硫利达嗪_用途_密度_熔点_硫利达嗪CAS号【50-52-2】

硫利达嗪是多巴胺受体D2家族蛋白的拮抗剂,具有强大的抗精神病和抗焦虑活性。硫利达嗪也是PI3K-Akt-mTOR信号通路的有效抑制剂,具有抗血管生成作用。硫利达嗪在各种类型的癌细胞中显示出抗增殖和诱导凋亡作用,对靶向癌干细胞(CSCs)具有特异性[1][2][3][4]。

[ 描述 ]:

硫利达嗪是多巴胺受体D2家族蛋白的拮抗剂,具有强大的抗精神病和抗焦虑活性。硫利达嗪也是PI3K-Akt-mTOR信号通路的有效抑制剂,具有抗血管生成作用。硫利达嗪在各种类型的癌细胞中显示出抗增殖和诱导凋亡作用,对靶向癌干细胞(CSCs)具有特异性[1][2][3][4]。

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

信号通路 >> 自噬 >> 自噬

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 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

信号通路 >> 抗感染 >> 细菌

[体外研究]

硫利达嗪(0.01-100μM；48小时)以浓度依赖性方式降低NCI-N87和AGS细胞的细胞活力[2]。硫利达嗪(15μM；24小时)降低宫颈癌细胞(HeLa、Caski和C33A)和子宫内膜癌细胞(HEC-1-A和KLE)的细胞活力[4]。硫利达嗪(1-15μM；24-48小时)通过线粒体凋亡途径和线粒体途径诱导胃癌细胞死亡[2]。硫利达嗪(15μM；24 h)通过干扰PI3K/Akt通路调节细胞周期进程,并诱导宫颈癌和子宫内膜癌细胞G1细胞周期阻滞[4]。硫利达嗪抑制鲍曼不动杆菌对抗生素敏感和多重耐药菌株的生长[3]。细胞活力测定[1]细胞系：NCI-N87和AGS细胞。浓度：0.01,0.1,0.5,1,5,10,20,50,100μM。培养时间：48小时。结果：对胃癌细胞具有细胞毒性。Western Blot分析[1]细胞系：NCI-N87和AGS细胞浓度：1,5,10,15μM。培养时间：24,48小时。结果：caspase-9、caspase-8和caspase-3的前体表达下调。

[体内研究]

硫利达嗪(25mg/kg；连续3周每3天注射一次)可延长荷瘤小鼠的存活时间,并减少肿瘤内多能性胚胎癌(EC)细胞的数量[5]。硫利达嗪(1.0-5.0 mg/kg；s.c.)可减少口腔行为,并选择性地阻止重复的头部摆动[1]。动物模型：裸鼠和Rag2KO小鼠注射iPS细胞或NT2D1细胞[5]剂量：25mg/kg。给药：每3天注射一次,持续3周。结果：减少了恶性畸胎瘤中OCT4表达细胞的数量,延长了荷瘤小鼠的生存期。对生育率没有影响。

[参考文献]

[1]. Tschanz JT, et, al. Atypical antipsychotic drugs block selective components of amphetamine-induced stereotypy. Pharmacol Biochem Behav. 1988 Nov;31(3):519-22.

[2]. Mu J, et, al. Thioridazine, an antipsychotic drug, elicits potent antitumor effects in gastric cancer. Oncol Rep. 2014 May;31(5):2107-14.

[3]. Kang S, et, al. Thioridazine induces apoptosis by targeting the PI3K/Akt/mTOR pathway in cervical and endometrial cancer cells. Apoptosis. 2012 Sep;17(9):989-97.

[4]. Loehr AR, et, al. Targeting Cancer Stem Cells with Differentiation Agents as an Alternative to Genotoxic Chemotherapy for the Treatment of Malignant Testicular Germ Cell Tumors. Cancers (Basel). 2021 Apr 23;13(9):2045.

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
515.7±50.0 °C at 760 mmHg

[ 熔点 ]:
72-74°

[ 分子式 ]:
C₂₁H₂₆N₂S₂

[ 分子量 ]:
370.574

[ 闪点 ]:
265.7±30.1 °C

[ 精确质量 ]:
370.153748

[ PSA ]:
57.08000

[ LogP ]:
6.13

[ 外观性状 ]:
液体

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.677

[ 储存条件 ]:
?20°C

[ 水溶解性 ]:
Practically insoluble in water, very soluble in methylene chloride, freely soluble in methanol, soluble in ethanol (96 per cent).

