Abstract
The enantiomers of the dopamine (DA) agonist PD 128483 ( 1) have been synthesized and characterized biochemically (D 1, D 2 receptor binding, effects on rat brain DA synthesis), electrophysiologically (inhibition of DA neuron firing) and behaviorally (effects on rat exploratory locomotor activity). While R-(+)− 1 is a potent D 2 agonist that stimulates both pre- and postsynaptic DA receptors, S-(−)− 1 is a weak partial DA agonist able to stimulate only the more sensitive presynaptic DA receptors (DA autoreceptors).
Published Version
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