地塞米松磷酸钠

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。

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)

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%

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