地塞米松磷酸钠

地塞米松磷酸钠用途

肾上腺皮质激素类药物，抗炎，抗毒，抗过敏。

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地塞米松磷酸钠作用

（1）抗炎作用：本品减轻和防止组织对炎症的反应，从而减轻炎症的表现。能够抑制炎症细胞，包括巨噬细胞和白细胞在炎症部位的集聚，并抑制吞噬作用、溶酶体酶的释放以及炎症化学中介物的合成和释放。
（2）免疫抑制作用：包括防止或抑制细胞介导的免疫反应，延迟性的过敏反应，减少T淋巴细胞、单核细胞、噬酸性细胞的数目，降低免疫球蛋白与细胞表面受体的结合能力，并抑制白介素的合成与释放，从而降低T淋巴细胞向淋巴母细胞转化，并减轻情原发免疫反应的扩展。本品还降低免疫复核物通过基底膜，并能减少补体成分及免疫球蛋白的浓度。

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地塞米松磷酸钠名称

[ CAS 号 ]:
2392-39-4

[ 中文名 ]:
地塞米松磷酸钠

[ 英文名 ]:
Dexamethasone 21-phosphate disodium salt

[中文别名 ]:

[英文别名 ]:

Turbinaire
Dexamethasone 21-Phosphate Disodium Salt Hydrate
Oradexon
UNII-AI9376Y64P
Hexadrol
Solu-Decadron
Dalalone
Wymesone
DEXAMETHASONE DISODIUM PHOSPHATE
Dexamethasone Sodium Phosphate

地塞米松磷酸钠生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 糖皮质激素受体

研究领域 >> 炎症/免疫

[ 靶点 ]

Glucocorticoid receptor[1]

[体外研究]

地塞米松调节几种转录因子,包括激活蛋白-1,核因子-AT和核因子-κB,导致激活和抑制参与炎症反应的关键基因[1]。地塞米松有效抑制A549细胞释放粒细胞-巨噬细胞集落刺激因子(GM-CSF),EC50为2.2 nM。发现地塞米松(EC50 = 36nM)诱导β2受体的转录与糖皮质激素受体(GR)DNA结合相关,并且发生在比GM-CSF释放抑制高10-100倍的浓度。地塞米松(IC50 = 0.5 nM)抑制3×κB(NF-κB,IκBα和I-κBβ),这与抑制GM-CSF释放有关[2]。

[体内研究]

用2×5mg/kg剂量的地塞米松治疗有效抑制脂多糖(LPS)诱导的炎症。在我们的实验系统中,与暴露于LPS并仅注射溶剂(盐水)的动物相比,用单剂量地塞米松10mg/kg(ip)治疗显着降低了粒细胞的募集以及氧自由基的自发产生。当在吸入LPS之前1小时和之后1小时施用时,效果是统计学显着的。 BALF中的粒细胞数量下降到与健康动物相当的水平(给定水雾剂)[3]。用地塞米松处理的大鼠比对照大鼠消耗更少的食物并且重量更轻。虽然他们的食物摄入量相似,但处理过的大鼠也比配对喂养的动物重量轻。 5天的地塞米松注射导致肝脏质量(+ 42％)和肝脏与体重比率(+ 65％)显着增加。治疗5天后,腓肠肌的湿重减少20％,但相对于体重(g/100 g体重),它仍未受影响,表明肌肉减重与体重减轻平行[4]。

[动物实验]

大鼠：使用雄性Sprague-Dawley大鼠。每天一次用地塞米松（1.5mg / kg体重）腹膜内注射地塞米松处理的大鼠5天，并允许随意喂食。对照大鼠不接受任何治疗并随意喂食。为了考虑地塞米松处理诱导的食物摄入减少，使用第三组配对喂养的大鼠。给这些大鼠提供与注射地塞米松的大鼠相同量的食物，并用每日等容的腹膜内注射NaCl（0.9％）处理5天。在最后注射地塞米松或NaCl后，将动物禁食过夜，然后通过断头处死[4]。小鼠：在所有实验中使用雌性C57Bl / 6JBom小鼠（10-12周龄）。地塞米松以1或10mg / kg的单次注射给药。将地塞米松溶于盐水中，在LPS暴露前1小时或1小时腹膜内注射400μL。在一个实验中，在攻击前1小时开始每4-5小时连续注射N-乙酰半胱氨酸（NAC）（100和500mg / kg）（总共5次注射）。对照组的LPS暴露的动物腹膜内注射溶剂（盐水）。通过将100μLNAAC（50,100或500mg / kg）或地塞米松（10mg / kg）滴注到用15mg / kg Rapinovet（iv）麻醉的小鼠的肺中进行气管内给药[3]。

[参考文献]

[1]. LaLone CA, et al. Effects of a glucocorticoid receptor agonist, Dexamethasone, on fathead minnow reproduction, growth, and development. Environ Toxicol Chem. 2012 Mar;31(3):611-22.

