M. Hirata et al., EVALUATION OF RADIOIODINATED IODOCLORGYLINE AS A SPECT RADIOPHARMACEUTICAL FOR MAO-A IN THE BRAIN, Nuclear medicine and biology, 22(2), 1995, pp. 175-180
An in vivo estimation of the newly synthesized MAO-A specific inhibito
r, [I-125]-labeled oro-6-iodophenoxy)propyl]-N-methyl-2-propynylamine
([I-125]-iodoclorgyline), was performed. Retention of the radioactivit
y of this radioligand was observed in the brain from 1 h post-injectio
n. Pretreatments with clorgyline and I-deprenyl showed selective bindi
ng of [I-125]-iodoclorgyline to MAO-A in the brain at 24 h post-inject
ion. Moreover, a good correlation (r = 0.907) between the uptake of [I
-125]-iodoclorgyline and MAO-A enzyme activity in the cortex was obser
ved in the pretreatment study with several doses of clorgyline. Althou
gh improvement to increase the brain/blood ratio is desirable because
of slow blood clearance of the radioactivity, radioiodinated iodoclorg
yline may serve as a useful SPECT radiopharmaceutical for quantitative
analysis of MAO-A in the brain.