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屈西多巴

屈西多巴用途

【用途1】
用于Shy-Drager氏完全症、家庭性淀粉样多神经病引起的起立性低血压、失神和头晕、帕金森氏症引起的足竦缩、起立性头晕。

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屈西多巴名称

[ CAS 号 ]:
23651-95-8

[ 中文名 ]:
屈昔多巴

[ 英文名 ]:
droxidopa

[中文别名 ]:

屈西多巴

[英文别名 ]:

DL-DOPS
DL-threo-Dihydroxyphenylserine
L-DOPS
3-dihydroxy-betthreo-dl-tyrosin
3-dihydroxy-dl-tyrosinethreo-bet
DROXIDOPA
L-threo-DOPS
DL-THREO-DOPS
L-threo-3,4-Dihydroxyphenylserine
Droxidopa L-threo 3,4-Dihydroxyphenylserine

屈西多巴生物活性

[ 描述 ]:

Droxidopa(L-DOPS, SM5688)是合成的氨基酸前体,可作为神经递质去甲肾上腺素和肾上腺素的原药,能透过血脑屏障。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

天然产物 >> 苯丙酸类

研究领域 >> 神经疾病

[参考文献]

[1]. Coll M, et al. Droxidopa, an oral norepinephrine precursor, improves hemodynamic and renal alterations of portal hypertensive rats. Hepatology. 2012 Nov;56(5):1849-60.

[2]. Mathias CJ. L-dihydroxyphenylserine (Droxidopa) in the treatment of orthostatic hypotension: the European experience. Clin Auton Res. 2008 Mar;18 Suppl 1:25-9.

[相关活性小分子]

屈西多巴物理化学性质

[ 密度 ]:
1.608g/cm3

[ 沸点 ]:
549.8±50.0 °C at 760 mmHg

[ 熔点 ]:
232-235° (dec); mp 229-232° (dec) (Ohashi)

[ 分子式 ]:
C₉H₁₁NO₅

[ 分子量 ]:
213.187

[ 闪点 ]:
286.3±30.1 °C

[ 精确质量 ]:
213.063721

[ PSA ]:
124.01000

[ LogP ]:
-0.95

[ 蒸汽压 ]:
0.0±1.6 mmHg at 25°C

[ 折射率 ]:
1.692

[ 储存条件 ]:
2-8C

屈西多巴MSDS

详细MSDS(安全技术说明书)

屈西多巴毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VT9626010

CHEMICAL NAME :: Serine, 3-(3,4-dihydroxyphenyl)-, L-threo-

CAS REGISTRY NUMBER :: 23651-95-8

LAST UPDATED :: 199603

DATA ITEMS CITED :: 12

MOLECULAR FORMULA :: C9-H11-N-O5

MOLECULAR WEIGHT :: 213.21

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 :: >10 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,758,1990

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 84 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,758,1990

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 16 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Lungs, Thorax, or Respiration - 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: 15(Suppl 2),257,1987

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >10 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,758,1990

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >10 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,758,1990

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >100 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,758,1990

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Cardiac - other changes Lungs, Thorax, or Respiration - dyspnea Kidney, Ureter, Bladder - other changes

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 40,1935,1989

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Cardiac - other changes Lungs, Thorax, or Respiration - respiratory depression Kidney, Ureter, Bladder - other changes

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 40,1935,1989 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 13200 mg/kg

SEX/DURATION :: female 15 day(s) pre-mating female 1-7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - ovaries, fallopian tubes

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: 15(Suppl 2),283,1987

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2200 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

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: 15(Suppl 2),283,1987

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1500 mg/kg

SEX/DURATION :: female 17-21 day(s) after conception lactating female 20 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - physical 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: 15(Suppl 2),283,1987

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 15 gm/kg

SEX/DURATION :: female 17-21 day(s) after conception lactating female 20 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Maternal Effects - parturition

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: 15(Suppl 2),283,1987

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屈西多巴安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
36/37/38

[ 安全声明 (欧洲) ]:
26

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
VT9626010

[ 海关编码 ]:
29225090

屈西多巴制备

【方法1】
DL-型的化合物(I)和手性试剂作用，再用3%盐酸处理，得L-型的(I)。然后氢解得屈昔多巴。

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屈西多巴文献

Application of the BCS biowaiver approach to assessing bioequivalence of orally disintegrating tablets with immediate release formulations.

Eur. J. Pharm. Sci. 64 , 37-43, (2014)

The aim of this study was to compare the dissolution profiles of oral disintegrating tablets (ODTs) and immediate release (IR) formulations in order to experimentally validate the regulatory biowaiver...

[Acute poisoning of droxidopa: report of a case].

Chudoku. Kenkyu. 26(3) , 244-5, (2013)

The noradrenaline precursor L-DOPS reduces pathology in a mouse model of Alzheimer's disease.

Neurobiol. Aging 33(8) , 1651-63, (2012)

Damage to noradrenergic neurons in the locus coeruleus (LC) is a hallmark of Alzheimer's disease (AD) and may contribute to disease progression. In 5xFAD transgenic mice, which accumulate amyloid burd...

更多文献

屈西多巴

屈西多巴用途

屈西多巴名称

屈西多巴生物活性

屈西多巴物理化学性质

屈西多巴MSDS

详细MSDS(安全技术说明书)

屈西多巴毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

屈西多巴安全信息

屈西多巴制备

屈西多巴文献

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