CAJ | 학술논문

以天然生长抑素(Somatostatin,SMS)、葡聚糖-10(Dextran10,Dx10)及巯基乙胺(Cysteamine)为原料,合成糖基化生长抑素配体化合物SMS-Dx10-Cysteamine;以125I-奥曲肽(125I-Tyr3-Octreotide)为放射性配基,进行受体竞争结合实验,测定SMS-Dx10-Cysteamine的IC50值;利用葡庚糖转换络合进行SMS-Dx10-Cysteamine 的99Tcm标记,重点探讨99Tcm标记条件及标记物体外稳定性;并用99Tcm-Cysteamine-Dx10-SMS进行正常SD大鼠体内分布、血浆清除及肿瘤模型动物显像实验.结果表明:配体化合物SMS-Dx10-Cysteamine保持了对生长抑素2型受体高亲和力,其IC50值与SMS相近;在最佳标记条件:0.3 g/L SnCl2,5 g/L SMS-Dx10-Cysteamine,标记介质pH=6.0,室温下反应30 min,99Tcm-Cysteamine-Dx10-SMS标记率约为85%,经分离纯化后,其放射化学纯度大于99%,标记物体外稳定;99Tcm-Cysteamine-Dx10-SMS在正常大鼠体内血浆半衰期为2.38 h,主要浓聚于肝、脾脏并经肾排泄;荷胰腺癌裸鼠显像表明,注射后6 h,肿瘤组织具有明显的放射性摄取,99Tcm-Cysteamine-Dx10-SMS有望成为一种生长抑素受体阳性肿瘤显像剂.
이천연생장억소(Somatostatin,SMS)、포취당-10(Dextran10,Dx10)급구기을알(Cysteamine)위원료,합성당기화생장억소배체화합물SMS-Dx10-Cysteamine;이125I-오곡태(125I-Tyr3-Octreotide)위방사성배기,진행수체경쟁결합실험,측정SMS-Dx10-Cysteamine적IC50치;이용포경당전환락합진행SMS-Dx10-Cysteamine 적99Tcm표기,중점탐토99Tcm표기조건급표기물체외은정성;병용99Tcm-Cysteamine-Dx10-SMS진행정상SD대서체내분포、혈장청제급종류모형동물현상실험.결과표명:배체화합물SMS-Dx10-Cysteamine보지료대생장억소2형수체고친화력,기IC50치여SMS상근;재최가표기조건:0.3 g/L SnCl2,5 g/L SMS-Dx10-Cysteamine,표기개질pH=6.0,실온하반응30 min,99Tcm-Cysteamine-Dx10-SMS표기솔약위85%,경분리순화후,기방사화학순도대우99%,표기물체외은정;99Tcm-Cysteamine-Dx10-SMS재정상대서체내혈장반쇠기위2.38 h,주요농취우간、비장병경신배설;하이선암라서현상표명,주사후6 h,종류조직구유명현적방사성섭취,99Tcm-Cysteamine-Dx10-SMS유망성위일충생장억소수체양성종류현상제.