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氯甲苯噻嗪

氯甲苯噻嗪用途

Diazoxide是一种ATP敏感性的钾离子通道激活剂; 可用于治疗高胰岛素血症。

氯甲苯噻嗪名称

[ CAS 号 ]:
364-98-7

[ 中文名 ]:
氯甲苯噻嗪

[ 英文名 ]:
diazoxide

[中文别名 ]:

[英文别名 ]:

diazoxidum [INN_la]
Hypertonalum
Diazoxido
Sodium dodecyl sulphate solution
EINECS 206-668-1
Mutabase
Proglycem
Dizoxide
Diazossido
MFCD00078578

氯甲苯噻嗪生物活性

[ 描述 ]:

Diazoxide是一种ATP敏感性的钾离子通道激活剂; 可用于治疗高胰岛素血症。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

信号通路 >> 跨膜转运 >> 钾通道

研究领域 >> 心血管疾病

[体外研究]

二氮嗪具有许多生理作用,包括降低血压和纠正低血糖。二氮嗪对心肌缺血具有强大的保护作用[1]。二氮嗪可以保护NSC-34神经元免受神经退行性损伤的主要来源。二氮嗪增加NSC-34运动神经元中的Nrf2核转位并防止内源性氧化损伤[2]。

[体内研究]

二氮嗪通过打开mitoKATP通道减弱复苏后脑损伤,保护线粒体功能,抑制脑细胞凋亡,并激活PKC通路[3]。在野生型小鼠中用二氮嗪治疗可降低眼压(IOP)21.5±3.2％,绝对眼压降低3.9±0.6 mm Hg [4]。

[细胞实验]

将二氮嗪溶解在DMSO中以制备50mM储备溶液。允许NSC-34细胞在降低的血清条件下分化8周，然后接种在24孔板中。将谷氨酸盐溶解在培养基中，并以10μM的浓度加入培养物中24小时。在谷氨酸暴露前2小时开始用100μM二氮嗪进行细胞处理。通过MTT测定法测量细胞活力[2]。

[动物实验]

大鼠：成年雄性Sprague-Dawley大鼠诱导脑缺血（每组10只）接受腹腔注射0.1％DMSO（1 mL;载体组），二氮嗪（10 mg / kg; DZ组）或二氮嗪（10只）在CPR后30分钟，加上5-羟基癸酸盐（5mg / kg; DZ + 5-HD组）。对照组（假手术组，n = 5）进行假手术，无心脏骤停。确定线粒体呼吸控制率（RCR）。使用TUNEL染色评估脑细胞凋亡。通过蛋白质印迹和免疫组织化学确定Bcl-2，Bax和蛋白激酶Cε（PKCε）在大脑皮质中的表达[3]。小鼠：通过在PBS中的10％聚乙氧基化蓖麻油中稀释100mM储备溶液来制备二氮嗪。在C57BL / 6野生型和Kir6.2（ - / - ）小鼠中，向每只小鼠的一只眼睛局部施用5μL的5mM二氮嗪滴剂，同时对照眼睛接受载体（DMSO和10％聚乙氧基化蓖麻油）与治疗眼睛的比例相同）。每天在治疗后1小时，4小时和23小时测量IOP。用二氮嗪和载体治疗每天持续连续14天[4]。

[参考文献]

[1]. Coetzee WA, et al. Multiplicity of effectors of the cardioprotective agent, diazoxide. Pharmacol Ther. 2013 Nov;140(2):167-75.

[2]. Virgili N, et al. K(ATP) channel opener diazoxide prevents neurodegeneration: a new mechanism of action viaantioxidative pathway activation. PLoS One. 2013 Sep 11;8(9):e75189.

[3]. Wu H, et al. Diazoxide Attenuates Postresuscitation Brain Injury in a Rat Model of Asphyxial Cardiac Arrest by Opening Mitochondrial ATP-Sensitive Potassium Channels. Biomed Res Int. 2016;2016:1253842.

[4]. Chowdhury UR, et al. ATP-sensitive potassium (K(ATP)) channel openers diazoxide and nicorandil lower intraocular pressure in vivo. Invest Ophthalmol Vis Sci. 2013 Jul 22;54(7):4892-9.

