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Tritium Radiolabeled Antisense Oligonucleotides for ADME Studies

Radiolabeling is an essential part of drug development. Using a radiolabeled compound, the ADME can be quantitatively determined. Most often carbon-14 is the isotope of choice but tritium is very useful for potent compounds like oligonucleotides. The position of label in the nucleotide must be carefully chosen to avoid exchange in vivo. One also needs to consider the position of the labeled nucleotide in the sequence so that the label is not lost to nuclease-catalysed degradation.

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