50-02-2

• 常用中文名：地塞米松
• 常用英文名：Dexamethasone
• CAS号：50-02-2
• 分子式：C₂₂H₂₉FO₅
• 分子量：392.461
• 相关类别： 原料药 激素及调节内分泌功能类药 肾上腺皮质激素类药
• 发布时间：2018-08-01 09:00:24
• 更新时间：2024-01-02 15:51:58
• Dexamethasone 是一种糖皮质激素受体 (glucocorticoid receptor) 激动剂。

名称

• 中文名: 地塞米松
• 英文名: dexamethasone
• 中文别名: 氟美松; 9Α-氟-16Α-甲基氢化泼尼松
• 英文别名: Auxiron; (8S,9R,10S,11S,13S,14S,16R,17R)-9-fluoro-11,17-dihydroxy-17-(hydroxyacetyl)-10,13,16-trimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one; Corson; Hl-dex; (11b,16a)-9-fluoro-11,17,21-trihydroxy-16-methylpregna-1,4-diene-3,20-dione; Adexone; pregna-1,4-diene-3,20-dione, 9-fluoro-11,17,21-trihydroxy-16-methyl-, (11b,16a)-; (8S,9R,10S,11S,13S,14S,16R,17R)-9-Fluor-11,17-dihydroxy-17-(hydroxyacetyl)-10,13,16-trimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-on; Pregna-1,4-diene-3,20-dione, 9-fluoro-11β,17,21-trihydroxy-16α-methyl-; Pregna-1,4-diene-3,20-dione, 9-fluoro-11,17,21-trihydroxy-16-methyl-, (11β,16α)-; 16a-Methyl-9a-fluoroprednisolone; MFCD00064136; Dezone; 16a-Methyl-9a-fluoro-D1-hydrocortisone; Dexamethasone Base; Dexamonozon; Dexone; (11β,16α)-9-Fluoro-11,17,21-trihydroxy-16-methylpregna-1,4-diene-3,20-dione; 1-Dehydro-16a-methyl-9a-fluorohydrocortisone; Dexamethasone; 9α-Fluoro-16α-methylprednisolone; mk125; Dexa-Mamallet; Dexa; 16α-Methyl-9α-fluoroprednisolone; Aphthasolone; EINECS 200-003-9; 9a-Fluoro-16a-methylprednisolone; 16a-Methyl-9a-fluoro-1,4-pregnadiene-11b,17a,21-triol-3,20-dione; 1-Dehydro-16α-methyl-9α-fluorohydrocortisone; Decacort; (8S,9R,10S,11S,13S,14S,16R,17R)-9-Fluoro-17-glycoloyl-11,17-dihydroxy-10,13,16-trimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one; DXM; Dxms; 9-Fluoro-11-β,17,21-trihydroxy-16-α-methylpregna-1,4-diene-3,20-dione

物化性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 568.2±50.0 °C at 760 mmHg
• 熔点: 255-264ºC
• 分子式: C₂₂H₂₉FO₅
• 分子量: 392.461
• 闪点: 297.5±30.1 °C
• 精确质量: 392.199890
• PSA: 94.83000
• LogP: 1.87
• 外观性状: 白色结晶固体
• 蒸汽压: 0.0±3.5 mmHg at 25°C
• 折射率: 1.592
• 储存条件: 2~8°C
• 稳定性:

  地塞米松的化学结构为泼尼松龙的B环9α位引入氟原子，D环16α位引入甲基；9α氟及16α甲基均使其抗炎活性显著增强，而16α甲基则显著地降低了地塞米松的水钠潴留副作用。地塞米松与泼尼松龙的临床生物等效剂量比为0.75:5，生物半衰期为36-54小时，列为长效糖皮质激素。

• 分子结构:

  1、摩尔折射率：100.23

  2、摩尔体积（cm³/mol）：296.2

  3、等张比容（90.2K）：812.3

  4、表面张力（dyne/cm）：56.5

  5、极化率（10-24cm3）：39.73

• 更多:

  1.性状：白色粉末

  2.熔点（℃）：255~264

  3.比旋光度（º,C=1, DIOXANE）：75

  4.溶解性：可溶于水，10mg/100mL，25℃；乙醇，1mg/mL。

生物活性

• 描述: Dexamethasone 是一种糖皮质激素受体 (glucocorticoid receptor) 激动剂。
• 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.

