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Labeling of ethambutol with 99mTc using a new reduction procedure. Pharmacokinetic study in the mouse and rat

✍ Scribed by J.E. Causse; R. Pasqualini; B. Cypriani; R. Weil; R. van der Valk; P. Bally; A. Dupuy; I. Couret; M. Benbarek; B. Descomps

Publisher: Elsevier Science
Year: 1990
Weight: 393 KB
Volume: 41
Category: Article
ISSN: 0883-2889
DOI: 10.1016/0883-2889(90)90010-e

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✦ Synopsis

Certain 99mTc-labeled derivatives of ethylene diamine substituted in NN', when labeled with 99mTc, have been proposed for studying renal excretion, and others for brain imaging. Ethambutol, a well known antituberculosis drug, possesses a structure very similar to these derivatives. We prepared a complex of [99mTc]ethambutol using hypophosphorus acid as the reducing agent. The complex was then analyzed by paper and cellulose F chromatography and by FAB mass spectrometry. A pharmacokinetic study in the mouse and rat indicated that the complex is eliminated by the kidney faster than DTPA, slower than [131I]hippuran and without significant renal retention. The [99mTc]ethambutol complex is easy to prepare and shows good stability in water at physiological pH, making it potentially useful in renal excretion studies.

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