CHEMICAL IDENTIFICATION

RTECS NUMBER :: SP2100000

CHEMICAL NAME :: Phenothiazine, 10-((1-methyl-2-piperidyl)ethyl)-2-(methylthio)-

CAS REGISTRY NUMBER :: 50-52-2

LAST UPDATED :: 199712

DATA ITEMS CITED :: 28

MOLECULAR FORMULA :: C21-H26-N2-S2

MOLECULAR WEIGHT :: 370.61

WISWESSER LINE NOTATION :: T C666 BN ISJ ES1 B2- BT6NTJ A1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 43 mg/kg

TOXIC EFFECTS :: Cardiac - other changes Lungs, Thorax, or Respiration - acute pulmonary edema Lungs, Thorax, or Respiration - cyanosis

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - child

DOSE/DURATION :: 28 mg/kg/2W-I

TOXIC EFFECTS :: Behavioral - muscle contraction or spasticity

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 14500 mg/kg/15Y-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - visual field changes Sense Organs and Special Senses (Eye) - retinal changes (pigmentary depositions, retinitis, other)

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 43 mg/kg

TOXIC EFFECTS :: Vascular - regional or general arteriolar or venous dilation Lungs, Thorax, or Respiration - chronic pulmonary edema Blood - hemorrhage

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - child

DOSE/DURATION :: 25 mg/kg

TOXIC EFFECTS :: Cardiac - change in rate Behavioral - toxic psychosis

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 24 mg/kg

TOXIC EFFECTS :: Autonomic Nervous System - parasympatholytic

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 5214 mg/kg/5Y-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - retinal changes (pigmentary depositions, retinitis, other)

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 995 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 150 mg/kg

TOXIC EFFECTS :: Behavioral - anticonvulsant Behavioral - antipsychotic

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 640 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Autonomic Nervous System - central sympatholytic Behavioral - alteration of classical conditioning

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 71 mg/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 385 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 65 mg/kg

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

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 310 mg/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 53 mg/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 1200 mg/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 26 mg/kg

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3040 mg/kg/22W-I

TOXIC EFFECTS :: Cardiac - EKG changes not diagnostic of specified effects

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 10 mg/kg

SEX/DURATION :: male 7 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - impotence

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 30 mg/kg

SEX/DURATION :: male 7 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - impotence

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3214 ug/kg

SEX/DURATION :: male 3 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - impotence

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 80 mg/kg

SEX/DURATION :: female 1-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

DOSE :: 100 mg/kg

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

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

MUTATION DATA

TEST SYSTEM :: Insect - Drosophila melanogaster

DOSE/DURATION :: 100 mg/L

REFERENCE :: IJEBA6 Indian Journal of Experimental Biology. (Publications & Information Directorate, CSIR, Hillside Rd., New Delhi 110 012, India) V.1- 1963- Volume(issue)/page/year: 11,403,1973 *** REVIEWS *** TOXICOLOGY REVIEW JMSCA9 Journal of Mental Science. (London, UK) V.4-108, 1857-1962. For publisher information, see BJPYAJ. Volume(issue)/page/year: 106,755,1960 TOXICOLOGY REVIEW IDPYAK Industrial Pharmacology. (Mount Kisco, NY) V.1-3, 1974-79. Discontinued. Volume(issue)/page/year: 1,203,1974 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5668 No. of Facilities: 35 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 430 (estimated) No. of Female Employees: 239 (estimated)

[ 符号 ]:

GHS02, GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H225-H301 + H311 + H331-H370-H412

[ 警示性声明 ]:
P210-P260-P273-P280-P301 + P310-P311

[ 危害码 (欧洲) ]:
F,T

[ 风险声明 (欧洲) ]:
11-23/24/25-39/23/24/25-52/53

[ 安全声明 (欧洲) ]:
16-36/37-45-61

[ 危险品运输编码 ]:
UN1230 - class 3 - PG 2 - Methanol, solution

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公司名：上海化源世纪贸易有限公司

区域：上海市普陀区

价格：

联系人：徐经理

产品详情：10-(2-(1-甲基哌啶-2-基)乙基)-2-(甲硫基)-10H吩噻嗪

公司名：上海源溪生物科技有限公司

区域：上海市浦东新区

价格：
￥需询单/1g

联系人：赖经理

产品详情：Thioridazine

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