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甲基泼尼松龙乙丙酸酯

甲基泼尼松龙乙丙酸酯用途

醋酸甲基泼尼松龙(ZK 91588)是一种糖皮质激素和抗炎药,具有微弱的全身效应。乙酰甲泼尼松龙是一种选择性糖皮质激素受体配体。乙酰甲泼尼龙可用于湿疹和其他炎症性皮肤疾病的研究[1][2][3]。

甲基泼尼松龙乙丙酸酯名称

[ CAS 号 ]:
86401-95-8

[ 中文名 ]:
甲基泼尼松龙乙丙酸酯

[ 英文名 ]:
Methylprednisolone aceponate

[中文别名 ]:

[英文别名 ]:

Aceponato de metilprednisolona [Spanish]
Advantan
Methylprednisoloni aceponas [Latin]
SH-440
Aceponate de methylprednisolone [French]
Methylprednisolone aceponate

甲基泼尼松龙乙丙酸酯生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 炎症/免疫

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 糖皮质激素受体

[体外研究]

醋酸甲基泼尼松龙抑制胶原酶启动子活性 (在海拉细胞中)、脂多糖诱导的 IL-12p40分泌 (在人 PBMC公司中) 和植物凝集素诱导的干扰素-γ分泌 (在人 PBMC公司中),集成电路50分别为 9.3、16.8、15.2 nM[3]。醋酸甲基泼尼松龙激活毫米电视启动子和塔特活性,第50周分别为 21.8和 20.5nM[3]

[体内研究]

醋酸甲基泼尼松龙(局部应用, 50μ,巴豆油引起的伊文蓝水肿模型) 具有抗炎作用,国际50为 0.0015%,全身副作用低[1]. 醋酸甲基泼尼松龙(0.0001%-0.1%局部应用) 在小鼠和大鼠的刺激性接触性皮炎中抑制水肿形成,第50版为 0.002%[3]。动物模型：刺激性接触性皮炎小鼠和大鼠[3]剂量：0.0001%-0.1%给药：局部应用,小鼠10µL,大鼠20µL。结果：显著抑制耳道炎症。

[参考文献]

[1]. Ruzicka T. Methylprednisolone aceponate in eczema and other inflammatory skin disorders -- a clinical update. Int J Clin Pract. 2006 Jan;60(1):85-92.

[2]. H.J. Zentel, et al. Preclinical evaluation of a new topical corticosteroid methylprednisolone aceponate. 1994. 3 (s1), S32-S38.

[3]. Schäcke H, et al. Characterization of ZK 245186, a novel, selective glucocorticoid receptor agonist for the topical treatment of inflammatory skin diseases. Br J Pharmacol. 2009 Oct;158(4):1088-103.

甲基泼尼松龙乙丙酸酯物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
595.8±50.0 °C at 760 mmHg

[ 分子式 ]:
C₂₇H₃₆O₇

[ 分子量 ]:
472.570

[ 闪点 ]:
193.1±23.6 °C

[ 精确质量 ]:
472.246094

[ PSA ]:
106.97000

[ LogP ]:
4.01

[ 蒸汽压 ]:
0.0±3.8 mmHg at 25°C

[ 折射率 ]:
1.560

甲基泼尼松龙乙丙酸酯毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TU3686900

CHEMICAL NAME :: Pregna-1,4-diene-3,20-dione, 21-(acetyloxy)-11-hydroxy-6-methyl-17-(1-oxopropoxy)- , (6-alpha,11-beta)-

CAS REGISTRY NUMBER :: 86401-95-8

LAST UPDATED :: 199612

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C27-H36-O7

MOLECULAR WEIGHT :: 472.63

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: Standard Draize test

ROUTE OF EXPOSURE :: Administration onto the skin

SPECIES OBSERVED :: Rodent - rabbit

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 19,3103,1991 ** ACUTE TOXICITY DATA **

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Kidney, Ureter, Bladder - incontinence

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 19,3015,1991

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >3 gm/kg

TOXIC EFFECTS :: Endocrine - other changes

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 19,3015,1991 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 7280 ug/kg/52W-C

TOXIC EFFECTS :: Endocrine - changes in thymus weight Blood - changes in leukocyte (WBC) count Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 19,3039,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3920 ug/kg/14W-C

TOXIC EFFECTS :: Liver - changes in liver weight Endocrine - changes in spleen weight Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 19,3021,1991 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 1620 ug/kg

SEX/DURATION :: male 60 day(s) pre-mating female 2 week(s) pre-mating - 7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Paternal Effects - other effects on male Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Effects on Embryo or Fetus - other effects to embryo

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 19,3063,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 3300 ug/kg

SEX/DURATION :: female 7-17 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 :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 19,3073,1991

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 - Maternal Effects - other effects Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 19,3073,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 27 mg/kg

SEX/DURATION :: female 17-22 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Maternal Effects - parturition Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 19,3089,1991

甲基泼尼松龙乙丙酸酯合成路线

详细合成路线

甲基泼尼松龙乙丙酸酯上下游产品

甲基泼尼松龙乙丙酸酯上游产品

甲基泼尼松龙乙丙酸酯下游产品

甲基泼尼松龙乙丙酸酯制备

甲基泼尼松龙(Ⅰ)和原丙酸三乙酯，在吡啶铺甲苯磺酸盐存在下，在二甲基甲酰胺和苯的混合溶剂中酯化，生成相应的二酯(Ⅱ)。(Ⅱ)和乙酸钠-乙酸在甲醇水溶液中，部分水解，得到丙酸酯(Ⅲ)，最后用乙酐和吡啶进行乙酰化，得到醋丙甲泼尼龙。