• Article

Radiosynthesis of a Photoaffinity Probe for the Cocaine Receptor of the Dopamine Transporter: 3b-(p-Chlorophenyl)tropan-2b-carboxylic Acid m-(125I]-Iodo)-p-Azidophenethyl Ester ([125I]-RTI-82)

The tropane alkaloid RTI‐82, an iodoarylazide, has been labeled with iodine‐125 for use as a photoaffinity probe for the cocaine binding site of the dopamine transporter. The one‐flask radiosynthesis involves nocarrier‐added electrophilic radioiodination of the corresponding aniline followed by diazotization and treatment with sodium azide. Isolation by reverse phase HPLC and solid phase extraction gives [125I]‐RTI‐82 in good yield (76 ± 7%, n=6), high radiochemical purity (>99.8%), and high specific radioactivity (1490 ‐ 1880 mCi/μmol).

Citation

Lever, J. R., Carroll, F., Patel, A., Abraham, P., Boja, J., Lewin, A., & Lew, R. (1993). Radiosynthesis of a Photoaffinity Probe for the Cocaine Receptor of the Dopamine Transporter: 3b-(p-Chlorophenyl)tropan-2b-carboxylic Acid m-(125I]-Iodo)-p-Azidophenethyl Ester ([125I]-RTI-82). Journal of Labelled Compounds and Radiopharmaceuticals, 33(12), 1131-1137. https://doi.org/10.1002/jlcr.2580331207

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