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左羟丙哌嗪

左羟丙哌嗪用途

Levodropropizine (DF-526) 是组胺受体抑制剂。Levodropropizine (DF-526) 是一种有效的, 良好耐受性的镇咳药。

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左羟丙哌嗪名称

[ CAS 号 ]:
99291-25-5

[ 中文名 ]:
左羟丙哌嗪

[ 英文名 ]:
Levodropropizine

[中文别名 ]:

[英文别名 ]:

(S)-dropropizine
Levdropropizina
1,2-Propanediol,3-(4-phenyl-1-piperazinyl)-,(R)
(-)-Dropropizine
rapitux
(+)-Dropropizine
(2S)-3-(4-phenylpiperazin-1-yl)propane-1,2-diol
(R)-3-(4-Phenylpiperazin-1-yl)propane-1,2-diol
Levdropropizina [Latin,Spanish]
(2S)-3-(4-Phenyl-1-piperazinyl)-1,2-propanediol

左羟丙哌嗪生物活性

[ 描述 ]:

Levodropropizine (DF-526) 是组胺受体抑制剂。Levodropropizine (DF-526) 是一种有效的, 良好耐受性的镇咳药。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 炎症/免疫

[参考文献]

[1]. Zanasi A, et al. Levodropropizine for treating cough in adult and children: a meta-analysis of published studies. Multidiscip Respir Med. 2015 May 31;10(1):19.

[相关活性小分子]

左羟丙哌嗪物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
412.7±34.0 °C at 760 mmHg

[ 熔点 ]:
102-106ºC

[ 分子式 ]:
C₁₃H₂₀N₂O₂

[ 分子量 ]:
236.310

[ 闪点 ]:
220.9±24.3 °C

[ 精确质量 ]:
236.152481

[ PSA ]:
46.94000

[ LogP ]:
0.46

[ 外观性状 ]:
白色晶体粉末

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.577

[ 储存条件 ]:
Refrigerator

左羟丙哌嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TZ1075100

CHEMICAL NAME :: 1,2-Propanediol, 3-(4-phenylpiperazin-1-yl)-, S(-)-

CAS REGISTRY NUMBER :: 99291-25-5

LAST UPDATED :: 199609

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C13-H20-N2-O2

MOLECULAR WEIGHT :: 236.35

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 :: 887 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Gastrointestinal - other changes

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 38,1150,1988

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 401 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity)

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 38,1150,1988

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1281 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Gastrointestinal - other changes

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 38,1150,1988

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 408 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity)

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 38,1150,1988

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 2493 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Gastrointestinal - other changes

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 38,1150,1988

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左羟丙哌嗪安全信息

[ 海关编码 ]:
2933599090

左羟丙哌嗪合成路线

详细合成路线

左羟丙哌嗪上下游产品

左羟丙哌嗪上游产品

左羟丙哌嗪下游产品

左羟丙哌嗪海关

[ 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%

左羟丙哌嗪文献

Efficacy and tolerability of levodropropizine and dropropizine in children with non-productive cough.

J. Int. Med. Res. 23(3) , 175-83, (1995)

The antitussive efficacy and tolerability of dropropizine and of its enantiomer levodropropizine were evaluated in children with non-productive cough; 258 were evaluable for tolerability and 254 for e...

Efficacy of levodropropizine in pediatric cough.

Pulm. Pharmacol. Ther. 25(5) , 337-42, (2012)

Cough in children is among the most common problems managed by pediatricians, and occurs more frequently in preschool than in older children. Most acute episodes of cough are due to viral upper respir...

Studies on the human metabolism and the toxicologic detection of the cough suppressant dropropizine in urine using gas chromatography-mass spectrometry.

Ther. Drug Monit. 26(4) , 441-9, (2004)

Studies are described on the metabolism and the toxicologic analysis of the nonopioid cough suppressant dropropizine [R,S-3-(4-phenyl-1-piperazinyl)1,2-propandiol, DRO] in human urine using gas chroma...

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