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丁苯那嗪

丁苯那嗪用途

Tetrabenazine是VMAT抑制剂,可作用于多动性运动障碍。

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丁苯那嗪名称

[ CAS 号 ]:
58-46-8

[ 中文名 ]:
丁苯那嗪

[ 英文名 ]:
Tetrabenazine

[中文别名 ]:

丁苯喹嗪

[英文别名 ]:

tetrabenazine
Ro 1-9569
Rubigen
Nitoman

丁苯那嗪生物活性

[ 描述 ]:

Tetrabenazine是VMAT抑制剂,可作用于多动性运动障碍。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 单胺转运蛋白

研究领域 >> 神经疾病

[参考文献]

[1]. Jankovic, J. and J. Beach, Long-term effects of tetrabenazine in hyperkinetic movement disorders. Neurology, 1997. 48(2): p. 358-62.

[2]. Kenney, C., C. Hunter, and J. Jankovic, Long-term tolerability of tetrabenazine in the treatment of hyperkinetic movement disorders. Mov Disord, 2007. 22(2): p. 193-7.

[3]. Ondo, W.G., P.A. Hanna, and J. Jankovic, Tetrabenazine treatment for tardive dyskinesia: assessment by randomized videotape protocol. Am J Psychiatry, 1999. 156(8): p. 1279-81.

[相关活性小分子]

利血平 | NBI-98782 | (+)-丁苯那嗪 | 盐酸Radafaxine | 4-羟基-3-甲氧基苯基丙酮酸

丁苯那嗪物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
448.9±45.0 °C at 760 mmHg

[ 熔点 ]:
128-130ºC

[ 分子式 ]:
C₁₉H₂₇NO₃

[ 分子量 ]:
317.423

[ 闪点 ]:
225.3±28.7 °C

[ 精确质量 ]:
317.199097

[ PSA ]:
38.77000

[ LogP ]:
3.48

[ 外观性状 ]:
固体;White to Light yellow powder to crystal

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.554

[ 储存条件 ]:
0-10°C;存放于惰性气体之中;避免空气,加热

丁苯那嗪MSDS

丁苯那嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DK2275000

CHEMICAL NAME :: 2H-Benzo(a)quinolizin-2-one, 1,3,4,6,7,11b-hexahydro-3-isobutyl-9,10-dimethoxy-

CAS REGISTRY NUMBER :: 58-46-8

BEILSTEIN REFERENCE NO. :: 0040090

LAST UPDATED :: 199612

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C19-H27-N-O3

MOLECULAR WEIGHT :: 317.47

WISWESSER LINE NOTATION :: T B666 DV GNTT&J E1Y1&1 LO1 MO1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 550 mg/kg

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

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,308,1972

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 250 mg/kg

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

REFERENCE :: NTIS** National Technical Information Service. (Springfield, VA 22161) Formerly U.S. Clearinghouse for Scientific & Technical Information. Volume(issue)/page/year: AD691-490

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 400 mg/kg

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

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,308,1972

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 150 mg/kg

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

REFERENCE :: PSCBAY Psychopharmacology Service Center, Bulletin. (Bethesda, MD) V.1-3, 1961-65. For publisher information, see PSYBB9. Volume(issue)/page/year: 2,17,1963 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 15 mg/kg

SEX/DURATION :: female 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - other measures of fertility

REFERENCE :: ENDOAO Endocrinology (Baltimore). (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21203) V.1- 1917- Volume(issue)/page/year: 78,225,1966

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丁苯那嗪安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

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

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 危险品运输编码 ]:
UN 3249

[ RTECS号 ]:
DK2275000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2933990090

丁苯那嗪合成路线

丁苯那嗪上下游产品

丁苯那嗪上游产品

丁苯那嗪下游产品

丁苯那嗪海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

丁苯那嗪文献

The VMAT-2 inhibitor tetrabenazine alters effort-related decision making as measured by the T-maze barrier choice task: reversal with the adenosine A2A antagonist MSX-3 and the catecholamine uptake blocker bupropion.

Psychopharmacol. Ser. 232(7) , 1313-23, (2015)

Depressed people show effort-related motivational symptoms, such as anergia, retardation, lassitude, and fatigue. Animal tests can model these motivational symptoms, and the present studies characteri...

Effect of NMDAR antagonists in the tetrabenazine test for antidepressants: comparison with the tail suspension test.

Acta Neuropsychiatr. 27 , 228-34, (2015)

The N-methyl-d-aspartate receptor (NMDAR) antagonist ketamine, produces rapid and enduring antidepressant effect in patients with treatment-resistant depression. Similar dramatic effects have not been...

"Mixed" anionic and non-ionic micellar liquid chromatography for high-speed radiometabolite analysis of positron emission tomography radioligands.

J. Chromatogr. A. 1281 , 54-9, (2013)

A mixed micellar liquid chromatographic (LC) method, the mobile phase consisting of anionic and non-ionic surfactants, has been developed for the high-speed direct radiometabolite analysis of positron...

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