Autoradiographic distribution of [3H]hemicholinium-3 binding sites in human brain.

Since previous radioligand binding studies support the evidence that [3H]hemicholinium-3 ([3H]HC-3) selectively labels the high-affinity choline uptake (HACU) process, we have studied the autoradiographic characteristics and regional distribution of [3H]HC-3 binding to post mortem human brain tissue. [3H]HC-3 specific binding was saturable, of high affinity and exhibited an uneven distribution. High densities were observed in caudate-putamen, nucleus basalis accesorius of the amygdala, hippocampal gyrus dentatus and CA3 field, locus niger, nucleus interpeduncularis and motor trigeminal and facial nuclei. Low densities were found in areas such as neocortex, thalamus, hypothalamus or cerebellum. Our results agree with those obtained in human brain membranes and are comparable to previous autoradiographic data from rat brain. Remarkably, the distribution of [3H]HC-3 binding sites closely corresponds with that of cholinergic enzymatic presynaptic markers and HACU. These findings, together with previous data from membrane studies, allow the use of [3H]HC-3 as a selective anatomical marker of cholinergic presynaptic terminals.