  [5]. Maher HM, et al. Simultaneous determination of selected tyrosine kinase inhibitors with corticosteroids and antiemetics in rat plasma by solid phase extraction and ultra-performance liquid chromatography-tandem mass spectrometry: Application to pharmacokinetic interaction studies. J Pharm Biomed Anal. 2016 May 30;124:216-27.

MSDS

模块1. 化学品 1.1 产品标识符 : 地塞米松 产品名称 1.2 鉴别的其他方法 Prednisolone F 9α-Fluoro-16α-methyl-11β,17α,21-trihydroxy-1,4-pregnadiene-3,20-dione (11β,16α)-9-Fluoro-11,17,21-trihydroxy-16-methylpregna-1,4-diene-3,20-dione 9α-Fluoro-16α-methylprednisolone 1.3 有关的确定了的物质或混合物的用途和建议不适合的用途 仅用于研发。不作为药品、家庭或其它用途。 上述信息视为正确，但不包含所有的信息，仅作为指引使用。本文件中的信息是基于我们目前所知，就正 确的安全提示来说适用于本品。该信息不代表对此产品性质的保证。 参见发票或包装条的反面。 模块2. 危险性概述 2.1 GHS-分类 急性毒性, 经口 (类别 5) 皮肤刺激 (类别 2) 眼睛刺激 (类别 2A) 呼吸过敏 (类别 1) 皮肤过敏 (类别 1) 特异性靶器官系统毒性（一次接触） (类别 3) 2.2 GHS 标记要素，包括预防性的陈述 象形图 警示词危险 危险申明 H303吞咽可能有害。 H315造成皮肤刺激。 H317可能导致皮肤过敏反应。 H319造成严重眼刺激。 H334吸入可能导致过敏或哮喘病症状或呼吸困难。 H335可能引起呼吸道刺激。 警告申明 预防措施 P261避免吸入粉尘/烟/气体/烟雾/蒸气/喷雾. P264操作后彻底清洁皮肤。 P271只能在室外或通风良好之处使用。 P272禁止将污染的工作服带出作业场所。 P280穿戴防护手套/ 眼保护罩/ 面部保护罩。 P285如通风不良，须戴呼吸防护设备。 事故响应 P302 + P352如果皮肤接触：用大量肥皂和水清洗。 P304 + P340如吸入: 将患者移到新鲜空气处休息，并保持呼吸舒畅的姿势。 P305 + P351 + P338如与眼睛接触，用水缓慢温和地冲洗几分钟。如戴隐形眼镜并可方便地取 出，取出隐形眼镜，然后继续冲洗. P321具体处置（见本标签上提供的急救指导）。 P333 + P313如出现皮肤刺激或皮疹：求医/就诊。 P337 + P313如仍觉眼睛刺激：求医/就诊。 P342 + P311如有呼吸系统病症：呼叫解毒中心或医生。 P362脱掉沾污的衣服，清洗后方可再用。 安全储存 P403 + P233存放于通风良的地方。 保持容器密闭。 P405存放处须加锁。 废弃处置 P501将内容物/ 容器处理到得到批准的废物处理厂。 2.3 其它危害物 - 无 模块3. 成分/组成信息 3.1 物 质 : Prednisolone F 别名 9α-Fluoro-16α-methyl-11β,17α,21-trihydroxy-1,4-pregnadiene-3,20-dione (11β,16α)-9-Fluoro-11,17,21-trihydroxy-16-methylpregna-1,4-diene-3,20- dione 9α-Fluoro-16α-methylprednisolone : C22H29FO5 分子式 : 392.46 g/mol 分子量 组分浓度或浓度范围 Dexamethasone <=100% 化学文摘登记号(CAS50-02-2 No.)200-003-9 EC-编号 模块4. 