产品说明书

Theophylline

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Chemical Structure| 58-55-9 同义名 : 1,3-Dimethylxanthine;Theo-24;NSC 2066
CAS号 : 58-55-9
货号 : A896968
分子式 : C7H8N4O2
纯度 : 98%
分子量 : 180.164
MDL号 : MFCD00079619
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: 10 mg/mL(55.5 mM),配合低频超声助溶,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

H2O: 5 mg/mL(27.75 mM),配合低频超声助溶

0.1 M NaOH: 20 mg/mL(111.01 mM),配合低频超声,水浴加热至45℃,并调节pH至10

动物实验配方:
生物活性
描述 Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histone deacetylase (HDAC) activator. The apparent suppression of airway inflammation by theophylline in asthmatic patients reinforces data from ill vitro experiments, showing inhibitory actions of theophylline on the pro-inflammatory functions of many immune cells[3]. Theophylline has emerged as a major prophylactic agent for controlling the symptoms of chronic asthma, but it provides little if any relief of pulmonary symptoms caused by irreversible chronic airways obstruction[4]. In addition, several studies in patients with COPD (Chronic obstructive pulmonary disease) have shown that theophylline and inhaled beta-agonists interact in an additive fashion, and the combination therapy results in additional objective and subjective improvement over that achieved by either preparation alone[5]. Intravenous theophyllines are a second line treatment for children suffering an acute exacerbation of asthma[6]. In asthma theophyllines should be considered for chronic stable asthma when treatment with optimal doses of inhaled steroids and bronchodilators fails to provide adequate control; for nocturnal asthma; and for prophylaxis and relief of symptoms in children and adults when inhaled treatment cannot be given. In general, theophyllines cannot be recommended for chronic airflow obstruction[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.55mL

1.11mL

0.56mL

27.75mL

5.55mL

2.78mL

55.50mL

11.10mL

5.55mL

参考文献

[1]Deree J, Martins JO, et al. Insights into the regulation of TNF-alpha production in human mononuclear cells: the effects of non-specific phosphodiesterase inhibition. Clinics (Sao Paulo). 2008 Jun;63(3):321-8.

[2]Marques LJ, Zheng L, et al. Pentoxifylline inhibits TNF-alpha production from human alveolar macrophages. Am J Respir Crit Care Med. 1999 Feb;159(2):508-11.

[3]Rabe KF, Dent G. Theophylline and airway inflammation. Clin Exp Allergy. 1998 Aug;28 Suppl 3:35-41

[4]Hendeles L, Massanari M, Weinberger M. Update on the pharmacodynamics and pharmacokinetics of theophylline. Chest. 1985 Aug;88(2 Suppl):103S-111S

[5]Vaz Fragoso CA, Miller MA. Review of the clinical efficacy of theophylline in the treatment of chronic obstructive pulmonary disease. Am Rev Respir Dis. 1993 Jun;147(6 Pt 2):S40-7

[6]Cooney L, Hawcutt D, Sinha I. The Evidence for Intravenous Theophylline Levels between 10-20mg/L in Children Suffering an Acute Exacerbation of Asthma: A Systematic Review. PLoS One. 2016 Apr 20;11(4):e0153877

[7]Johnston ID. Theophylline in the management of airflow obstruction. 2. Difficult drugs to use, few clinical indications. BMJ. 1990 Apr 7;300(6729):929-31