胆碱受体激动药Chapter 7

第7章胆碱受体激动药

Chapter7Cholinoceptoragonists第一节

M胆碱受体激动药AcetylcholinereceptoragonistsarechemicalsthatrecognizeanddirectlybindtotheAChRsinthecentralandperipheralnervoussystems.ThesedrugsmimictheeffectsofAChandsocausemuscariniceffectsornicotiniceffectsintheperipheralandcentralnervoussystems.常用胆碱酯类药物乙酰胆碱（acetylcholine,ACh）醋甲胆碱（methacholine）卡巴胆碱（carbachol）贝胆碱（bethanechol）胆碱酯类药物共性季胺基团亲水性强，脂溶性差，不宜口服不易透过血脑屏障主要由乙酰胆碱酯酶水解，难易程度相差大激动M受体为主，空间选择性高，(S)-效能强于(R)-PropertiesofCommonlyUsedCholineEsterscholineestersusceptibilitytocholinesterasemuscarinicactionnicotinicactionacetylcholine++++++++++methacholine+++++nonecarbacholnegligible+++++bethanecholchloridenegligible++none乙酰胆碱(acetylcholine,ACh)药理作用

Bloodvesselsarteriesdilation(viaEDRF).

constriction(high-dosedirecteffect)

Heartsinoatrialnodedecreaseinrate(negativechronotropy)atriadecreaseincontractilestrength(negativeinotropy)

decreaseinrefractoryperiodatrioventricularnodedecreaseinconductionvelocity(negativedromotropy).increaseinrefractoryperiodventriclessmalldecreaseincontractilestrength药理作用：胃肠道、泌尿道gastrointestinaltract

motilityincreasesphinctersrelaxationsecretionstimulationurinarybladderdetrusorcontractiontrigoneandsphincterrelaxation

药理作用：其他glandssweat,salivary,lacrimal,

nasopharyngealsecretionEyesphinctermuscleofiriscontraction(miosis)ciliarymusclecontractionfornearvisionlungbronchialmusclecontraction(bronchoconstriction)bronchialglandsstimulation醋甲胆碱(methacholine)特点水解速度慢，作用时间较ACh长有muscarine样的作用，无nicotine样作用心血管系统作用明显用途口腔黏膜干燥症偶用于支气管高敏性的诊断禁忌证支气管哮喘、甲亢、冠状动脉缺血和溃疡病卡巴胆碱(carbachol)特点不易被AChE水解，作用时间长选择性差，对M