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Binding of 125 I‐iodovinyltetrabenazine to CNS vesicular monoamine transport sites
Author(s) -
Kung MeiPing,
Canney Daniel J.,
Frederick Dana,
Zhuang Zheng,
Billings Jeffrey J.,
Kung Hank F.
Publication year - 1994
Publication title -
synapse
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.809
H-Index - 106
eISSN - 1098-2396
pISSN - 0887-4476
DOI - 10.1002/syn.890180308
Subject(s) - tetrabenazine , monoamine neurotransmitter , in vitro , chemistry , ligand (biochemistry) , binding site , vesicular transport protein , vesicular monoamine transporter 2 , biophysics , pharmacology , neuroscience , biochemistry , biology , serotonin , receptor , vesicle , dopamine , membrane
Binding characteristics of a novel radioiodinated tetrabenazine (TBZ) analog (iodovinyltetrabenazine; 125 I‐TBZ‐Fraction I) were evaluated. In rat striatal homogenates, 125 I‐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 125 I‐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. © 1994 Wiley‐Liss, Inc.