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7-(2-羟丙基)茶碱

7-(2-羟丙基)茶碱用途

Proxyphylline是一种甲基黄嘌呤衍生物,临床上作为心脏兴奋剂,血管扩张剂和支气管扩张剂使用。

7-(2-羟丙基)茶碱名称

[ CAS 号 ]:
603-00-9

[ 中文名 ]:
羟丙茶碱

[ 英文名 ]:
Proxyphylline

[中文别名 ]:

[英文别名 ]:

MFCD00022833
7-(2-hydroxypropyl)-1,3-dimethylpurine-2,6-dione
(1,3-Dimethyl-7-[2-hydroxypropyl]-2,6-dioxopurine)
EINECS 210-028-7
Proxyphylline
7-(2-Hydroxypropyl)theophylline

7-(2-羟丙基)茶碱生物活性

[ 描述 ]:

Proxyphylline是一种甲基黄嘌呤衍生物,临床上作为心脏兴奋剂,血管扩张剂和支气管扩张剂使用。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 腺苷受体

研究领域 >> 心血管疾病

[体外研究]

Proxyphylline已显示出血管扩张和心脏刺激作用。 Proxyphylline产生与确定的正性肌力作用相关的冠状动脉血流增加[1]。 Proxyphylline抑制气管PDE活性,100μg/ mL代谢茶碱可获得气管平滑肌的半最大松弛[2]

[体内研究]

在一项双盲交叉研究中,proxyphylline表现出支气管扩张作用[3]。 Proxyphylline抑制人肺组织中的cAMP和cGMP水解。在低cAMP浓度下,代谢茶碱的表观抑制常数为0.06-0.7mM,在高cAMP浓度下为1.0mM [3]。

[参考文献]

[1]. Takeda K, et al. Effects of aminophylline, proxyphylline and a proxyphylline-Melilotus extract-rutin mixture(theoesberiven) on the heart and the coronary circulation. Jpn J Pharmacol. 1977 Oct;27(5):709-20.

[2]. Kukovetz WR, et al. Overadditive synergism between theophylline, diprophylline and proxyphylline in tracheal smooth muscle relaxation. Arzneimittelforschung. 1983;33(10):1450-4.

[3]. Rasmussen FV, et al. Pharmacokinetics and bronchodilatory effect of proxyphylline and theophylline. Eur J Respir Dis. 1984 Jan;65(1):20-7.

[4]. Selvig K, et al. Inhibition of human lung cyclic nucleotide phosphodiesterases by proxyphylline, theophylline and their metabolites. Acta Pharmacol Toxicol (Copenh). 1982 Sep;51(3):250-2.

[相关活性小分子]

7-(2-羟丙基)茶碱物理化学性质

[ 密度 ]:
1.46 g/cm3

[ 沸点 ]:
487.2ºC

[ 熔点 ]:
134-136ºC

[ 分子式 ]:
C₁₀H₁₄N₄O₃

[ 分子量 ]:
238.24300

[ 闪点 ]:
248.5ºC

[ 精确质量 ]:
238.10700

[ PSA ]:
82.05000

[ 外观性状 ]:
固体;White to Almost white powder to crystal

[ 折射率 ]:
1.664

[ 储存条件 ]:
Refrigerator

[ 水溶解性 ]:
水溶性：完全溶解；可溶于：乙醇；微溶：丙酮；极微溶：乙醚

7-(2-羟丙基)茶碱MSDS

7-(2-羟丙基)茶碱毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XH5907500

CHEMICAL NAME :: Theophylline, 7-(2-hydroxypropyl)-

CAS REGISTRY NUMBER :: 603-00-9

LAST UPDATED :: 199806

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C10-H14-N4-O3

MOLECULAR WEIGHT :: 238.28

WISWESSER LINE NOTATION :: T56 BN DN FNVNVJ B1YQ1 F1 H1

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 :: 460 mg/kg

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 19,845,1980

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 445 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,720,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 430 mg/kg

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 19,845,1980

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 739 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,1178,1995

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 505 mg/kg

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

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 27,14,1977

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 410 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 6,601,1956

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 475 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,1178,1995

7-(2-羟丙基)茶碱安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22

[ 安全声明 (欧洲) ]:
36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
XH5907500

[ 海关编码 ]:
2939590000

7-(2-羟丙基)茶碱合成路线

7-(2-羟丙基)茶碱上下游产品

7-(2-羟丙基)茶碱上游产品

7-(2-羟丙基)茶碱下游产品

7-(2-羟丙基)茶碱海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 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 ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

7-(2-羟丙基)茶碱文献

Endocrine regulation of airway contractility is overlooked.

J. Endocrinol. 222(2) , R61-73, (2014)

Asthma is a prevalent respiratory disorder triggered by a variety of inhaled environmental factors, such as allergens, viruses, and pollutants. Asthma is characterized by an elevated activation of the...

High-performance liquid chromatographic determination of (R)-and (S)-proxyphylline in human plasma.

J. Chromatogr. A. 491(2) , 355-66, (1989)

A reversed-phase high-performance liquid chromatographic assay has been developed for determination of (R)-(--)-and (S)-(+)-proxyphylline in human plasma. The procedure is based on liquid-solid extrac...

Acute intoxication with theophylline, proxyphylline and diprophylline in a 3-month-old infant after rectal application: pharmacokinetic data under hemoperfusion.

Acta Paediatr. Scand. 79(1) , 112-4, (1990)

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