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琥珀酸舒马普坦

琥珀酸舒马普坦用途

Sumatriptan succinate (GR 43175) 是5-HT1受体激动剂,可作用于偏头疼。

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琥珀酸舒马普坦名称

[ CAS 号 ]:
103628-48-4

[ 中文名 ]:
琥珀酸舒马曲普坦

[ 英文名 ]:
Sumatriptan succinate

[中文别名 ]:

[英文别名 ]:

Sumatriptan succinate
MFCD00866222

琥珀酸舒马普坦生物活性

[ 描述 ]:

Sumatriptan succinate (GR 43175) 是5-HT1受体激动剂,可作用于偏头疼。

[ 相关类别 ]:

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

[参考文献]

[1]. Dechant KL, et al. Sumatriptan. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in the acute treatment of migraine and cluster headache.

[2]. Derry CJ, et al. Sumatriptan (oral route of administration) for acute migraine attacks in adults. Cochrane Database Syst Rev. 2012 Feb 15;2:CD008615.

[3]. Depré M, et al. Lack of hemodynamic interaction between CGRP-receptor antagonist telcagepant (MK-0974) and sumatriptan: results from a randomized study in patients with migraine. Cephalalgia. 2013 Dec;33(16):1292-301.

琥珀酸舒马普坦物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
497.7ºC at 760 mmHg

[ 熔点 ]:
165-166°C

[ 分子式 ]:
C₁₈H₂₇N₃O₆S

[ 分子量 ]:
341.426

[ 闪点 ]:
254.8ºC

[ 精确质量 ]:
341.140930

[ PSA ]:
148.18000

[ LogP ]:
0.34

[ 外观性状 ]:
固体;White to Orange to Green powder to crystal

[ 蒸汽压 ]:
1.24E-17mmHg at 25°C

[ 折射率 ]:
1.552

[ 储存条件 ]:
Store at +4°C

[ 水溶解性 ]:
水溶性：可溶；水溶解度：170 g/l 24 °C；极微溶：甲醇；不溶：乙醚,乙醇

琥珀酸舒马普坦MSDS

琥珀酸舒马普坦毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: EJ9940000

CAS REGISTRY NUMBER :: 103628-48-4

LAST UPDATED :: 199606

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C14-H21-N3-O2-S.C4-H6-O4

MOLECULAR WEIGHT :: 413.54

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2939 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Lungs, Thorax, or Respiration - respiratory depression Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 21,2059,1993

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1680 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 21,2059,1993

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 43112 ug/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - respiratory depression Liver - other changes

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 21,2059,1993

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >700 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 21,2065,1993

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >140 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 21,2065,1993 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 5250 mg/kg

SEX/DURATION :: male 10 week(s) pre-mating female 2 week(s) pre-mating - 3 week(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - ovaries, fallopian tubes Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,3817,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2600 mg/kg

SEX/DURATION :: female 18-21 day(s) after conception lactating female 22 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,3849,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 26 gm/kg

SEX/DURATION :: female 18-21 day(s) after conception lactating female 22 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - other postnatal measures or effects

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,3849,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3500 mg/kg

SEX/DURATION :: male 10 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,3817,1994

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琥珀酸舒马普坦安全信息

[ 符号 ]:

GHS05

[ 信号词 ]:
Danger

[ 危害声明 ]:
H318

[ 警示性声明 ]:
P280-P305 + P351 + P338 + P310

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S16-S26-S36-S61-S60

[ 危险品运输编码 ]:
UN 1648 3/PG 2

[ 海关编码 ]:
2935009090

琥珀酸舒马普坦合成路线

琥珀酸舒马普坦上下游产品

琥珀酸舒马普坦上游产品

琥珀酸舒马普坦下游产品

琥珀酸舒马普坦海关

[ 海关编码 ]: 2935009090

[ 中文概述 ]:
2935009090 其他磺（酰）胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:35.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

琥珀酸舒马普坦文献

Multidrug toxicity involving sumatriptan.

J. Anal. Toxicol. 39(1) , 75-9, (2015)

A multidrug fatality involving sumatriptan is reported. Sumatriptan is a tryptamine derivative that acts at 5-HT(1B/1D) receptors and is used for the treatment of migraines. The decedent was a 21-year...

Thermal and 31P-NMR studies to elucidate sumatriptan succinate entrapment behavior in phosphatidylcholine/cholesterol liposomes. Comparative 31P-NMR analysis on negatively and positively-charged liposomes.

Colloids Surf. B Biointerfaces 105 , 14-23, (2013)

In this paper, two techniques, differential scanning calorimetry (DSC) and phosphorus nuclear magnetic resonance ((31)P-NMR), have been used to characterize sumatriptan succinate-loaded charged liposo...

Identification of active ingredients in Wuzhuyu decoction improving migraine in mice by spectral efficiency association.

Mol. Med. Report. 12 , 1524-34, (2015)

Wuzhuyu decoction is a traditional Chinese medicine used for the effective treatment of migraines, termed 'Jueyin headache', in China. However, there have been few investigations to clarify the compos...

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