[2]. Adcock IM, et al. Ligand-induced differentiation of glucocorticoid receptor (GR) trans-repression and transactivation: preferential targetting of NF-kappaB and lack of I-kappaB involvement. Br J Pharmacol. 1999 Jun;127(4):1003-11.

[3]. Rocksén D, et al. Differential anti-inflammatory and anti-oxidative effects of Dexamethasone and N-acetylcysteine in endotoxin-induced lung inflammation. Clin Exp Immunol. 2000 Nov;122(2):249-56.

[4]. Roussel D, et al. Dexamethasone treatment specifically increases the basal proton conductance of rat liver mitochondria. FEBS Lett. 2003 Apr 24;541(1-3):75-9.

[相关活性小分子]

地塞米松磷酸钠物理化学性质

[ 密度 ]:
1.32g/cm3

[ 沸点 ]:
669.6ºC at 760 mmHg

[ 熔点 ]:
233-235 °C

[ 分子式 ]:
C₂₂H₂₈FNa₂O₈P

[ 分子量 ]:
516.405

[ 闪点 ]:
358.7ºC

[ 精确质量 ]:
516.130127

[ PSA ]:
156.83000

[ LogP ]:
2.88910

[ 外观性状 ]:
白色至灰白色粉末

[ 蒸汽压 ]:
2.81E-15mmHg at 25°C

[ 折射率 ]:
1.591

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
H2O: 50 mg/mL, clear, faintly yellow

地塞米松磷酸钠MSDS

详细MSDS(安全技术说明书)

地塞米松磷酸钠毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TU4056000

CHEMICAL NAME :: Pregna-1,4-diene-3,20-dione, 9-fluoro-11-beta,17,21-trihydroxy-16-alpha-methyl-, 21-(dihydrogen phosphate) disodium salt

CAS REGISTRY NUMBER :: 2392-39-4

LAST UPDATED :: 199806

DATA ITEMS CITED :: 27

MOLECULAR FORMULA :: C22-H28-F-O8-P.2Na

MOLECULAR WEIGHT :: 516.45

WISWESSER LINE NOTATION :: L E5 B666 OV AHTTT&J A1 BF CQ E1 FV1OPWO FQ G1 &-NA- 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - infant

DOSE/DURATION :: 1500 ug/kg/3D-I

TOXIC EFFECTS :: Brain and Coverings - recordings from specific areas of CNS

REFERENCE :: LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 1,632,1987

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 320 mg/kg

TOXIC EFFECTS :: Gastrointestinal - other changes

REFERENCE :: LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 1,1035,1986

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - child

DOSE/DURATION :: 1 mg/kg

TOXIC EFFECTS :: Gastrointestinal - peritonitis

REFERENCE :: AJEMEN American Journal of Emergency Medicine. (WB Saunders, Philadelphia, PA) V.1- 1983- Volume(issue)/page/year: 10,268,1992

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 357 ug/kg

TOXIC EFFECTS :: Gastrointestinal - peritonitis

REFERENCE :: AJEMEN American Journal of Emergency Medicine. (WB Saunders, Philadelphia, PA) V.1- 1983- Volume(issue)/page/year: 10,268,1992

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1800 mg/kg

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

REFERENCE :: ATSUDG Archives of Toxicology, Supplement. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) No.1- 1978- Volume(issue)/page/year: 7,90,1984

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 550 mg/kg

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

REFERENCE :: ATSUDG Archives of Toxicology, Supplement. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) No.1- 1978- Volume(issue)/page/year: 7,90,1984

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 932 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: -,785,1995 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 7500 ug/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 119,391,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 119,391,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 400 ug/kg

SEX/DURATION :: female 19-20 day(s) after conception

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

REFERENCE :: PEDIAU Pediatrics. (American Academy of Pediatrics, P.O. Box 1034, Evanston, IL 60204) V.1- 1948- Volume(issue)/page/year: 65,287,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 10 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 119,391,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 119,391,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 12800 ug/kg

SEX/DURATION :: female 11-14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

REFERENCE :: SEIJBO Senten Ijo. Congenital Anomalies. (Nippon Senten Ijo Gakkai, c/o Kinki Daigaku Igakubu Kaibagaku Kyoshitsu, 380 Nishiyama, Sayama-cho, Mirami-Kawachi-gun, Osaka-fu, Japan) V.1-26, 1960-86. For publisher information, see CGANE7. Volume(issue)/page/year: 13,245,1973

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 130 ug/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 119,391,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 650 ug/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 119,391,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 9 mg/kg

SEX/DURATION :: female 21-26 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - parturition Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: JOENAK Journal of Endocrinology. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1939- Volume(issue)/page/year: 64,363,1975

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 300 ug/kg

SEX/DURATION :: female 25-27 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - gastrointestinal system

REFERENCE :: JSGRA2 Journal of Surgical Research. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1961- Volume(issue)/page/year: 57,274,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

