动物专用抗原虫药咪哇苯脉研究进展赵蕾蕾1,杨娟1,刘义明1,李鹏飞2,王中杰3,苏丹3,李秀波1(1.中国农业科学院饲料研究所,北京100081;2.中国兽医药品监察所,北京100081;3.中国农业大学,北京100193)摘要:咪IL坐苯服是一种具有11好治疗和预防作用的动物专用抗原虫药。文章综述了其理化性质、抗原虫机理、药代动力学、毒性、残留和临床应用等方血的研究进展,旨在为其在兽医临床的合理使用提供理论依据。关键词:咪I座苯脉;抗原虫;药代动力学;毒性;残留;临床应用:S859.79文献标识码:B:1671—7236(2012)02—0151—05ResearchProgressinAnimal—specificAntiprotozoalDrugImidocarbZHAOLei—lei1,YANGJuanl,LIUYi—min91,LIPeng—tei2,WANGZhong—激e3,SUDan3,LIXiu—bOl(KeyLaboratoryofVeterinaryPharmaceuticalDevelopment,MinistryofAgriculture,EngineeringTechnologyResearchCenterofTraditionalChineseVeterinaryMedicineofGansuProvince.LanzhouInstituteofHusbandryandPharmaceuticalSciencesofCAAS,Lanzhou730050,China)Abstract:ToscreenChinesemateriamedicaforpreventionandcureembryoimplantationdysfunction,mousemodelwithembryoimplantationdysfunctionwasestablishedbyinjectedsubcutaneouslywithmifepristoneplexprescriptioncomposedofsuchChinesemateriamedicaasSalviamiltiorrhiza.Radixastragali,Szechwanlovagerhizome.RadixScutellariae,Rhizomaatractylodismacrocephalae,Semencuscutae,Herbataxilli.Radixdipsaci,RadixcodonopsisoRadixangelicaesinensisandsomeofthemwereevaluatedinthemodel,pregnancyrate(PR),numberofembryoimplantation,progestin(P‘),estradiol(E2)andratioofprogestintOestradiol(P4/E2)werethemainindex.TheresultsofthescreentestshowedthatPRwassignificantlyhigherinprescriptionsgroupthanthatinprescription1group,Semencu$cutaegroupandRadixdipsacigroup(P<O.05)。andwashigherthanthosein由eprescription2groupandcontrolgroup,whichindicatedthatprescriptionswasbenefittOembryoimplantationinmice.PharmacodynamictestshowedthatPRwasextremesignificantlyhigherintocolys—isgroupthanthoseinthecontrolgroupandhigh—dosegroup(Psignificantlyhigherthanthatinthelow—osegroup(PP'levelandP4/E2wereextremesignificantlyhigherinthetocolysisgroupthanthoseinthehigh—dosegroup,low—dosegroup,controlgroupandhealthgroup(PP4/Ezwassignificantlyhigherinthetocolysisgroupthanthatinmiddle——dosegroup(PEzlevelinserumwassignificantlylowerinthetocolysisgroup□low-dosegroupandhealthgroupthanthatin山ehigh一dosegroupandthecontrolgroup(Pinserumwassignifi一cantlyhigherinthemiddle-dosegroupthanthatinthecontrolgroup(Pconclusion,prescription3couldimproveprogestinlevelinserumandtheratioofprogestintOestradiolinmice,whichwerehelpfulforembryoimplantation.Keywords:embryoimplantationdysfunction;Chinesemateriamedica;progestin;estradiol咪哩苯脉(imidocarb,IM)又称双豚苯腿或咪多卡,是一利动物专用抗原虫药物(王兆学等,2008),山瑞士Monbijoustrasse公司研发,1969年其二盐酸盐首次在瑞士面市。1969年Schmidt等在应用鼠骆巴贝斯虫筛选均二苯脉类化合物时,发现该药具有极好的抗梨形虫作用。随后相继证明其对马、牛、羊及犬等的巴贝斯虫病也有良好的治疗和预防作用(李德昌,1986)o该药已广泛应用于世界各地,是当今国际公认的最佳抗原虫纵李光壁等,2008),文章就该药的研究进展作一概述。1理化性质咪哇苯又称双咪苯服咪I座I咻卡普(Marchetti等,2008),为均二苯服(carbanilide)类中联咪(dia—midine)的衍生物(Rie等,2011),分子式Ci9H20N6O,分子质量为348.40g/mol,化学名为N,N,-二[3—(4,5二冬1-1H-咪哇-2-基)苯基]服(李光壁等,2008),商品名为imizol(李德昌,1986),结构式见图1。用于临床的咪I座苯腿衍生物有两种:二盐酸咪哇苯服(imidocarbdihydrochloride,MD)和二丙酸咪...