188Re直接标记octreotide的方法学
Investigations of directly labelling octreotide with 188Re
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摘要: 188Re标记octreotide可用直接标记法或间接标记法。直接标记法包括预锡化法和分步还原法,分步还原法需先用还原剂还原octreotide,然后用SnCl2还原188ReO4-进行直接标记;预锡化法则直接以SnCl2还原octreotide和188ReO4-,打开octreotide分子内双硫键,使188Re直接标记octreotide。预锡化直接标记法简便快速,能够得到较高的放化纯度,无须进一步纯化,适合用于制备药盒。Abstract: Octreotide can be labelled with 188Re by using the direct labelling approach and the bifunctional chelate approach.The direct labelling approach concludes pretinning procedure and two-step reduction method.By pretinning pro-cedure,both octreotide and perrhenate are reduced by SnCl2.Rhenium of a lower oxidation state is bound to octreotide directly.By two-step reduction method,octreotide and the perrhenate are reduced by different reduction agent respectively.The direct radiolabelling approaches allow very high radiochemical purity,high specific activity formulation,low radiocolloid formation and good in vitro stability,without the need for post-radiolabel ling purification to eliminate the un-bound free radioisotope.A kit could be developed which would merely require the mixing of perrhenate with the other reagents in a single vial.
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Key words:
- octreotide /
- receptor /
- somatostatin /
- 188Re /
- isotope labelling
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