二马来酸硫乙基哌嗪

二马来酸硫乙基哌嗪用途

Thiethylperazine dimaleate 是一种吩噻嗪衍生物,也是一种口服活性多巴胺 D2 受体和组胺 H1 受体拮抗剂。Thiethylperazine dimaleate 也是一种选择性的 ABCC1 激活剂,可减少小鼠中的淀粉样 β (Aβ) 负荷。Thiethylperazine dimaleate 具有止吐,抗精神病和抗菌作用。

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二马来酸硫乙基哌嗪名称

[ CAS 号 ]:
1179-69-7

[ 中文名 ]:
马来酸乙巯拉嗪

[ 英文名 ]:
Thiethylperazine dimaleate

[英文别名 ]:

2-butenedioate
torecandimaleate
Thiethylperazinbishydrogenmaleat
THIETHYLPERAZINE MALEATE (200 MG)
torecanmaleate
torecanbimaleate
thiethylperazine dimaleate
torecan
toresten
tresten

二马来酸硫乙基哌嗪生物活性

[ 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 ]

Dopamine D2-receptor[1] Histamine H1-receptor[1] ABCC1[2] Enterococcus faecalis[3]

[体外研究]

在低至2μg/mL的浓度下,噻乙基哌嗪可增强抗生素(万古霉素)的活性。噻乙基哌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球菌ATCC 51299和万古霉素耐药的粪肠球菌(VREF),MIC值分别为8μg/mL、16μg/mL和8μg/mL[3]。

[体内研究]

Thiethylperazine(3 mg/kg；肌肉注射；每日两次；持续30天；幼年APP/PS1小鼠)治疗显著降低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：3mg/kg,肌肉注射,每日2次,连续30d,结果：APP/PS1小鼠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.

二马来酸硫乙基哌嗪物理化学性质

[ 密度 ]:
1.24g/cm3

[ 沸点 ]:
559.8ºC at 760 mmHg

[ 熔点 ]:
62-64ºC

[ 分子式 ]:
C₃₀H₃₇N₃O₈S₂

[ 分子量 ]:
631.760

[ 闪点 ]:
292.4ºC

[ 精确质量 ]:
631.202209

[ PSA ]:
209.52000

[ LogP ]:
4.40320

[ 蒸汽压 ]:
1.46E-12mmHg at 25°C

[ 储存条件 ]:
2-8°C，密封，干燥，避光

二马来酸硫乙基哌嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: SP0350000

CAS REGISTRY NUMBER :: 1179-69-7

LAST UPDATED :: 199504

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C22-H29-N3-S2.2C4-H4-O4

MOLECULAR WEIGHT :: 631.82

WISWESSER LINE NOTATION :: T C666 BN ISJ ES2 B3- AT6N DNTJ D1 &OV1U1VO

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 :: 1260 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: -,51,1972

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 90 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: -,51,1972

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 680 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: -,51,1972

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 217 mg/kg

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

REFERENCE :: MEXPAG Medicina Experimentalis. (Basel, Switzerland) V.1-11, 1959-64; V.18-19, 1968-69. For publisher information, see JNMDBO. Volume(issue)/page/year: 4,145,1961

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 93 mg/kg

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

REFERENCE :: MEXPAG Medicina Experimentalis. (Basel, Switzerland) V.1-11, 1959-64; V.18-19, 1968-69. For publisher information, see JNMDBO. Volume(issue)/page/year: 4,145,1961

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 1050 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: -,51,1972

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 27 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: -,51,1972 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5553 No. of Facilities: 23 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 722 (estimated) No. of Female Employees: 377 (estimated)