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A radioreceptor binding assay was developed to determine the selectivity of beta-adrenoceptor agents in rat brain. This was achieved by using the highly selective unlabelled antagonists CGP 20712A and ICI 118-551 to block beta 1- or beta 2-sub-populations respectively in rat cerebral cortex membranes. This permitted the selective labelling of beta-adrenoceptors with the antagonist (-)-[125I]pindolol. Using this method, compounds could be routinely screened and selectivity profiles for binding in the CNS determined with a high degree of sensitivity and resolution.
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