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醋酸地塞米松

醋酸地塞米松用途

Dexamethasone是糖皮质素类甾体化合物,有抗炎和免疫抑制活性。

醋酸地塞米松名称

[ CAS 号 ]:
1177-87-3

[ 中文名 ]:
醋酸地塞米松

[ 英文名 ]:
Dexamethasone-17-acetate

[中文别名 ]:

[英文别名 ]:

MFCD00027407
Dexamethasone acetate
EINECS 214-646-8
DEXAMETHASONE 21-ACETATE
Dexamethasone (acetate)

醋酸地塞米松生物活性

[ 描述 ]:

Dexamethasone是糖皮质素类甾体化合物,有抗炎和免疫抑制活性。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 糖皮质激素受体

信号通路 >> 自噬 >> 自噬

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]

先前已报道用2×5mg/kg剂量的地塞米松有效抑制脂多糖(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]

小鼠[3]雌性C57Bl / 6JBom小鼠（10-12周龄）用于所有实验。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，从攻击前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）麻醉的小鼠的肺中来进行气管内给药。使用大鼠[4]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。特别选择地塞米松剂量（1.5mg / kg /天）和治疗持续时间（5天），因为该治疗诱导了可重复且显着的分解代谢状态。对照大鼠未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。

[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]

醋酸地塞米松物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
579.4±50.0 °C at 760 mmHg

[ 熔点 ]:
238-240 °C(lit.)

[ 分子式 ]:
C₂₄H₃₁FO₆

[ 分子量 ]:
434.498

[ 闪点 ]:
304.2±30.1 °C

[ 精确质量 ]:
434.210480

[ PSA ]:
100.90000

[ LogP ]:
2.96

[ 外观性状 ]:
白色或近乎于白色结晶粉末

[ 蒸汽压 ]:
0.0±3.6 mmHg at 25°C

[ 折射率 ]:
1.571

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
水溶性：实际上不溶；水溶解度：100 mg/l 25 °C；可溶于：乙醇,丙酮,二噁烷,氯仿

醋酸地塞米松MSDS

详细MSDS(安全技术说明书)

醋酸地塞米松毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TU4050000

CHEMICAL NAME :: Pregna-1,4-diene-3,20-dione, 9-fluoro-11-beta,17,21-trihydroxy-16-alpha-methyl-, acetate

CAS REGISTRY NUMBER :: 1177-87-3

LAST UPDATED :: 199701

DATA ITEMS CITED :: 12

MOLECULAR FORMULA :: C24-H31-F-O6

MOLECULAR WEIGHT :: 434.55

WISWESSER LINE NOTATION :: L E5 B666 OV AHTTT&J A1 BF CQ E1 FV1OV1 FQ G1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1 mg/kg

SEX/DURATION :: female 15-19 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 :: FESTAS Fertility and Sterility. (American Fertility Soc., 608 13th Ave. S, Birmingham, AL 35282) V.1- 1950- Volume(issue)/page/year: 22,735,1971

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 1200 ug/kg

SEX/DURATION :: female 12-13 day(s) after conception

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

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 23,15,1981

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 1200 ug/kg

SEX/DURATION :: female 12-13 day(s) after conception

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

REFERENCE :: DPTHDL Developmental Pharmacology and Therapeutics. (S. Karger Pub., Inc., 79 Fifth Ave., New York, NY 10003) V.1- 1980- Volume(issue)/page/year: 4,89,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 2400 ug/kg

SEX/DURATION :: female 12-13 day(s) after conception

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

REFERENCE :: DPTHDL Developmental Pharmacology and Therapeutics. (S. Karger Pub., Inc., 79 Fifth Ave., New York, NY 10003) V.1- 1980- Volume(issue)/page/year: 4,89,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 12800 ug/kg

SEX/DURATION :: female 9-12 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)

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 :: Subcutaneous

DOSE :: 12800 ug/kg

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

TOXIC EFFECTS :: 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 :: Intravenous

DOSE :: 128 mg/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 - 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 :: Ocular

DOSE :: 1200 ug/kg

SEX/DURATION :: female 10-13 day(s) after conception

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

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 16,175,1977

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Ocular

DOSE :: 6 mg/kg

SEX/DURATION :: female 10-13 day(s) after conception

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

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 16,175,1977

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 6 mg/kg

SEX/DURATION :: female 24-26 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - biochemical and metabolic

REFERENCE :: BCPCA6 Biochemical Pharmacology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.1- 1958- Volume(issue)/page/year: 27,1007,1978

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 9 mg/kg

SEX/DURATION :: female 5-7 day(s) after conception

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

REFERENCE :: BIREBV Biology of Reproduction. (Soc. for the Study of Reproduction, 309 W. Clark St., Champaign, IL 61820) V.1- 1969- Volume(issue)/page/year: 30,544,1984

醋酸地塞米松安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H317

[ 警示性声明 ]:
P280

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

[ 危害码 (欧洲) ]:
Xi:Irritant

[ 风险声明 (欧洲) ]:
R43

[ 安全声明 (欧洲) ]:
S36/37

[ 危险品运输编码 ]:
2811.0

[ WGK德国 ]:
3

[ RTECS号 ]:
TU4050000

[ 危险类别 ]:
6.1

[ 海关编码 ]:
2937229000

醋酸地塞米松合成路线

详细合成路线

醋酸地塞米松上下游产品

醋酸地塞米松上游产品

醋酸地塞米松下游产品

醋酸地塞米松制备

可用16α,17α-环氧孕甾-4-烯-3,11,20-三酮（即16α,17α-环氧-11-酮基黄体酮）经（3-位、20-位酮基）缩酮化、（11-位酮基）还原、消除[9（11）-位脱水形成双键]、（环氧基与甲基溴化镁）加成并水解（形成17α-羟基，16β-甲基）、水解（脱除乙二醇）得17α-羟基-16β-甲基孕甾-4,9（11）-二烯-3,20-二酮，然后经（4、5-位）脱氢（形成双键）、（21-位）碘化、（21-位碘经乙酰氧基）置换，[9（11）-位双键与次溴酸]加成、[9（11）-位]环氧化、9（11）位氟化氢加成后制得该品。

醋酸地塞米松海关

[ 海关编码 ]: 2937229000

醋酸地塞米松文献

Upregulation of nucleoside triphosphate diphosphohydrolase-1 and ecto-5'-nucleotidase in rat hippocampus after repeated low-dose dexamethasone administration.

J. Mol. Neurosci. 55(4) , 959-67, (2015)

Although dexamethasone (DEX), a synthetic glucocorticoid receptor (GR) analog with profound effects on energy metabolism, immune system, and hypothalamic-pituitary-adrenal axis, is widely used therape...

Drug release mechanisms of steroid eluting rings in cardiac pacemaker lead electrodes.

Conf. Proc. IEEE Eng. Med. Biol. Soc. 2012 , 681-4, (2012)

This paper reports on the drug release mechanisms of silicone structures with embedded steroids applied in pacing leads. Different derivatives of the steroid dexamethasone, which is associated with th...

Intra-articular bioactivity of a p38 MAPK inhibitor and development of an extended-release system.

Eur. J. Pharm. Biopharm. 93 , 110-7, (2015)

In the treatment of arthritic diseases, oral or systemic administration of anti-inflammatory substances, such as p38 MAPK inhibitors, is hampered by numerous side effects. To overcome them, formulatio...

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