急救措施 4.1 必要的急救措施描述 一般的建议 请教医生。 向到现场的医生出示此安全技术说明书。 吸入 如果吸入,请将患者移到新鲜空气处。 如呼吸停止,进行人工呼吸。 请教医生。 皮肤接触 用肥皂和大量的水冲洗。 请教医生。 眼睛接触 用水冲洗眼睛作为预防措施。 食入 切勿给失去知觉者通过口喂任何东西。 用水漱口。 请教医生。 4.2 主要症状和影响，急性和迟发效应 据我们所知，此化学，物理和毒性性质尚未经完整的研究。, 胎儿发育, 视力模糊, 尿频, 恶心, 呕吐, 食欲改变, 胃/肠功能紊乱, 神经过敏, 睡眠紊乱, 增重, 头晕, 面部潮红, 头痛, 发汗, 过敏反应, 长期或频繁接触会导致：, 痤疮, 皮肤病, 骨痛, 红眼, 眼睛感光过敏, 催泪。, 高血压, 月经紊乱, 肌肉无力, 局部水肿, 不规则心率, 肌肉痉挛, 肌肉痛, 疲倦, 虚弱, 失眠, 背痛, 腿部疼痛, 腹痛, 大便带血 4.3 及时的医疗处理和所需的特殊处理的说明和指示 无数据资料 模块5. 消防措施 5.1 灭火介质 灭火方法及灭火剂 用水雾,抗乙醇泡沫,干粉或二氧化碳灭火。 5.2 源于此物质或混合物的特别的危害 碳氧化物, 氟化氢 5.3 给消防员的建议 如必要的话,戴自给式呼吸器去救火。 5.4 进一步信息 无数据资料 模块6. 泄露应急处理 6.1 作业人员防护措施、防护装备和应急处置程序 使用个人防护用品。 避免粉尘生成。 避免吸入蒸气、烟雾或气体。 保证充分的通风。 避免吸入粉尘。 6.2 环境保护措施 不要让产品进入下水道。 6.3 泄漏化学品的收容、清除方法及所使用的处置材料 收集和处置时不要产生粉尘。 扫掉和铲掉。 放入合适的封闭的容器中待处理。 6.4 参考其他部分 丢弃处理请参阅第13节。 模块7. 操作处置与储存 7.1 安全操作的注意事项 避免接触皮肤和眼睛。 避免形成粉尘和气溶胶。 在有粉尘生成的地方,提供合适的排风设备。 7.2 安全储存的条件,包括任何不兼容性 避光。 贮存在阴凉处。 使容器保持密闭，储存在干燥通风处。 建议的贮存温度： 2 - 8 °C 对光线敏感 7.3 特定用途 无数据资料 模块8. 接触控制和个体防护 8.1 容许浓度 最高容许浓度 没有已知的国家规定的暴露极限。 8.2 暴露控制 适当的技术控制 根据良好的工业卫生和安全规范进行操作。 休息前和工作结束时洗手。 个体防护设备 眼/面保护 面罩與安全眼鏡请使用经官方标准如NIOSH (美国) 或 EN 166(欧盟) 检测与批准的设备防护眼部。 皮肤保护 戴手套取 手套在使用前必须受检查。 请使用合适的方法脱除手套(不要接触手套外部表面),避免任何皮肤部位接触此产品. 使用后请将被污染过的手套根据相关法律法规和有效的实验室规章程序谨慎处理. 请清洗并吹干双手 所选择的保护手套必须符合EU的89/686/EEC规定和从它衍生出来的EN 376标准。 完全接触 物料: 丁腈橡胶 最小的层厚度 0.11 mm 溶剂渗透时间: 480 min 测试过的物质Dermatril® (KCL 740 / Z677272, 规格 M) 飞溅保护 物料: 丁腈橡胶 最小的层厚度 0.11 mm 溶剂渗透时间: 480 min 测试过的物质Dermatril® (KCL 740 / Z677272, 规格 M) , 测试方法 EN374 如果以溶剂形式应用或与其它物质混合应用，或在不同于EN 374规定的条件下应用，请与EC批准的手套的供应商联系。 这个推荐只是建议性的,并且务必让熟悉我们客户计划使用的特定情况的工业卫生学专家评估确认才可. 这不应该解释为在提供对任何特定使用情况方法的批准. 身体保护 全套防化学试剂工作服, 防护设备的类型必须根据特定工作场所中的危险物的浓度和数量来选择。 