Dopamine and dopamine receptors as target sites for cardiovascular drug action.

It is controversial whether dopamine (DA) is a peripheral neurotransmitter in the cardiovascular/renal system. The endogenous concentration of DA in the heart and blood vessels is generally only a fraction (5%) of that of norepinephrine (NE). With perhaps the exception of the kidney, the majority of the evidence suggests a precursor role for this amine rather than that of a neurotransmitter. The main weakness of arguments favoring DA as a vascular neurotransmitter is relative lack of data showing selective DA release and lack of effects of selective DA antagonists on neural stimulation. However, DA receptors have been characterized in cardiovascular tissues and are of two types: DA1 receptors located on vascular smooth muscle (postjunctional), which appear to mediate relaxation of the muscle, and DA2 receptors located on sympathetic nerves (pejunctional), which inhibit NE release. These receptors are interesting and potential target sites for novel cardiovascular drug action for the treatment of hypertension and renal ischemia. Moreover, selective DA receptor agonists will be important tools in understanding the role of DA receptors in normal and disease states.