Multiple central WB-4101 binding sites and the selectivity of prazosin

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Under the conditions employed in a standard displacement assay of [ 3H]WB-4101 from calf neocortical membrane homogenates (0.22 n M total [ 3H]WB-4101), 70–80% of this radioligand is bound to a high affinity receptor site and 20–30% to a second, lower affinity site. This latter site is not the one previously shown to bind alpha agonists. Binding parameters for WB-4101 to each site have been determined. Prazonin is extremely selective for the high affinity site as indicated by a biphasic displacement of [ 3H]WB-4101.