Abstract
Hemicholinium-3 (HC-3) is a potent inhibitor of the high-affinity choline uptake system (NACU). Here we report on the biochemical characterization and autoradiographic distribution of [3H]hemicholinium-3 binding sites in rat brain, confirming and expanding results from previous studies. The binding of [ 3H]HC-3 to striatal membranes was specific, to a single site, sodium-dependent, saturable, and of high-affinity, K d values being about 3 n m for striatum, 5 n m for the hippocampus and 12 n m for neocortex. [ 3H]HC-3 specific binding exhibited a pharmacological profile suggestive of physiologically relevant interactions and fully comparable to that reported for HACU. The uneven distribution of [ 3H]HC-3 binding sites exhibited a high degree of correspondence with the reported distribution of HACU and other enzymatic presynaptic cholinergic markers. The punctual differences between our study and previous works on [ 3H]HC-3 binding are analysed. We conclude that [3H]HC-3 labelling may be used as a selective and quantifiable marker of the cholinergic presynaptic terminals in close relationship with HACU.
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