8617531190177 |
peter@yan-xi.com | China | 5873 | 58 |
Sinoway Industrial co., ltd. | 0592-5800732; +8613806035118 |
xie@china-sinoway.com | China | 990 | 58 |
Henan Bao Enluo International TradeCo.,LTD | +86-17331933971 +86-17331933971 |
deasea125996@gmail.com | China | 2503 | 58 |
Zibo Hangyu Biotechnology Development Co., Ltd | +86-0533-2185556 +8617865335152 |
Mandy@hangyubiotech.com | China | 10977 | 58 |
Hebei Zhuanglai Chemical Trading Co.,Ltd | +8613343047651 |
admin@zlchemi.com | China | 3002 | 58 |
Hebei Shengyang Water Conservancy Engineering Co., Ltd. | +8615373025980 |
clara@hbshengyang.com | China | 873 | 58 |
Nanjing Gold Pharmaceutical Technology Co. Ltd. | 025-84209270 15906146951 |
CHINA | 115 | 55 | |
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21668 | 55 |
Shanghai Time Chemicals CO., Ltd. | +86-021-57951555 +8617317452075 |
jack.li@time-chemicals.com | China | 1807 | 55 |
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