<生产厂家价格>

乙巯匹拉嗪

乙巯匹拉嗪用途

噻乙基拉嗪是吩噻嗪衍生物,是一种口服有效的多巴胺D2受体和组胺H1受体拮抗剂。Thiethylprazine也是一种选择性ABCC1活化剂,可降低小鼠的淀粉样β(aβ)负荷。噻乙基拉嗪具有止吐、抗精神病和抗菌作用[1][2][3]。

乙巯匹拉嗪名称

[ CAS 号 ]:
1420-55-9

[ 中文名 ]:
乙巯匹拉嗪

[ 英文名 ]:
thiethylperazine

[中文别名 ]:

吐来抗

[英文别名 ]:

Ethylthioperazine.
Torecane
Tietylperazine
thietylperazine

乙巯匹拉嗪生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 感染

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

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

D2 Receptor

H1 Receptor

[体外研究]

噻乙基拉嗪在浓度低至2μg/mL时可增强抗生素(万古霉素)活性。噻乙基拉嗪抑制万古霉素敏感的粪肠球菌ATCC 29212、万古霉素耐药的粪肠杆菌ATCC 51299和万古霉素抗性的粪肠菌(VREF),MIC值分别为8μg/mL、16μg/mL和8μg/mL[3]。

[体内研究]

噻乙基拉嗪(3 mg/kg；肌肉注射；每天两次；持续30天)显著降低年轻APP/PS1小鼠的Aβ42水平[2]。动物模型：幼年Aβ前体蛋白(APPswe)和突变早老素-1(PS1)(APP/PS1)小鼠[2]剂量：3 mg/kg给药：肌肉注射；每天两次；30天结果：APP/PS1小鼠的Aβ42水平显著降低。

[参考文献]

[1]. Czeizel AE, et al. Case-control study of teratogenic potential of thiethylperazine, an anti-emetic drug. BJOG. 2003 May;110(5):497-9.

[2]. Krohn M, et al. Cerebral amyloid-β proteostasis is regulated by the membrane transport protein ABCC1 in mice. J Clin Invest. 2011 Oct;121(10):3924-31.

[3]. Rahbar M, et al. Enhancement of vancomycin activity by phenothiazines against vancomycin-resistant Enterococcus faecium in vitro. Basic Clin Pharmacol Toxicol. 2010 Aug;107(2):676-9.

乙巯匹拉嗪物理化学性质

[ 密度 ]:
1.24g/cm3

[ 沸点 ]:
559.8ºC at 760mmHg

[ 熔点 ]:
62-64°

[ 分子式 ]:
C₂₂H₂₉N₃S₂

[ 分子量 ]:
399.61600

[ 闪点 ]:
292.4ºC

[ 精确质量 ]:
399.18000

[ PSA ]:
60.32000

[ LogP ]:
4.97960

[ 折射率 ]:
1.5605 (estimate)

乙巯匹拉嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: SP0280000

CHEMICAL NAME :: Phenothiazine, 2-(ethylthio)-10-(3-(4-methyl-1-piperazinyl)propyl)-

CAS REGISTRY NUMBER :: 1420-55-9

LAST UPDATED :: 199512

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C22-H29-N3-S2

MOLECULAR WEIGHT :: 399.66

WISWESSER LINE NOTATION :: T C666 BN ISJ ES2 B3- AT6N DNTJ D1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Rectal

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 857 ug/kg/2D-I

TOXIC EFFECTS :: Behavioral - ataxia

REFERENCE :: DICPBB Drug Intelligence and Clinical Pharmacy. (POB 42435, Cincinnati, OH 45242) V.3- 1969- Volume(issue)/page/year: 19,550,1985

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 680 mg/kg

TOXIC EFFECTS :: Behavioral - antipsychotic

REFERENCE :: DNEUD5 Developments in Neuroscience (Amsterdam). (Elsevier Science Pub. Co., Inc., 52 Vanderbilt Ave., New York, NY 10017) V.1- 1977- Volume(issue)/page/year: 7,45,1980

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 71600 ug/kg

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 2,411,1968 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4792 No. of Facilities: 18 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 1333 (estimated) No. of Female Employees: 656 (estimated)