~(111)In-DTPA-octreotide的标记条件研究及初步动物实验

  • 摘要: 研究了一步法不经纯化111In标记生长激素抑制素(SMS)类似物DTPA-octreotide的标记条件,其中包括反应时间、DTPA-octreotide用量、反应体积等。标记率达99%,比活度为277.5PBq/mol,产物的放化纯度>99%。对标记物的稳定性及其在小鼠体内的分布也进行了观察。

     

    Abstract: LABELINGSTUDYON111In┐OCTREOTIDEANDPRIMARYANIMALTESTSWangFanFanHongqiangXiaoLun*WangYishanJinXiaohaiChenDamingBaiHongshengChengZhenDuJin(ChinaInstituteofAtomicEnergy,Beijing102413)ABSTRACTOctreotide,asomatostatinanalogue,isausefulligandforinvitrodetectionofsomato-statinreceptor.111In-DTPA-octreotidecanbeusedforthevisualizationofsomatostatinrecep-tor-positivetumorsbygammacamerascintigraphy.Inthepaper,thelabelingconditioninclud-ingtheefectsofreactiontime,theDTPA-octreotidequantityandthereactionvolumeonla-belingyieldarestudied.ThelabelingyieldisanalysedbyHPLC,anditreachesupto99%withoutfurtherpurification.Spectificactivityofradiolabeledcompoundis277.5PBq/mol,theradiochemicalpurityismorethan99%.Theinvitrostabilityof111In-DTPA-octreotideandthebiodistributioninratsaremeasured.Itisshownthattheradiochemicalpuritydecreaseswithstocktimeandthe%ID·g-1inadrenalsishigherthanotherorgans.111In-DTPA-octreotideclearanceintissuesisslowerthanthatof111In-DTPA.Keywords111In-DTPA-octreotidelabelingconditionbiodistribution

     

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