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替普瑞酮

替普瑞酮用途

Teprenone 是一种抗溃疡药,为热休克蛋白 (heat shock proteins) 的诱导剂。

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替普瑞酮名称

[ CAS 号 ]:
6809-52-5

[ 中文名 ]:
6,10,14,18-四甲基-5,9,13,17-十九碳四烯-2-酮

[ 英文名 ]:
Teprenone

[中文别名 ]:

[英文别名 ]:

Geranylgeranyl acetone
GGA
geranylgeranylacetone
Teprenone
E36U31
MFCD00866901
Selbex

替普瑞酮生物活性

[ 描述 ]:

Teprenone 是一种抗溃疡药,为热休克蛋白 (heat shock proteins) 的诱导剂。

[ 相关类别 ]:

信号通路 >> 细胞周期/DNA损伤 >> HSP

信号通路 >> 代谢酶/蛋白酶 >> HSP

研究领域 >> 神经疾病

[ 靶点 ]

HSP

[体外研究]

替普瑞酮是HSP的诱导物。替普瑞酮(Geranylgeranylacetone,1μM)显着防止乙醇诱导的脱落,并减少胃粘膜细胞中的乳酸脱氢酶(LDH)释放。替普瑞酮(1μM)逐渐增加HSC70水平,并在30-60分钟内快速积累应激诱导型HSP90,HSP70和HSP60浓度。替普瑞酮还激活热休克因子1 [1]。替普瑞酮(0-20μM)在照射(IR)后略微增加人脐静脉内皮细胞(HUVEC)活力。替普瑞酮(10μM)对HUVEC迁移和侵袭没有影响,但在有和没有IR的情况下增强HUVEC管形成和伤口愈合。替普瑞酮(10μM)还通过诱导HUVEC中的VEGF和eNOS表达来促进血管生成[3]。

[体内研究]

替普瑞酮(200mg/kg,口服)导致大鼠中HSP70mRNA的积累,并且与载体预处理的大鼠相比,通过Teprenone预处理的大鼠的粘膜中的应力添加增强了积累。替普瑞酮(200mg/kg,口服)显着抑制大鼠2小时和4小时应激负荷后的溃疡形成[1]。替普瑞酮(每天200mg/kg)诱导来自大鼠视网膜的视网膜神经节细胞(RGC)中的HSP72。替普瑞酮显着降低RGC的损失(在眼压升高后评估),减轻视神经损伤,减少RGC层中TUNEL阳性细胞的数量,并增加青光眼大鼠模型中的HSP72 [2]。替普瑞酮(200mg/kg,po)对小鼠的辐射诱导的肠损伤具有保护作用[3]。

[细胞实验]

在Teprenone和/或放射治疗之前，将人脐静脉内皮细胞（HUVEC）以1×10 2个细胞/孔的密度接种到48孔板上。在无血清培养基中使用0.5mg / mL MTT溶液处理后48小时测定细胞活力。将该溶液与细胞在含有5％CO 2的37℃湿润气氛中温育2小时。然后，除去MTT溶液，将细胞溶解在100μLDMSO中。用ELISA分光光度计在540nm处测量上清液的光密度[3]。

[动物实验]

将重约250g的雄性Wister品系大鼠单独圈养在保持在23℃，12小时明暗循环的房间中的金属丝网笼中。允许大鼠自由进入标准实验室食物。替尼龙（200mg / kg;含5％阿拉伯树胶和0.008％α-生育酚的乳液）或载体（含有0.008％α-生育酚的5％阿拉伯胶乳）以5mL / kg的体积通过金属口服给药管道连接到6毫升注射器。两小时后，将大鼠置于约束笼中，然后垂直浸入23℃的水中至剑突过程的水平。在指定的时间通过断头处死大鼠[1]。

[参考文献]

[1]. Hirakawa T, et al. Geranylgeranylacetone induces heat shock proteins in cultured guinea pig gastric mucosal cells and rat gastric mucosa. Gastroenterology. 1996 Aug;111(2):345-57.

[2]. Caprioli J, et al. Retinal ganglion cell protection with geranylgeranylacetone, a heat shock protein inducer, in a rat glaucoma model. Trans Am Ophthalmol Soc. 2003;101:39-50; discussion 50-1.

[3]. Han NK, et al. Geranylgeranylacetone Ameliorates Intestinal Radiation Toxicity by Preventing Endothelial Cell Dysfunction. Int J Mol Sci. 2017 Oct 7;18(10).

[相关活性小分子]

替普瑞酮物理化学性质

[ 密度 ]:
0.9±0.1 g/cm3

[ 沸点 ]:
442.2±24.0 °C at 760 mmHg

[ 分子式 ]:
C₂₃H₃₈O

[ 分子量 ]:
330.55

[ 闪点 ]:
168.0±9.8 °C

[ PSA ]:
17.07000

[ LogP ]:
8.20

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.483

[ 储存条件 ]:
?20°C

替普瑞酮MSDS

详细MSDS(安全技术说明书)

替普瑞酮毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RA5391300

CHEMICAL NAME :: 5,9,13,17-Nonadecatetraen-2-one, 6,10,14,18-tetramethyl-

CAS REGISTRY NUMBER :: 6809-52-5

LAST UPDATED :: 199110

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C23-H38-O

MOLECULAR WEIGHT :: 330.61

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 :: >15 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,703,1990

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3500 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,703,1990

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >10 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,703,1990

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >5 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,703,1990

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3750 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 16,357,1985

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >10 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,703,1990

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >5 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,703,1990

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >1 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,703,1990

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替普瑞酮安全信息

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38:Irritating to eyes, respiratory system and skin .

[ 安全声明 (欧洲) ]:
S26-S36/37/39

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

[ RTECS号 ]:
RA5391300

[ 海关编码 ]:
2914190090

替普瑞酮合成路线

详细合成路线

替普瑞酮上下游产品

替普瑞酮上游产品

替普瑞酮下游产品

替普瑞酮海关

[ 海关编码 ]: 2914190090

[ 中文概述 ]:
2914190090 其他不含其他含氧基的无环酮。监管条件:无。增值税率:17.0%。退税率:9.0%。最惠国关税:5.5%。普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 丙酮报明包装

[ Summary ]:
2914190090 other acyclic ketones without other oxygen function。Supervision conditions:None。VAT:17.0%。Tax rebate rate:9.0%。MFN tariff:5.5%。General tariff:30.0%

替普瑞酮文献

Heat shock protein 72 suppresses apoptosis by increasing the stability of X-linked inhibitor of apoptosis protein in renal ischemia/reperfusion injury.

Mol. Med. Report. 11(3) , 1793-9, (2014)

X‑linked inhibitor of apoptosis protein (XIAP) negatively regulates apoptotic pathways at a post‑mitochondrial level. XIAP functions by directly binding and inhibiting activation of specific caspases....

Aldioxa improves delayed gastric emptying and impaired gastric compliance, pathophysiologic mechanisms of functional dyspepsia.

Sci. Rep. 5 , 17519, (2015)

Delayed gastric emptying and impaired gastric accommodation (decreased gastric compliance) play important roles in functional dyspepsia (FD). Here we screen for a clinically used drug with an ability ...

Efficacy of omeprazole, famotidine, mosapride and teprenone in patients with upper gastrointestinal symptoms: an omeprazole-controlled randomized study (J-FOCUS).

BMC Gastroenterol. 12 , 42, (2012)

In Japan, treatment guidelines are lacking for patients with upper gastrointestinal symptoms. We aimed to compare the efficacy of different drugs for the treatment of uninvestigated upper gastrointest...

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