Binding of 125I-iodovinyltetrabenazine to CNS vesicular monoamine transport sites.
Binding characteristics of a novel radioiodinated tetrabenazine (TBZ) analog (iodovinyltetrabenazine; 125I-TBZ-Fraction I) were evaluated. In rat striatal homogenates, 125I-TBZ-I displayed a pharmacological profile consistent with specific binding to vesicular monoamine transport (VMAT) sites. In vitro autoradiographic studies using rat brain sections further demonstrated that 125I-TBZ-I labeled the regions rich in VMAT sites, and it may be a useful marker for these sites. This novel radioiodinated ligand, with high specific activity and high binding affinity, may provide a powerful tool for the in vitro assessment of neuronal loss in various neurodegenerative diseases.
Kung
M P
MP
Department of Radiology, University of Pennsylvania, Philadelphia 19104.
Canney
D J
DJ
Frederick
D
D
Zhuang
Z
Z
Billings
J J
JJ
Kung
H F
HF
D000818:Animals; D015306:Biogenic Monoamines / Q000378:metabolism*; D001692:Biological Transport; D015415:Biomarkers; D001921:Brain / Q000378:metabolism*; D007457:Iodine Radioisotopes; D008297:Male; D017072:Neostriatum / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D013747:Tetrabenazine / Q000031:analogs & derivatives / Q000493:pharmacokinetics*
D015306:Biogenic Monoamines; D015415:Biomarkers; D007457:Iodine Radioisotopes; D013747:Tetrabenazine