Labeling of ethambutol with 99mTc using a new reduction procedure. Pharmacokinetic study in the mouse and rat.
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.
Causse
J E
JE
Institut de Biologie, Faculté de Médecine, Montpellier, France.
Pasqualini
R
R
Cypriani
B
B
Weil
R
R
van der Valk
R
R
Bally
P
P
Dupuy
A
A
Couret
I
I
Benbarek
M
M
Descomps
B
B
D000818:Animals; D004977:Ethambutol / Q000493:pharmacokinetics*; D007553:Isotope Labeling / Q000379:methods; D007668:Kidney / Q000000981:diagnostic imaging / Q000378:metabolism; D051379:Mice; D015609:Organotechnetium Compounds / Q000493:pharmacokinetics*; D011877:Radionuclide Imaging; D051381:Rats; D014018:Tissue Distribution
D015609:Organotechnetium Compounds; C064843:technetium Tc 99m ethambutol; D004977:Ethambutol