| Description | Doxofylline (Doxophylline) is a methylxanthine derivative with the presence of a dioxolane group in position 7. As a drug used in the treatment of asthma, doxofylline has shown similar efficacy to theophylline but with significantly fewer side effects in animal and human studies. |
| In vitro | 有效治疗剂量下,Doxofylline比茶碱的心脏兴奋作用小,因此Doxofylline不会使心脏频率明显增高,也没有致心律失常的作用.30 mg/kg 的Doxofylline会使麻醉的猫心率增加13 beats/min. |
| In vivo | Doxofylline具有PDE抑制剂的活性,并能增加cAMP的水平,因此可以用于治疗哮喘和慢性阻塞性肺疾病。Doxofylline与茶碱相比,极大地减少对腺苷A1和A2受体的亲和力,这可能使其具有更好的安全性,且Doxofylline不干扰钙离子内流或拮抗钙通道阻滞剂。Doxofylline抑制腺苷诱导气管平滑肌松弛的EC50值比氨茶碱高15倍,且减少腺苷对豚鼠心房负性肌力作用的EC50值比氨茶碱高15倍。 |
| Synonyms | Doxophylline, 多索茶碱 |
| molecular weight | 266.25 |
| Molecular formula | C11H14N4O4 |
| CAS | 69975-86-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (187.79 mM) H2O: 22 mg/mL (82.6 mM) Ethanol: 2 mg/mL (7.51 mM) |
| References | 1. Shukla D, et al. Expert Opin Pharmacother, 2009, 10(14), 2343-2356. 2. Dini FL, et al. Curr Med Res Opin, 2001, 16(4), 258-268. |