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,(,610041),,;,,,,DryobalaropsaromaticaGaerta.f.,Blumeabalsamifera(L.)DC.,,,(d2borneol);(l2borne2ol);,55%,35%(isoborneol)Cinnamomumcamphora(L.)Sieb.,d2borneol,2005[1,2],:,,,,,,,,,,,,,,,1ADME80,3H,,5min,30min,,72h;,,18h,24h[3]3H2.8min,,0.25,5.3h,18h[4]20min45min,16.4mg/L57.4g/g,5min10g/g[5]5min,30min,;0.07513h,0.2735h[6]303mg/kg,,,1/2,18h1/10,[7]22.11990,5mg/kg,25min(tetramethylpyrazine,TMP),TMP,AUC,TMP[8]100mg/,5min4h[9],30mg/kg,44.8%,AUC88.7%[10];20mg/kg,;30min,,(102030mg/L)[11]300mg/kg,,,[12]2.2CT,1.5g/kg,CT,,,,[13]100mg/kg,/,,,[14],1.5g/kg40min,152030min,[15],48min1.5g/kg14,,;;,,/[16]400800mg/kg10min,24h,,,[17],40min,iNOS782007;23(1),iNOS,iNOSiNOS,,[1820]750mg/kg(Carbamazepine,CBZ),CBZ10,112(10,112epoxidecarbam2azepine,ECBZ),CBZECBZ;CBZ/,ECBZ/,[21]300mg/kg,,4,30min,;1252505001000mg/kg,250mg/kg;250mg/kg,00.582448h,0.5848h,;40mg/kg,[22]10%1h,20min,[23]600mg/kg15min,AUCCmax285.14gmin/g1.98g/g569.46gmin/g5.08g/g,,[24]95%1g/kg10mg/kg,,2.5120min,[25][26]2.3,,19893H25%,0.51,9h,[27]2,28.53.5,[28],,[29],Higuchi,6813%[30]1%3%,;3%[31]2%1.71[32]1%2.19,[33,34],,1.536%;3%1.5%,36%,[35]2%,[36]2%2.3[37]0.5123%;,,1%,[38],123%,2%,6.1[39],2%;,[40,41],[42]2.4,0.5123%,1%[43](102030g/L)Rg1,10g/L[44]00.030.060.120.240.48%2,5.64.24.716.413.112.9%[45],125I2(2cobrotoxin,Nt),[46,47]0.04%15120min[48],,,[49]2.5,,,,(Matin2Darbycaninekidneyepithelium,MDCKE)(MDCKE),0.086mol/LMD2CKE424h,4h,,;24h,;24h,,,[50]MDCKEHelaP2gp,,P2gp,,[51]882007;23(1)3,,,,,,,,,;,1;,,,,[6,13,50,51],,,1,,,..,2005;28(9)7817822.(2005,).,2005403,.3H22.,1981;(05)4,,,.3H2.,1982;(8)575,..,1993;4(4)38406,,,..,2002;13(6)3813827,,,..,2006;17(4)2652678,,,..,1990;11(1)42449,.Gc2Msd.,1994;29(9)69770110,,..,2001;21(5)26426611,,,..,2003;20(4)24524812,,.GC2MS^n.,2006;41(16)1259126213,,,.Ct.,1992;3(4)283414,,,..,1994;11(1)374015,,,.,.,1993;10(4)21121316,..,1995;(6)313317,,,..,2003;28(2)9910118,..,2002;13(5)28728819,,,..,2001;9(4)20720920,,,.iNOS.,2002;18(5)59059121,,,..,2005;21(10)1263126622,,,..,2002;37(4)27527723,,,..,2004;25(2)15615724,,,..,2004;39(4)28929125,,,..,2006;15(1)303126,,,..,2005;16(17)1291129327,,,..,1989;20(1)252628,,,.2.,1989;24(7)55655929,..,2000;31(8)60760930,..:,2006;25(1)303131,..,1999;34(2)10410632..,2003;(92)747533,,,..,2006;17(6)1003100434,,,..,2006;4(2)11111335,,,..,1992;8()17818036,..,1998;29(6)39139337,..,2000;25(1)323438,,..,2001;23(12)86486739,..,2004;10(16)18618840,,..,2004;13(5)41641841,,,..,2005;45(5)161742,,,..,2003;12(1)3436(86)2007;23(1)1,