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泰必利

泰必利用途

硫必利是一种非典型抗精神病药,是一种选择性多巴胺D2受体拮抗剂,几乎不易引起催化反应和镇静。对于D1,硫必利的IC50值分别为1440、45.8、>100和11.7μM；D2；D3；D4,分别为[1]。

泰必利名称

[ CAS 号 ]:
51012-32-9

[ 中文名 ]:
硫必利

[ 英文名 ]:
Tiapride

[中文别名 ]:

[英文别名 ]:

EINECS 256-907-9
MFCD00242730

泰必利生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 多巴胺受体

信号通路 >> 神经信号通路 >> 多巴胺受体

研究领域 >> 神经疾病

[ 靶点 ]

D2 Receptor:110-320 nM (IC50)

D3 Receptor:180 nM (IC50)

[参考文献]

[1]. D H Peters, et al. Tiapride. A review of its pharmacology and therapeutic potential in the management of alcohol dependence syndrome. Drugs. 1994 Jun;47(6):1010-32.

[2]. T Arima, et al. Comparison of effects of tiapride and sulpiride on D-1, D-2, D-3 and D-4 subtypes of dopamine receptors in rat striatal and bovine caudate nucleus membranes. Jpn J Pharmacol. 1986 Jul;41(3):419-23.

泰必利物理化学性质

[ 密度 ]:
1.15 g/cm3

[ 沸点 ]:
498.1ºC at 760 mmHg

[ 熔点 ]:
120ºC

[ 分子式 ]:
C₁₅H₂₄N₂O₄S

[ 分子量 ]:
328.42700

[ 闪点 ]:
255.1ºC

[ 精确质量 ]:
328.14600

[ PSA ]:
87.58000

[ LogP ]:
2.82590

[ 储存条件 ]:
2-8°C

泰必利毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CV4203700

CHEMICAL NAME :: Benzamide, N-(2-(diethylamino)ethyl)-2-methoxy-5-(methylsulfonyl )-

CAS REGISTRY NUMBER :: 51012-32-9

LAST UPDATED :: 199612

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C15-H24-N2-O4-S

MOLECULAR WEIGHT :: 328.47

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 1197 mg/kg

SEX/DURATION :: female 38 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina

REFERENCE :: THERAP Therapie. (Doin, Editeurs, 8, Place de l'Odeon, F-75006 Paris, France) V.1- 1946- Volume(issue)/page/year: 30,231,1975

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 850 mg/kg

SEX/DURATION :: female 27 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - menstrual cycle changes or disorders

REFERENCE :: THERAP Therapie. (Doin, Editeurs, 8, Place de l'Odeon, F-75006 Paris, France) V.1- 1946- Volume(issue)/page/year: 30,231,1975

泰必利安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

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

[ WGK德国 ]:
2

[ RTECS号 ]:
CV4203800

[ 海关编码 ]:
2924299090

泰必利海关

[ 海关编码 ]: 2924299090

[ 中文概述 ]:
2924299090. 其他环酰胺（包括环氨基甲酸酯）（包括其衍生物以及他们的盐）. 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:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 包装

[ Summary ]:
2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

泰必利文献

Serotonergic signalling suppresses ataxin 3 aggregation and neurotoxicity in animal models of Machado-Joseph disease.

Brain 138 , 3221-37, (2015)

Polyglutamine diseases are a class of dominantly inherited neurodegenerative disorders for which there is no effective treatment. Here we provide evidence that activation of serotonergic signalling is...

German insurer finds a third of people over 65 take five or more drugs a day.

BMJ 346 , f3905, (2013)

Pharmacological treatment of tic disorders and Tourette Syndrome.

Neuropharmacology 68 , 143-9, (2013)

The present review gives an overview of current pharmacological treatment options of tic disorders and Tourette Syndrome (TS). After a short summary on phenomenology, clinical course and comorbid cond...

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泰必利