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1、抗過(guò)敏藥Antiallergicdrug我在花粉的刺激下膿包成堆Flower?你在春天的花朵里自拍紛飛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]-6,11-二氫苯駢[b,e]氧雜卓-2-乙酸鹽酸Structure-activityrelationship(SAR):1.烯基碳和氮原子間相隔2個(gè)碳原子最佳,延長(zhǎng)或縮短碳鏈對(duì)H1受體的親和力減弱;氮原子上以二甲基取代抑制支氣管哮喘作用最強(qiáng),以二乙基取代抑制作用減弱,以嗎琳和哌啶取代活性消失。2.分子中梭基是必要的官能團(tuán),梭基和二苯駢氧卓環(huán)之間以亞甲基相連,抗過(guò)敏活性最強(qiáng),但適當(dāng)延長(zhǎng)或縮短連接基團(tuán)對(duì)H1受體的親和力變化影響不大。
8、3.二苯駢氧卓環(huán)也是必要的,開(kāi)環(huán)化合物失去所有的活性。4.反式異構(gòu)體比順式體對(duì)H1受體的親和力強(qiáng),但它對(duì)M1受體親和力也強(qiáng),副作用多。6.Studyontoxicityandsideeffect:Preclinicalandclinicalstudieshaveshown:n
