Oxtriphylline
(Synonyms: 胆茶碱,Cholinophylline, Zy 15061) 目录号 : GC44521A choline salt form of theophylline
Cas No.:4499-40-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Oxtriphylline is a choline salt form of theophylline . It dose-dependently decreases histamine-induced contractions of isolated guinea pig trachea and increases cAMP levels in guinea pig tracheal smooth muscle cells in vitro. [1]Formulations containing oxtriphylline were previously used in the treatment of asthma.
Reference:
[1]. Bilcíková, L., Bauer, V., and Kolena, J. The effects of methylxanthines, ethymizol, ephedrine and papaverine on guinea pig and dog trachea. Gen. Physiol. Biophys. 6(2), 137-148 (1987).
| Cas No. | 4499-40-5 | SDF | |
| 别名 | 胆茶碱,Cholinophylline, Zy 15061 | ||
| 化学名 | 2-hydroxy-N,N,N-trimethyl-ethanaminium salt with 3,9-dihydro-1,3-dimethyl-1H-purine-2,6-dione | ||
| Canonical SMILES | CN(C(N1C)=O)C2=C(N=C[N-]2)C1=O.C[N+](CCO)(C)C | ||
| 分子式 | C7H7N4O2•C5H14NO | 分子量 | 283.3 |
| 溶解度 | 10mg/mL in PBS, pH 7.2 | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5298 mL | 17.6491 mL | 35.2983 mL |
| 5 mM | 0.706 mL | 3.5298 mL | 7.0597 mL |
| 10 mM | 0.353 mL | 1.7649 mL | 3.5298 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Study of Oxtriphylline SA in 50 asthmatics
J Asthma 1983;20(3):177-81.PMID:6345499DOI:10.3109/02770908309114941.
Fifty clinically stable patients with asthma on maintenance theophylline therapy, mean dose of 15 mg kg-1 per day, were switched to an equivalent dose (X 1.56) of Oxtriphylline SA for seven doses. All subjects remained clinically stable after the change during the study period. Oxtriphylline SA appears to be useful for the maintenance treatment of asthma and can be safely substituted for other theophylline maintenance regimens.
Pharmacokinetics and taste acceptance of an alcohol-free Oxtriphylline solution
Ann Allergy 1980 Oct;45(4):224-7.PMID:7425393doi
As follow-up to earlier studies done on the pharmacokinetics of theophylline preparations in young children, an alcohol-free Oxtriphylline syrup preparation was studied. Oxtriphylline syrup demonstrated no appreciable change in the pharmacokinetic parameter of half-life in this young age group. Therapeutic dose relationship were studied in conjunction with trough level measurements. Patient acceptance of this preparation is judged to be excellent.
Relation of oral dose of Oxtriphylline to serum theophylline level
Can Med Assoc J 1981 Dec 15;125(12):1336-8.PMID:7034918doi
Serum theophylline levels were studied in relation to oral doses of Oxtriphylline in 30 patients with reversible airway obstruction. A wide scattering of levels was observed and was attributed to widely differing rates of metabolism of the drug. From the data obtained it was concluded that the most commonly prescribed daily dose of Oxtriphylline, 800 mg, will produce a therapeutic level of theophylline in only about one quarter of patients. A daily starting dose of 15 to 20 mg/kg, however, will produce therapeutic levels in approximately one third of patients without significant toxic effects. Once the patient's conditions is stable the serum theophylline concentration should be measured; if it is subtherapeutic the dose of Oxtriphylline should be increased slowly and the serum theophylline concentration remeasured until a level of 10 to 20 microgram/ml is achieved.
Theophylline pharmacokinetics: variations between two similar study populations using oral Oxtriphylline syrup
Ann Allergy 1980 Feb;44(2):67-70.PMID:7362087doi
The pharmacokinetics of two unmatched populations of asthmatic children, one from an asthmatic convalescent center in Denver and the other from an urban outpatient clinic, are compared after single and repeated dosing of a new asthma formulation, Oxtriphylline syrup. Significant differences (p less than 0.05) in populations' theophylline total body clearance, apparent volume of distribution and absorption rates suggest future studies of multiple center design representing patterns of asthma more typical to the population at large would be more appropriate for selection of theophylline dosage guidelines.
Anticholinergic and sympathomimetic combination therapy of asthma
J Allergy Clin Immunol 1983 Mar;71(3):317-23.PMID:6219156DOI:10.1016/0091-6749(83)90086-6.
The role of the anticholinergic drug, ipratropium bromide, in maintenance antiasthmatic therapy was evaluated in a double-blind crossover trial of three bronchodilator regimens: (1) inhaled ipratropium, placebo, and oral Oxtriphylline; (2) inhaled fenoterol, placebo, and oral Oxtriphylline; and (3) both inhaled ipratropium and fenoterol plus oral Oxtriphylline. Twenty-two asthmatics were treated with all three regimens, each for 1 mo, allocated in random sequence. On the first and last treatment days of each month, spirometric measurements were performed before and 0.5, 1, 2, 3, 4, and 6 hr after administration of the test drugs. On the first treatment day of each month, all regimens produced significant bronchodilatation at 30 min after dose, an improvement that declined between 3 and 6 hr after dose. After continuous administration for 1 mo the two combinations employing fenoterol showed a decline in bronchodilator responsiveness from the initial treatment day, measured as the level of response (V50) or duration of response (FEV1, VC). Ipratropium plus Oxtriphylline showed no such decline, suggesting the development of tolerance to long-term administration of fenoterol. Overall benefit at the end of 1 mo, measured as the area under the curves of FEV1, VC, or V50 vs time after dose, was greatest for the triple drug regimen. There were no differences in heart rate, blood pressure response, or side effects among the three treatments. It is concluded that when the anticholinergic drug ipratropium is administered concurrently with an inhaled beta 2 agonist and an oral theophylline derivative, increased bronchodilatation occurs with no detectable additional side effects.