呼吸系统防护 如须暴露于有害环境中,请使用P95型(美国)或P1型(欧盟 英国 143)防微粒呼吸器。如需更高级别防护,请使用OV/AG/P99型(美国)或ABEK-P2型 (欧盟 英国 143) 防毒罐。 呼吸器使用经过测试并通过政府标准如NIOSH（US）或CEN（EU）的呼吸器和零件。 模块9. 理化特性 9.1 基本的理化特性的信息 a) 外观与性状 形状: 粉末 b) 气味 无数据资料 c) 气味阈值 无数据资料 d) pH值 无数据资料 e) 熔点/凝固点 熔点/凝固点: 262 - 264 °C f) 沸点、初沸点和沸程 无数据资料 g) 闪点 无数据资料 h) 蒸发速率 无数据资料 i) 易燃性(固体,气体) 无数据资料 j) 高的/低的燃烧性或爆炸性限度 无数据资料 k) 蒸气压 无数据资料 l) 蒸汽密度 无数据资料 m) 密度/相对密度 无数据资料 n) 水溶性 无数据资料 o) n-辛醇/水分配系数 无数据资料 p) 自燃温度 无数据资料 q) 分解温度 无数据资料 r) 粘度 无数据资料 模块10. 稳定性和反应活性 10.1 反应性 无数据资料 10.2 稳定性 无数据资料 10.3 危险反应 无数据资料 10.4 应避免的条件 发光。 10.5 不相容的物质 强氧化剂 10.6 危险的分解产物 其它分解产物 - 无数据资料 模块11. 毒理学资料 11.1 毒理学影响的信息 急性毒性 半数致死剂量 (LD50) 经口 - 大鼠 - > 3,000 mg/kg 皮肤刺激或腐蚀 无数据资料 眼睛刺激或腐蚀 无数据资料 呼吸道或皮肤过敏 吸入可引起过敏。 接触皮肤可引起过敏。 生殖细胞致突变性 无数据资料 致癌性 IARC: 此产品中没有大于或等于 0。1%含量的组分被 IARC鉴别为可能的或肯定的人类致癌物。 生殖毒性 无数据资料 特异性靶器官系统毒性（一次接触） 吸入 - 可能引起呼吸道刺激。 无数据资料 特异性靶器官系统毒性（反复接触） 无数据资料 吸入危险 无数据资料 潜在的健康影响 吸入吸入可能有害。 可能引起呼吸道刺激。 摄入如服入是有害的。 皮肤通过皮肤吸收可能有害。 可能引起皮肤刺激。 眼睛可能引起眼睛刺激。 接触后的征兆和症状 据我们所知，此化学，物理和毒性性质尚未经完整的研究。, 胎儿发育, 视力模糊, 尿频, 恶心, 呕吐, 食欲改变, 胃/肠功能紊乱, 神经过敏, 睡眠紊乱, 增重, 头晕, 面部潮红, 头痛, 发汗, 过敏反应, 长期或频繁接触会导致：, 痤疮, 皮肤病, 骨痛, 红眼, 眼睛感光过敏, 催泪。, 高血压, 月经紊乱, 肌肉无力, 局部水肿, 不规则心率, 肌肉痉挛, 肌肉痛, 疲倦, 虚弱, 失眠, 背痛, 腿部疼痛, 腹痛, 大便带血 附加说明 化学物质毒性作用登记: TU3980000 模块12. 生态学资料 12.1 生态毒性 无数据资料 12.2 持久性和降解性 无数据资料 12.3 潜在的生物累积性 无数据资料 12.4 土壤中的迁移性 无数据资料 12.5 PBT 和 vPvB的结果评价 无数据资料 12.6 其它不良影响 无数据资料 模块13. 废弃处置 13.1 废物处理方法 产品 将剩余的和不可回收的溶液交给有许可证的公司处理。 与易燃溶剂相溶或者相混合，在备有燃烧后处理和洗刷作用的化学焚化炉中燃烧 受污染的容器和包装 按未用产品处置。 模块14. 运输信息 14.1 联合国危险货物编号 欧洲陆运危规: -国际海运危规: -国际空运危规: - 14.2 联合国运输名称 欧洲陆运危规: 非危险货物 国际海运危规: 非危险货物 国际空运危规: 非危险货物 14.3 运输危险类别 欧洲陆运危规: -国际海运危规: -国际空运危规: - 14.4 包裹组 欧洲陆运危规: -国际海运危规: -国际空运危规: - 14.5 环境危险 欧洲陆运危规: 否国际海运危规国际空运危规: 否 海洋污染物（是/否）: 否 14.6 对使用者的特别提醒 无数据资料 模块 15 - 法规信息 N/A 模块16 - 其他信息 N/A

