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甲磺酸多拉司琼

甲磺酸多拉司琼用途

Dolasetron(MDL-73147)甲磺酸盐是5-HT3受体拮抗剂,用于只治疗化疗引起的恶心和呕吐症状。

甲磺酸多拉司琼名称

[ CAS 号 ]:
115956-13-3

[ 中文名 ]:
甲磺酸多拉司琼

[ 英文名 ]:
Dolasetron (Mesylate)

[中文别名 ]:

多拉司琼甲磺酸盐

[英文别名 ]:

MFCD01718979
Dolasetron mesylate
EINECS 214-599-3
Dolasetron (Mesylate)

甲磺酸多拉司琼生物活性

[ 描述 ]:

Dolasetron(MDL-73147)甲磺酸盐是5-HT3受体拮抗剂,用于只治疗化疗引起的恶心和呕吐症状。

[ 相关类别 ]:

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

研究领域 >> 其他

[参考文献]

[1]. Faria C, et al. Outcomes Associated with 5-HT3-RA Therapy Selection in Patients with Chemotherapy-Induced Nausea and Vomiting: A Retrospective Claims Analysis. Am Health Drug Benefits. 2014 Jan;7(1):50-8.

[相关活性小分子]

甲磺酸多拉司琼物理化学性质

[ 沸点 ]:
535.1ºC at 760 mmHg

[ 分子式 ]:
C₂₀H₂₄N₂O₆S

[ 分子量 ]:
420.48

[ 闪点 ]:
277.4ºC

[ PSA ]:
134.38000

[ LogP ]:
2.97740

[ 外观性状 ]:
白色粉末

[ 蒸汽压 ]:
1.65E-22mmHg at 25°C

[ 储存条件 ]:
2-8°C

甲磺酸多拉司琼毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: NL6015300

CHEMICAL NAME :: 1H-Indole-3-carboxylic acid, octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl ester, (2-alpha,6-alpha,8-alpha,9a-beta)-, monomethanesulfonate, monohydrate

CAS REGISTRY NUMBER :: 115956-13-3

LAST UPDATED :: 199801

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C19-H20-N2-O3.C-H4-O3-S.H2-O

MOLECULAR WEIGHT :: 438.54

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 2400 ug/kg

TOXIC EFFECTS :: Behavioral - headache Gastrointestinal - decreased motility or constipation Gastrointestinal - other changes

REFERENCE :: BDDID8 Biopharmaceutics & Drug Disposition. (John Wiley & Sons, Baffins Lane, Chichester, W. Sussex PO19 1UD, UK) V.1- 1979- Volume(issue)/page/year: 18,361,1997

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 2400 ug/kg/10M-C

TOXIC EFFECTS :: Behavioral - hallucinations, distorted perceptions Behavioral - headache

REFERENCE :: BDDID8 Biopharmaceutics & Drug Disposition. (John Wiley & Sons, Baffins Lane, Chichester, W. Sussex PO19 1UD, UK) V.1- 1979- Volume(issue)/page/year: 18,361,1997

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 545 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 18,506,1993

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 165 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 18,506,1993

甲磺酸多拉司琼安全信息

[ 风险声明 (欧洲) ]:
R20/21/22