..,,200357,662,6732..,2003;35(8)6356403,.:.,2003;24(3)1124HardmanJG,LimbirdLE,eds.Goodman&Gilman’s,ThePharmacologi2calBasisofTherapeutics.10edition,,McGraw2Hill.2002(English):175,560,2004()132,4285,..,2005;27(3)1306LiuJS,ZhuYL,YuCM,etal.ThestructureofhuperzineAandB,twonewalkaloidsexhibitingmarkedanticholinesteraseactivity.CanJChem,1986;64(4)8777,,..,1986;7(2)1108WangH,TangXC.AnticholinesteraseeffectsofhuperzineA,E2020andtacrineinrats.ActaPharmacolSin,1998;19(1)279TangXC,DeSarnoP,Sugayak,etal.ComparisonofhuperzineA,anewcholinesteraseinhibitoronthecentralcholinergicsystemoftherat.JNeuros2ciRes,1989;24(2)27610TangXC,KindelCH,KozikowskiAP,etal.ComparisonoftheeffectsofthenaturalandsynthetichuperzineAonratbraincholinegicfunctioninvitroandinvivo.JEnthnopharmacol,1994;44(3)14711ZhuXD,GiacobiniE.Secondgenerationcholinesteraseinhibitors:effectof(L)2huperzineAoncorticalbiogenicamines.JNeurosciRes,1995;41(6)82812,..,2005;16(16)126613,,.Alzheimer’s.,2001;36(5)28914WangR,XiaoXQ,TangXC.HuperzineAattenuateshydrogenperox2ide2inducedapoptosisbyregulatingexpressionofapoptosis2relatedgenesinratPC12cells.Neuroreport,2001;12(12)262915XiaoXQ,ZhangHY,TangXC.HuperzineAattenuatesamyloidbeta2peptidefragment252352inducedapoptosisinratcorticalneuronsviainhibi2tingreactiveoxygenspeciesformationandcaspase23activation.JNeusosciRes,2002;67(1)3016ZhouJ,TangXC.HuperzineAattenuatesapoptosisandmitochondria2dependentcaspase23inratcorticalneurons.FEBSLett,2002;526(123)2117,,,.[Ca2+],,.,2004;23(2)7318,,,.NM2DAmRNA.,2005;25(9)80019YeJW,CaiJX,TangXC,etal.ImprovingeffectsofhuperzineAonspa2tialworkingmemoryinagedmonkeysandyoungadultmonkeyswithexperim2intalcognitiveimpairment.JPharmacolExpTher,1999;288(2)81420,,,..,1988;9(3)19321QianBC,WangM,ZhouZF,etal.PharmacokineticsoftablethuperzineAinsixvolunteers.ActaPharmacolSin,1995;16(5)39622..,2000;19(1)3323,,,..,2000;19(1)1024,,,..,2004;8(7)121625,,,..,1991;12(3)25026,,,.Alzheimer’s.,1995;4(4)19627XuSS,XieHB,DuZW,etal.Efficacyoftablethuperzine2Aonmemoryandcognitioninpatientswithbenignsenescentforgetfulness.ChinJClinPharmacolTher,1997;2(1):128,,,..,2002;82(14)94129,,,..,2001;14(2)7530GeertsH.NC2531(Neurochem).CurrOpinInvestigDrugs,2004;5(1)9531,..,2005;40(21)1616()43,,..,2002;7(5)43443644,,,.Rg1.,2006;41(4)26126445,,,..:,2001;29(A01)414346,,,.^1252.,2004;22(4)20020247,,..,2006;23(2)16917148,,,..,2003;28(1)818249,,,..,1998;8(2)676950,..,2004;24(7)63263451,.P2.,2003;14(2)9699682007;23(1)
本文标题:冰片促透作用研究进展
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