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : TU3980000 CHEMICAL NAME : Pregna-1,4-diene-3,20-dione, 9-fluoro-11-beta,17,21-trihydroxy-16-alpha-methyl- CAS REGISTRY NUMBER : 50-02-2 LAST UPDATED : 199806 DATA ITEMS CITED : 85 MOLECULAR FORMULA : C22-H29-F-O5 MOLECULAR WEIGHT : 392.51 WISWESSER LINE NOTATION : L E5 B666 OV KU MUTJ A1 BF CQ E1 FV1Q FQ G1 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Multiple routes SPECIES OBSERVED : Human - woman DOSE/DURATION : 4759 ug/kg/18D-I TOXIC EFFECTS : Kidney, Ureter, Bladder - urine volume increased TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >3 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 54 mg/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - lacrimation Gastrointestinal - hypermotility, diarrhea Skin and Appendages - hair TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 14 mg/kg TOXIC EFFECTS : Nutritional and Gross Metabolic - weight loss or decreased weight gain TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 410 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 4400 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 7200 ug/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - lacrimation Gastrointestinal - hypermotility, diarrhea TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 70 mg/kg/14D-I TOXIC EFFECTS : Endocrine - changes in spleen weight Endocrine - changes in thymus weight Immunological Including Allergic - decrease in cellular immune response TYPE OF TEST : TCLo - Lowest published toxic concentration ROUTE OF EXPOSURE : Inhalation SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 26700 ug/m3/30M/21D-I TOXIC EFFECTS : Endocrine - other changes Endocrine - changes in thymus weight Blood - changes in erythrocyte (RBC) count TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Administration onto the skin SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 7500 ug/kg/30D-I TOXIC EFFECTS : Endocrine - changes in thymus weight Nutritional and Gross Metabolic - weight loss or decreased weight gain Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 3 mg/kg/14D-I TOXIC EFFECTS : Endocrine - changes in thymus weight Blood - changes in leukocyte (WBC) count Immunological Including Allergic - hypersensitivity delayed TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 250 ug/kg/26W-I TOXIC EFFECTS : Endocrine - other changes Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Related to Chronic Data - changes in testicular weight TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 280 ug/kg/28D-I TOXIC EFFECTS : Endocrine - changes in adrenal weight Endocrine - changes in spleen weight Nutritional and Gross Metabolic - weight loss or decreased weight gain TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 3821 ug/kg/14D-C TOXIC EFFECTS : Endocrine - changes in spleen weight Endocrine - changes in thymus weight Blood - other changes TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 6 mg/kg SEX/DURATION : female 8-13 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system 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 - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 880 ug/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 8800 ug/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Effects on Embryo or Fetus - other effects to embryo TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 7500 ug/kg SEX/DURATION : female 15-17 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - body wall TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 8800 ug/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - parturition Reproductive - Effects on Newborn - live birth index (measured after birth) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Administration onto the skin DOSE : 4200 ug/kg SEX/DURATION : male 9 week(s) pre-mating female 2 week(s) pre-mating - 7 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 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Administration onto the skin DOSE : 1802 ug/kg SEX/DURATION : male 26 week(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 1500 ug/kg SEX/DURATION : female 17-19 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - respiratory system TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 5 mg/kg SEX/DURATION : female 14-18 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - biochemical and metabolic TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 3 mg/kg SEX/DURATION : female 14-15 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - biochemical and metabolic TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 2 mg/kg SEX/DURATION : female 20 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - respiratory system TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 1500 ug/kg SEX/DURATION : female 16 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - other effects to embryo TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 3 mg/kg SEX/DURATION : male 3 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - other effects on male TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 700 ug/kg SEX/DURATION : female 12-18 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - endocrine system TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 900 ug/kg SEX/DURATION : female 8-16 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - musculoskeletal system TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 1100 ug/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 3600 ug/kg SEX/DURATION : female 8-16 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord) Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 11 mg/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - body wall Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 1500 ug/kg SEX/DURATION : female 16-20 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - cytological changes (including somatic cell genetic material) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - endocrine system TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Parenteral DOSE : 1500 ug/kg SEX/DURATION : female 16 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - other