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Radiolabelling optimization of 5-(4-[125I]-iodophenyl)-2,3 dihydro-5-hydroxy-5H-imidazo[2,1-a]isoindole or [125I]-iodo mazindol : A potential tool for spect explorations

✍ Scribed by E. Galinier; J. E. Ombetta; Y. Frangin; J. Mertens; J. C. Besnard; D. Guilloteau

Publisher
John Wiley and Sons
Year
1994
Tongue
French
Weight
467 KB
Volume
34
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

The radiolabelling of an iodinated analog of mazindol, 5‐(4‐[^125^I]‐iodophenyl)‐2,3‐dihydro‐5‐hydroxy‐5H‐imidazo[2,1‐a]isoindole, was performed in order to develop a potential tool for SPECT exploration of the presynaptic dopamine transporter in the human brain. Radiosynthesis was performed by iodide for bromide nucleophilic exchange from a brominated precursor. The reaction was carried out in the presence of the copper I catalyst and reducing and complexing agents. In these radiolabelling conditions, [^125^I] iodomazindol exhibited a tautomeric equilibrium. Therefore, in order to obtain the best labelling conditions, we studied variables such as copper I catalyst and brominated precursor concentrations, reaction temperature and heating time involved in the reaction.

This study of the kinetics could be used as a pattern for the radiosynthesis of other compounds which can be present in a tautomeric equilibrium under particular conditions. Indeed, we describe a convenient procedure to obtain each tautomeric form with high radiochemical purity in optimum radiolabelling conditions.

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