DOSE :: 8 mg/kg

SEX/DURATION :: female 11-14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - body wall

REFERENCE :: ANIFAC Annales de Chirurgie Infantile. (Paris, France) V.1- 1960(?)- Volume(issue)/page/year: 3,73,1962

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

DOSE :: 8 mg/kg

SEX/DURATION :: female 11-14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: ANIFAC Annales de Chirurgie Infantile. (Paris, France) V.1- 1960(?)- Volume(issue)/page/year: 3,73,1962

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

DOSE :: 4 mg/kg

SEX/DURATION :: female 11 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Fertility - abortion

REFERENCE :: ANIFAC Annales de Chirurgie Infantile. (Paris, France) V.1- 1960(?)- Volume(issue)/page/year: 3,73,1962

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 145 ug/kg

SEX/DURATION :: female 20 week(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - parturition

REFERENCE :: AAAHAN Australian Journal of Experimental Agriculture and Animal Husbandry. (Commonwealth Scientific and Industrial Research Organization, 314 Albert St., E. Melbourne, Vic. 3002, Australia) V.1- 1961- Volume(issue)/page/year: 16,462,1976

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 2739 ug/kg

SEX/DURATION :: female 21 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects

REFERENCE :: JRFSAR Journal of Reproduction and Fertility, Supplement. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) No.1- 1966- Volume(issue)/page/year: 32,247,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 1304 ug/kg

SEX/DURATION :: female 10 day(s) pre-mating

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

REFERENCE :: JRFSAR Journal of Reproduction and Fertility, Supplement. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) No.1- 1966- Volume(issue)/page/year: 32,247,1982 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 82148 No. of Facilities: 67 (estimated) No. of Industries: 2 No. of Occupations: 1 No. of Employees: 680 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 82148 No. of Facilities: 363 (estimated) No. of Industries: 2 No. of Occupations: 7 No. of Employees: 16943 (estimated) No. of Female Employees: 14180 (estimated)

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地塞米松磷酸钠安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H351-H361

[ 警示性声明 ]:
P280-P301 + P312 + P330

[ 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;R40;R63

[ 安全声明 (欧洲) ]:
S36/37/39

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

[ WGK德国 ]:
3

[ RTECS号 ]:
TU4056000

[ 海关编码 ]:
2937290090

地塞米松磷酸钠海关

[ 海关编码 ]: 2919900090

[ 中文概述 ]:
HS:2919900090 其他磷酸酯及其盐（包括乳磷酸盐）（包括它们的卤化，磺化，硝化和亚硝化衍生物）增值税率:17.0% 退税率:9.0% 监管条件:AB(入境货物通关单,出境货物通关单) 最惠国关税:6.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ 监管条件 ]: A.入境货物通关单 B.出境货物通关单

[ 检验检疫 ]: R.进口食品卫生监督检验 S.出口食品卫生监督检验 M.进口商品检验 N.出口商品检验

[ Summary ]:
2919900090 other phosphoric esters and their salts, including lactophosphates; their halogenated, sulphonated, nitrated or nitrosated derivatives。supervision conditions:AB(certificate of inspection for goods inward,certificate of inspection for goods outward)。VAT:17.0%。tax rebate rate:9.0%。MFN tariff:6.5%。general tariff:30.0%

地塞米松磷酸钠文献

Developmental Expression and Glucocorticoid Control of the Leptin Receptor in Fetal Ovine Lung.

PLoS ONE 10 , e0136115, (2015)

The effects of endogenous and synthetic glucocorticoids on fetal lung maturation are well-established, although the role of leptin in lung development before birth is unclear. This study examined mRNA...

Contralateral eye comparison of descemet membrane endothelial keratoplasty and descemet stripping automated endothelial keratoplasty.

Am. J. Ophthalmol. 159(1) , 155-9.e1, (2014)

To compare objective and subjective outcomes after Descemet membrane endothelial keratoplasty (DMEK) and Descemet stripping automated endothelial keratoplasty (DSAEK) in the fellow eye of the same pat...

Eliminating antibiotic prophylaxis for intravitreal injections: a consecutive series of 18,839 injections by a single surgeon.

Retina (Philadelphia, Pa.) 35(4) , 783-8, (2015)

By optimizing the protocol for intravitreal injections, the risk of endophthalmitis can be minimized. This study assesses the incidence of endophthalmitis and other complications after a consecutive s...

更多文献

地塞米松磷酸钠

地塞米松磷酸钠用途

地塞米松磷酸钠作用

地塞米松磷酸钠名称

地塞米松磷酸钠生物活性

地塞米松磷酸钠物理化学性质

地塞米松磷酸钠MSDS

详细MSDS(安全技术说明书)

地塞米松磷酸钠毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

地塞米松磷酸钠安全信息

地塞米松磷酸钠海关

地塞米松磷酸钠文献

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