effects to embryo Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - physical TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 5 mg/kg SEX/DURATION : female 6-15 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 3600 ug/kg SEX/DURATION : female 7-15 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 28800 ug/kg SEX/DURATION : female 7-15 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous 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 - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - musculoskeletal system TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 400 ug/kg SEX/DURATION : female 6-15 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular DOSE : 50 mg/kg SEX/DURATION : female 13 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - skin and skin appendages 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) 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 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Parenteral DOSE : 6 mg/kg SEX/DURATION : female 16 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Parenteral DOSE : 400 ug/kg SEX/DURATION : female 16 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - respiratory system TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intratesticular DOSE : 18 mg/kg SEX/DURATION : male 1 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - testes, epididymis, sperm duct TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular DOSE : 3700 mg/kg SEX/DURATION : female 18-23 week(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - parturition Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - physical TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 400 ug/kg SEX/DURATION : female 13-16 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 2 mg/kg SEX/DURATION : female 13-16 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetal death TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 130 ug/kg SEX/DURATION : female 6-18 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 390 ug/kg SEX/DURATION : female 6-18 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular DOSE : 1600 ug/kg SEX/DURATION : female 25-26 day(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - parturition TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Ocular DOSE : 554 ug/kg SEX/DURATION : female 6-18 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - gastrointestinal system Reproductive - Specific Developmental Abnormalities - urogenital system Reproductive - Specific Developmental Abnormalities - other developmental abnormalities TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Parenteral DOSE : 2 mg/kg SEX/DURATION : female 25-26 day(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - parturition TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Parenteral DOSE : 360 ug/kg SEX/DURATION : female 25-27 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - endocrine system Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular DOSE : 6667 ug/kg SEX/DURATION : female 14 week(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - parturition Reproductive - Specific Developmental Abnormalities - blood and lymphatic systems (including spleen and marrow) Reproductive - Specific Developmental Abnormalities - urogenital system TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Parenteral DOSE : 6670 ug/kg SEX/DURATION : female 14 week(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - parturition TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Parenteral DOSE : 3750 ug/kg SEX/DURATION : female 14 week(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - parturition Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular DOSE : 4 mg/kg SEX/DURATION : female 11 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) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular DOSE : 1905 ug/kg SEX/DURATION : female 45 week(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - parturition TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular DOSE : 800 ug/kg SEX/DURATION : female 45-46 week(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - parturition Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular DOSE : 120 ug/kg SEX/DURATION : female 40 week(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - parturition Reproductive - Effects on Newborn - other postnatal measures or effects TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular DOSE : 60 ug/kg SEX/DURATION : female 39 week(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - immune and reticuloendothelial system TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Parenteral DOSE : 889 ug/kg SEX/DURATION : female 45-46 week(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - parturition Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 877 mg/kg SEX/DURATION : male 20 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - testes, epididymis, sperm duct TYPE OF TEST : Micronucleus test TYPE OF TEST : DNA inhibition TYPE OF TEST : Mutation test systems - not otherwise specified TYPE OF TEST : Sister chromatid exchange MUTATION DATA TYPE OF TEST : DNA inhibition TEST SYSTEM : Bird - chicken Embryo DOSE/DURATION : 150 pmol/L REFERENCE : NATUAS Nature. (Nature Subscription Dept., POB 1018, Manasguan, NJ 08736) V.1- 1869- Volume(issue)/page/year: 257,804,1975 *** REVIEWS *** TOXICOLOGY REVIEW AJOGAH American Journal of Obstetrics and Gynecology. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63146) V.1- 1920- Volume(issue)/page/year: 96,985,1966 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 81600 No. of Facilities: 862 (estimated) No. of Industries: 2 No. of Occupations: 2 No. of Employees: 1035 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X1854 No. of Facilities: 403 (estimated) No. of Industries: 1 No. of Occupations: 5 No. of Employees: 4029 (estimated) No. of Female Employees: 2015 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 81600 No. of Facilities: 728 (estimated) No. of Industries: 4 No. of Occupations: 20 No. of Employees: 30657 (estimated) No. of Female Employees: 17738 (estimated)

