关键词: 塞曲司特, 呋咱氮氧类化合物, 羟基胍类化合物, 抗哮喘, 一氧化氮

Abstract: AIM: To estimate the antiasthmatic activity of new compounds :SDF-1, SDG-1 and SDG-3.F-1 is a furoxan derivative, G-1 and G-3 are hydroxylguanidine derivatives, SDF-1 is a novel seratrodast derivative connected with F-1, SDG-1 a seratrodast derivative connected with G-1, and SDG-3 a novel seratrodast derivative connected with G-3.METHODS: Firstly, the in vivo antiasthmatic activity was estimated in asthmatic guinea pigs induced by acetylcholine and histamine.Secondly, the in vitro NO releasement of these compounds was determined following the procedures of Griess.Finally, tracheal smooth muscle relexant potency of these compounds was evaluated on trachea of guinea pigs.RESULTS: The in vivo antiasthmatic activity of SDF-1 was more potent than seratrodast (P<0.01), and SDG-1 and SDG-3 were slightly more potent than seratrodast (P<0.05).The in vitro NO releasement of SDF-1 and SDG-1 was higher than F-1 and G-1, the original compounds of SDF-1 and SDG-1, while SDG-3 was lower than its original compounds G-3.In the evaluation on trachea contracted by carbcholine, SDF-1 and SDG-1 were more potent than seratrodast, F-1 and G-1 (P<0.01), but SDG-3 only slightly more potent than seratrodast (P<0.01).In the evaluation on trachea contracted by histamine, SDF-1, SDG-1 and SDG-3 were slightly more potent than seratrodast and their original compounds (P<0.01).CONCLUSION: The antiasthmatic activity of new compounds are more potent than seratrodast and their original NO donors.

Key words: seratrodast, furoxan derivatives, NHydroxyguanidine, antiasthma, NO in vitro releasement