, Volume 73, Issue 1, pp 7-21

Human dopamine receptor subtypes—in vitro binding analysis using3H-SCH 23390 and3H-raclopride

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Affinities and regional densities of the D1- and D2-dopamine receptor subtypes were studied in the human post-mortem brain in vitro using the two selective radioligands3H-SCH23390 and3H-raclopride.3H-Raclopride binding was confined to the caudate nucleus, the putamen and the substantia nigra, while3H-SCH23390 bound to cortical regions as well. The binding of3H-SCH 23390 was reduced by a low concentration of ketanserin, indicating binding to 5-HT2 receptors in addition to the D1dopamine receptors. The endogenous neurotransmitter dopamine interacted potently both with the D1-dopamine receptor and the D2-dopamine receptor, displaying two affinity states for each subtype. The distribution of the dopamine receptor subtypes obtained in the present in vitro investigation is in agreement with data obtained with11C-SCH 23390 and11C-raclopride in positron emission tomographic studies in human volunteers.