1179-69-7

• 常用中文名：二马来酸硫乙基哌嗪
• 常用英文名：Thiethylperazine dimaleate
• CAS号：1179-69-7
• 分子式：C₃₀H₃₇N₃O₈S₂
• 分子量：631.760
• 相关类别： 信号通路 抗感染 细菌
• 发布时间：2018-08-20 19:39:48
• 更新时间：2024-01-11 16:26:26
• 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。

名称

• 中文名: 马来酸乙巯拉嗪
• 英文名: thiethylperazine maleate
• 英文别名: 2-butenedioate; torecandimaleate; 2-(Ethylsulfanyl)-10-[3-(4-methylpiperazin-1-yl)propyl]-10H-phenothiazine (2Z)-but-2-enedioate (1:2); Thiethylperazinbishydrogenmaleat; THIETHYLPERAZINE MALEATE (200 MG); torecanmaleate; torecanbimaleate; thiethylperazine dimaleate; 10H-Phenothiazine, 2-(ethylthio)-10-[3-(4-methyl-1-piperazinyl)propyl]-, (2Z)-2-butenedioate (1:2); torecan; toresten; tresten; 2-(Ethylsulfanyl)-10-[3-(4-methyl-1-piperazinyl)propyl]-10H-phenothiazine (2Z)-2-butenedioate (1:2); gs-95

物化性质

• 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

生物活性

• 描述: 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。
• 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.

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)

安全

• 危害码 (欧洲): Xi