盐酸依普拉酮

盐酸依普拉酮用途

Eprazinone dihydrochloride 是一种具有粘液溶解,分泌分解,镇咳和支气管解痉性质的药物。Eprazinone dihydrochloride 是一种神经激肽 1 受体 (NK1R) 的配体。Eprazinone dihydrochloride 可用于慢性支气管炎的研究,可改善肺功能和动脉血氧分压。

盐酸依普拉酮名称

[ CAS 号 ]:
10402-53-6

[ 中文名 ]:
盐酸依普拉酮

[ 英文名 ]:
Eprazinone 2HCl

[中文别名 ]:

氯化胆硷

[英文别名 ]:

UNII:394X1L8I9Y
Eprazinone dihydrochloride
eprazinone di-hcl

盐酸依普拉酮生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 炎症/免疫

信号通路 >> 神经信号通路 >> 神经激肽受体

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 神经激肽受体

[ 靶点 ]

Neurokinin 1 receptor[1]

[体外研究]

尽管在25μM浓度下,依丙嗪酮对[125I]BH-SP与NK1R的结合表现出相当弱的抑制作用,且拮抗作用约为30%,但NK1R阻断可促进其粘溶活性[2]。

[体内研究]

200 mg/kg剂量的Eprazinone(50-200 mg/kg；经口灌胃；每日；连续4天；成年雄性大鼠)显著增加总磷脂和单个磷脂(磷脂酰肌醇除外)水平,降低总中性脂质。低剂量的Eprazinone显著降低中性脂质水平而不影响磷脂[1]。在气道上皮研究中,粘膜加入Eprazinone可引起剂量依赖性的部分可逆性短路电流(Isc)降低。在较低浓度的依丙嗪酮下,Isc的减少完全是由于净氯化物分泌的减少,而在较高浓度下,钠和氯化物的运输都受到影响[1]。动物模型：成年雄性无病原体Fischer 344近交系大鼠(200-250 g)[1]剂量：50 mg/kg、100 mg/kg和200 mg/kg给药：口服灌胃；每日；连续4天结果：200 mg/kg给药可显著提高总和个体(磷脂酰肌醇除外)磷脂水平,降低总中性脂质。

[参考文献]

[1]. R S Thrall, et al. Eprazinone Alters Lung Lavage Lipid Levels and Transtracheal Ion Transport. Exp Lung Res. May-Jun 1992;18(3):409-20.

[2]. Yvonne Krautscheid, et al. Pharmacophore Modeling, Virtual Screening, and in Vitro Testing Reveal Haloperidol, Eprazinone, and Fenbutrazate as Neurokinin Receptors Ligands. J Chem Inf Model. 2014 Jun 23;54(6):1747-57.

盐酸依普拉酮物理化学性质

[ 密度 ]:
1.064 g/cm3

[ 沸点 ]:
503.9ºC at 760 mmHg

[ 分子式 ]:
C₂₄H₃₄Cl₂N₂O₂

[ 分子量 ]:
453.445

[ 闪点 ]:
258.5ºC

[ 精确质量 ]:
452.199738

[ PSA ]:
32.78000

[ LogP ]:
5.38060

[ 外观性状 ]:
一种白色或近乎于白色晶体

[ 蒸汽压 ]:
2.8E-10mmHg at 25°C

[ 储存条件 ]:
2~8℃

盐酸依普拉酮MSDS

详细MSDS(安全技术说明书)

盐酸依普拉酮毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UH1599500

CHEMICAL NAME :: Propiophenone, 2-(4-(beta-ethoxyphenethyl)-1-piperazinyl)methyl-, dihydrochloride

CAS REGISTRY NUMBER :: 10402-53-6

LAST UPDATED :: 199503

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C24-H32-N2-O2.2Cl-H

MOLECULAR WEIGHT :: 453.50

WISWESSER LINE NOTATION :: T6N DNTJ A1Y1&VR& D1YR&O2 &GH 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 763 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,232,1979

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 191 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,232,1979

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 238 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,232,1979

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 286 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,232,1979

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 116 mg/kg

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

REFERENCE :: PCIPDV Beijing Yixueyuan Xuebao. Journal of Peking Medical College. (Beijing Yixueyuan, Beijiaohaidianqu, Beijing, Peop. Rep. China) 19??-V.17(3), 1985. Volume(issue)/page/year: 13(2),98,1981

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 300 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 2,314,1968

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 20 mg/kg

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

REFERENCE :: PCIPDV Beijing Yixueyuan Xuebao. Journal of Peking Medical College. (Beijing Yixueyuan, Beijiaohaidianqu, Beijing, Peop. Rep. China) 19??-V.17(3), 1985. Volume(issue)/page/year: 13(2),98,1981

盐酸依普拉酮安全信息

[ 危害码 (欧洲) ]:
Xi

[ 海关编码 ]:
2933990090

盐酸依普拉酮海关

[ 海关编码 ]: 2933599090

[ 中文概述 ]:
2933599090. 其他结构上有嘧啶环的化合物(包括其他结构上有哌嗪环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%