产品说明书

Proxyphylline

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Chemical Structure| 603-00-9 同义名 : 7-(2-羟丙基)茶碱 ;NSC 163343;Monophylline;Spasmolysin
CAS号 : 603-00-9
货号 : A325694
分子式 : C10H14N4O3
纯度 : 99%
分子量 : 238.243
MDL号 : MFCD00022833
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(440.73 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Proxyphylline is a methylxanthine derivative used as a cardiac stimulant, vasodilator and bronchodilator[1]. Proxyphylline inhibits tracheal PDE-activity and half-maximum relaxation of tracheal smooth muscle is obtained with 100 μg/mL proxyphylline[2]. Proxyphylline exhibits bronchodilatory effect[3]. Proxyphylline inhibits cAMP and cGMP hydrolysis in human lung tissue. The apparent inhibition constant of proxyphylline is 0.06-0.7 mM at low cAMP concentrations and it is 1.0 mM at high cAMP concentrations [4]. In guinea pigs (modified Konzett-Rössler method) the reduction in response to metacholine caused by increasing doses of proxyphylline and salbutamol significantly exceeded that of either drug alone. The combination of oral proxyphylline and salbutamol is clinically useful in increasing drug response without increased adverse effects[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.20mL

0.84mL

0.42mL

20.99mL

4.20mL

2.10mL

41.97mL

8.39mL

4.20mL

参考文献

[1]Takeda K, Katano Y, Nakagawa Y, Tsukada T, Nakazawa M. 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, Pöch G, Holzmann S. Overadditive synergism between theophylline, diprophylline and proxyphylline in tracheal smooth muscle relaxation. Arzneimittelforschung. 1983;33(10):1450-4

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

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

[5]Kanto J, Allonen H, Kulmala T, Mäntylä R, Tala E. Interaction between proxyphylline and salbutamol. Int J Clin Pharmacol Ther Toxicol. 1981 Aug;19(8):346-9