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1、抗过敏药Antiallergicdrug我在花粉的刺激下脓包成堆Flower?你在春天的花朵里自拍纷飞Content:1.Allergydiseaseandhistamine2.Thedevelopmentofantiallergicdrug3.Newallergymedicine--OlopatadineHydrochloride4.Thechemicalstructure5.Structure-activityrelationship(SAR)6.Studyontoxicityandsideeffect7.Indicati
2、ons8.Syntheticroute9.Prospects10.Howtochoosetheallergymedicine?1.AllergydiseaseandhistamineWhenbodyhasbeenstimulatedbytheantigenicsubstances,itmaybecausethetissuedamageorphysicaldisorders,namelypathologicalimmuneresponsetodiseases.Histamineininflammationandallergicd
3、iseasesplayanimportantroleinphysi-ological,histamineofproinflammatoryandimmuneadjustmentisbythreekind-sofhistamineH1,H2,H3.Histamineisthemostimportantmediumallergicdisease.2.ThedevelopmentofantiallergicdrugAntiallergicdrugsarealsocalledantihistamines,withthecontinuo
4、usdevelopmentofpharmacology,antihistamineshavebeendevelopedtosixcategoriesnearlyhundredkindsofvarieties.ThefirstgenerationofantiallergicdrugThefirstgenerationofhistamineH1receptorantagonisthasstrongcentralnervouscalmingandcholinefightingeffects.Thesecondgenerationof
5、antiallergicdrugTheadvantagesofsecondgenerationantiallergic:(1)betterclinicalcurativeeffect(2)long-termeffect(3)nosideeffecttocentralnervoussystem(4)noresistingcholineeffect(5)eutherapeutictoasthma(6)goodtolerabilitySlightlyCNSeffect:①Sleepiness②headache③whettheappe
6、titeandsideeffecttocardiovascularsystem3.Newallergymedicine--OlopatadineHydrochlorideOlopatadineasanewkindofrelativelyhighselectivityantiallergic,ConcordeFermentationbyJapanlistedcompanydevelopmentandantiallergic,successivelyonthemarketinEurope,America,Japanandother
7、countries.4.Thechemicalstructure11-[(反)-3-二甲胺基丙烯]-6,11-二氢苯骈[b,e]氧杂卓-2-乙酸盐酸Structure-activityrelationship(SAR):1.烯基碳和氮原子间相隔2个碳原子最佳,延长或缩短碳链对H1受体的亲和力减弱;氮原子上以二甲基取代抑制支气管哮喘作用最强,以二乙基取代抑制作用减弱,以吗琳和哌啶取代活性消失。2.分子中梭基是必要的官能团,梭基和二苯骈氧卓环之间以亚甲基相连,抗过敏活性最强,但适当延长或缩短连接基团对H1受体的亲和力变化影响不大。
8、3.二苯骈氧卓环也是必要的,开环化合物失去所有的活性。4.反式异构体比顺式体对H1受体的亲和力强,但它对M1受体亲和力也强,副作用多。6.Studyontoxicityandsideeffect:Preclinicalandclinicalstudieshaveshown:n
