Properties of [3H]haloperidol and [3H]dopamine binding associated with dopamine receptors in calf brain membranes

Burt, D.R.; Creese, I.; Snyder, S.H.

Molecular Pharmacology 12(5): 800-812


ISSN/ISBN: 0026-895X
PMID: 995128
Accession: 068539571

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[3H]Haloperidol and [3H]dopamine bound in saturable fashion to membranes from calf brain with high affinity and other characteristics indicated an association with postsynaptic dopamine receptors. Kinetic analysis of rates of association and dissociation yielded KD values in agreement with equilibrium measurements. Regional variations in [3H]dopamine and [3H]haloperidol binding were parallel and corresponded to regional differences in dopaminergic innervation. Drug specificity did not appear to differ between limbic and striatal areas. The relative potencies of various agonists and antagonists on the binding of the 2 ligands paralleled their pharmacological actions at dopamine receptor sites. Dopamine agonists had 6-38 times more affinity for [3H]dopamine than [3H]haloperidol binding sites. Dopamine antagonists had 20-12,000 times more affinity for [3H]haloperidol than [3H]dopamine binding sites. Ergot derivatives, including d-LSD, and other serotonin antagonists had substantial affinity for both types of binding.