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- W2020963200 abstract "The pharmacophore L-2-Br-tyrosine (2-Br-T) was obtained by a stereospecific synthesis in which benzophenonimine glycinesultame, sodium hexamethyldisilane and O-(methoxycarbonyl)-3-bromo-4-bromo ethylphenol are successively coupled followed by hydrolysis. Radioiodination (N.C.A.123/125I) was performed by Cu1+ assisted nucleophilic exchange on 2-Br-T with a mean labelling yield of 85%. RPHPLC coupled to C18 Sep-pak recovery allowed to obtain the radioactive compound with a radiochemical purity of >98%. The in vitro evaluation was carried out on WiDr cells (human colon carcinoma). L-2-125I- tyrosine (2-*I-T) was shown to follow for the larger part the L-transport system. For times up to 60 minutes the uptake was comparable with that of the reference 3H-tyr. A considerable amount of the radioactivity uptake was slowly washed out in efflux conditions. In comparison with 3H-tyr the incorporation in proteins was low. This can point to a retention mechanism which can be favourable for diagnosis. In vivo in rats bearing R1M rabdomyosarcoma tumours, the uptake in the tumour 40 minutes p.i. represented 1% ID/g with a tumour to blood ratio of 1.8. The tracer is fastly cleared from the blood to the bladder." @default.
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- W2020963200 date "2001-05-01" @default.
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- W2020963200 title "L-[2-RADIOIODO]-Tyrosine a potential tumour tracer for spect. Radiosynthesis, in vitro and in vivo evaluation" @default.
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