安全

• 符号: GHS07, GHS08
• 信号词: Danger
• 危害声明: H315-H317-H319-H334-H335
• 警示性声明: P261-P280-P305 + P351 + P338-P342 + P311
• 个人防护装备: dust mask type N95 (US);Eyeshields;Faceshields;Gloves
• 危害码 (欧洲): Xn:Harmful
• 风险声明 (欧洲): R40
• 安全声明 (欧洲): S45
• 危险品运输编码: NONH for all modes of transport
• WGK德国: 2
• RTECS号: TU3980000
• 海关编码: 2937210000

合成路线

1966-25-2 ~% 50-02-2

文献：Crowe, D. F.; Christie, P. H.; DeGraw, J. I.; Fujiwara, A. N.; Grange, E.; et al. Tetrahedron, 1983 , vol. 39, # 19 p. 3083 - 3090

1177-87-3 ~5% 50-02-2

文献：Holland, Herbert L. Steroids, 1995 , vol. 60, # 9 p. 646 - 649

13209-41-1 ~% 50-02-2

文献：Crowe, D. F.; Christie, P. H.; DeGraw, J. I.; Fujiwara, A. N.; Grange, E.; et al. Tetrahedron, 1983 , vol. 39, # 19 p. 3083 - 3090

14518-56-0 ~% 50-02-2

文献：Crowe, D. F.; Christie, P. H.; DeGraw, J. I.; Fujiwara, A. N.; Grange, E.; et al. Tetrahedron, 1983 , vol. 39, # 19 p. 3083 - 3090

88509-22-2 ~% 50-02-2

文献：Crowe, D. F.; Christie, P. H.; DeGraw, J. I.; Fujiwara, A. N.; Grange, E.; et al. Tetrahedron, 1983 , vol. 39, # 19 p. 3083 - 3090

88509-18-6 ~% 50-02-2

文献：Crowe, D. F.; Christie, P. H.; DeGraw, J. I.; Fujiwara, A. N.; Grange, E.; et al. Tetrahedron, 1983 , vol. 39, # 19 p. 3083 - 3090

80163-63-9 ~% 50-02-2

文献：Crowe, D. F.; Christie, P. H.; DeGraw, J. I.; Fujiwara, A. N.; Grange, E.; et al. Tetrahedron, 1983 , vol. 39, # 19 p. 3083 - 3090

上下游产品

上游产品  3
1177-87-3 13209-41-1 80163-63-9
下游产品  6
382-67-2 312-93-6 1880-61-1 282092-82-4
282092-83-5 37927-01-8

制备

一种新的地塞米松21-羟基物的生产工艺方法，以中间体21-醋酸酯为底物，以含0～10％氯仿的适量甲醇作为溶剂对底物进行半溶，用碱作为催化剂进行水解反应，反应完全后用醋酸中和，将反应液减压浓缩至适量体积，降温，过滤，用水冲洗滤饼，干燥得21-羟基物。该工艺可缩短生产周期，提高21-羟基物的质量和收率，减少21-羟基物中杂质的含量。

海关

海关编码	2937210000