Doxofylline 是腺苷 A1 受体拮抗剂，且能抑制磷酸二酯酶 IV，用于治疗哮喘。

Doxofylline 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.

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.

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。

69975-86-6

C11H14N4O4

266.257

Doxophylline;多索茶碱

H2O:22 mg/mL (82.6 mM)
Ethanol:2 mg/mL (7.51 mM)
DMSO:49 mg/mL (184 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years