[相关活性小分子]

氯甲苯噻嗪物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 沸点 ]:
414.8±47.0 °C at 760 mmHg

[ 熔点 ]:
>310°C

[ 分子式 ]:
C₈H₇ClN₂O₂S

[ 分子量 ]:
230.671

[ 闪点 ]:
204.6±29.3 °C

[ 精确质量 ]:
229.991669

[ PSA ]:
66.91000

[ LogP ]:
1.08

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.692

[ 储存条件 ]:
Store at RT

[ 水溶解性 ]:
0.1 M NaOH: soluble

氯甲苯噻嗪MSDS

详细MSDS(安全技术说明书)

氯甲苯噻嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DK8185000

CHEMICAL NAME :: 2H-1,2,4-Benzothiadiazine, 7-chloro-3-methyl-, 1,1-dioxide

CAS REGISTRY NUMBER :: 364-98-7

LAST UPDATED :: 199504

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C8-H7-Cl-N2-O2-S

MOLECULAR WEIGHT :: 230.68

WISWESSER LINE NOTATION :: T66 BSWM ENJ D1 IG

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 :: 980 mg/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 143,446,1963

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 510 mg/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 143,446,1963

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 444 mg/kg

TOXIC EFFECTS :: Vascular - BP lowering not characterized in autonomic section

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 136,344,1962

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 326 mg/kg

TOXIC EFFECTS :: Vascular - BP lowering not characterized in autonomic section

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 136,344,1962

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 228 mg/kg

TOXIC EFFECTS :: Vascular - BP lowering not characterized in autonomic section

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 136,344,1962 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 65 mg/kg

SEX/DURATION :: female 110-114 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - other effects to embryo

REFERENCE :: JCNDBK Journal of Clinical Pharmacology and New Drugs. (Stamford, CT) V.11-13, 1971-73. For publisher information, see JCPCBR. Volume(issue)/page/year: 11,206,1971 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X7114 No. of Facilities: 63 (estimated) No. of Industries: 1 No. of Occupations: 3 No. of Employees: 612 (estimated) No. of Female Employees: 395 (estimated)

氯甲苯噻嗪安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R22;R36/37/38

[ 安全声明 (欧洲) ]:
S22;S26;S36

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

[ WGK德国 ]:
3

[ RTECS号 ]:
DK8185000

[ 海关编码 ]:
2933990090

氯甲苯噻嗪合成路线

详细合成路线

氯甲苯噻嗪上下游产品

氯甲苯噻嗪上游产品

氯甲苯噻嗪下游产品

氯甲苯噻嗪制备

由5-氯-2-乙酰胺基-N-乙酰基苯磺酰胺经高温环合而得。环合反应在250-260℃进行，搅拌15min。然后冷却，待物料凝固后研细，用乙醇洗涤，得二氮嗪粗品。用40倍量的80%乙醇重结晶，得成品。

氯甲苯噻嗪海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 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:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

氯甲苯噻嗪文献

Magnesium isoglycyrrhizinate protects hepatic L02 cells from ischemia/reperfusion induced injury.

Int. J. Clin. Exp. Pathol. 7(8) , 4755-64, (2014)

Human liver ischemia/reperfusion injury (IRI) is a common and major clinical problem complicating liver surgery and transplantation. The pathogenesis underlying IRI is complex, involving a series of s...

Accelerated recovery of mitochondrial membrane potential by GSK-3β inactivation affords cardiomyocytes protection from oxidant-induced necrosis.

PLoS ONE 9(11) , e112529, (2014)

Loss of mitochondrial membrane potential (ΔΨm) is known to be closely linked to cell death by various insults. However, whether acceleration of the ΔΨm recovery process prevents cell necrosis remains ...

ATP-sensitive potassium (K(ATP)) channel openers diazoxide and nicorandil lower intraocular pressure in vivo.

Invest. Ophthalmol. Vis. Sci. 54(7) , 4892-9, (2013)

To evaluate the expression of ATP-sensitive potassium (K(ATP)) channel subunits and study the effect of K(ATP) channel openers diazoxide and nicorandil on intraocular pressure (IOP) in an in vivo mous...

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