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1、W&SPharmchemchinalimitedHttp://www.wspharmchem.comE-mail:wspharmchem@gmail.comIvermectinMonographNumber:5268Title:IvermectinCASRegistryNumber:70288-86-7AdditionalNames:22,23-Dihydroabamectin;22,23-dihydroavermectinB1;22,23-dihydroC-076B1Manufacturers'Codes:MK-933Trademarks:Cardomec(Mer
2、ck&Co.);Cardotek-30(Merck&Co.);Eqvalan(Merial);Heartgard30(Merial);Ivomec(Merial);Mectizan(Merck&Co.);Noromectin(Norbrook);Stromectol(Merck&Co.);Zimecterin(Merck&Co.)LiteratureReferences:Semi-syntheticderivofabamectin,q.v.,oneoftheavermectins,q.v.Ivermectincontainsatleast80%of22,23-dih
3、ydroavermectinB1aandnotmorethan20%of22,23-dihydroavermectinB1b.Prepn:JPKokai7961198;J.C.Chabala,M.H.Fisher,US4199569(1979,1980bothtoMerck&Co.);J.C.Chabalaetal.,J.Med.Chem.23,1134(1980).Approachestosynthesis:H.Mroziketal.,TetrahedronLetters23,2377(1982);M.E.Jungetal.,ibid.28,5977(1987);
4、M.E.Jung,L.J.Street,Heterocycles27,45(1988).Antiparasiticactivity:J.R.Egertonetal.,Brit.Vet.J.136,88(1980);E.T.Lyonsetal.,Am.J.Vet.Res.41,2069(1980);L.S.Blair,W.C.Campbell,ibid.2108.Acaricidalefficacy:C.A.Wilkinsetal.,Am.J.Vet.Res.41,2112(1980);R.O.Drummondetal.,J.Econ.Entomol.74,432(1
5、981).Irreversibleeffectsonadultparasitesinonchocerciasis:A.P.Plaisieretal.,J.Infect.Dis.172,204(1995).Metabolisminanimals:S.-H.L.Chiuetal.,DrugMetab.Dispos.14,590(1986).Pharmacokineticsinhorsesandsheep:S.E.Marrineretal.,J.Vet.Pharmacol.Ther.10,175(1987).Evaluationinhumanonchocerciasis(
6、riverblindness):M.A.Azizetal.,Lancet2,171(1982);P.T.Soboslayetal.,Trop.Med.Parasitol.38,8(1987).Clinicaltrialinonchocerciasis:A.T.Whiteetal.,J.Infec.Dis.156,463(1987).HPLCdetermnincattleandsheeptissues:P.C.Twayetal.,J.Agr.FoodChem.29,1059(1981);inhumanplasmaandmilk:R.Chiouetal.,J.Chrom
7、atog.416,196(1987).Reviewofchemistryandbiology:W.C.Campbelletal.,Science221,823-828(1983).Reviewofuseintreatmentofheartwormindogs:W.C.Campbell,Sem.Vet.Med.Surg.2,48-55(1987).Reviewofclinicaluseandpharmacology:W.C.Campbell,G.W.Benz,J.Vet.Pharmacol.Ther.7,1-16(1984);T.B.Barragry,Can.Ve
