The Dopamine/Neuroleptic Receptor

Abstract

The neuroleptic/dopamine receptor, with its picomolar affinity for potent neuroleptics, is the functional dopamine receptor of the brain. This receptor has been termed the D₂ dopamine receptor, and it inhibits or interferes with dopamine-stimulated adenylate cyclase. This D₂ receptor has two states, each having different affinity for dopamine. The high-affinity state, termed D₂^high, has a 10 nM affinity for dopamine and is the functional correlate for dopamine autoreceptors and for the dopamine receptor in the pituitary gland. The low-affinity state, termed D₂^low, has a 2000 nM affinity for dopamine, and may possibly represent the desensitized state of the dopamine receptor or the functional post-synaptic receptor.