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茶碱广泛用于慢性哮喘,但临床效果变化不定,最佳血药浓度范围太窄(10～20μg/ml),如血药浓度过高则出现CNS和心血管兴奋作用.本文报道为克服此缺点而合成的新化合物1-甲基-3-异丁基-8-{2-乙基-〔1一(4-二苯甲基哌嗪基)〕}-3,7-二氢(1H)嘌呤-2,6-二酮(代号S9795)的药理作用特征.试验项目有抗支气管收缩活性,包括对抗组织胺等介质引起的支气管痉挛,S9795的作用强度比氨茶碱高10倍.防治抗原气溶胶引起的实验性哮喘.S9795比茶碱作用强20倍,它可减少狗自主呼吸阻力,对心血管功能无明显影响,它可对抗吸入组胺引起的呼吸阻力增加,而不对抗组织胺引起的全身性降低血压作
Theophylline is widely used in chronic asthma, but the clinical effect of variable, the optimal range of plasma concentration is too narrow (10 ~ 20μg / ml), such as the blood concentration is too high CNS and cardiovascular excitement reported in this paper to overcome this The novel compound 1-methyl-3-isobutyl-8- {2-ethyl- [1-benzodiazepine]}} ) Purine-2,6-dione (code name S9795) pharmacological effects of the pilot project has anti-bronchoconstriction activity, including the fight against histamine and other media-induced bronchospasm, the role of S9795 intensity than aminophylline 10 times. Antigenic aerosols caused by experimental asthma.S9795 20 times stronger than the theophylline, it can reduce the dogs spontaneous respiratory resistance, no significant effect on cardiovascular function, it can resist inhalation of histamine caused by respiratory resistance increased, without resistance to tissue Amine-induced systemic hypotension