Prejunctional Dopamine Receptor Stimulants

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Abstract
Research efforts devoted to the search for compounds interacting with peripheral dopamine (DA) receptors has centered almost exclusively on the vascular DA (DA1 receptor. This is not altogether surprising in view of the attractive pharmacological profile such a drug would have on the cardiovascular system and on renal function. Relatively little attention has been given, however, to the therapeutic possibilities of compounds interacting with peripheral, prejunctional DA (DA2) receptors, although this mechanism also is not without interest, having the potential for producing a hemodynamic picture resembling that of centrally acting α2-adrenoceptor stimulants of the clonidine type, without at the same time inducing central sedation and other side effects characteristic of this substance class. Such a compound would, theoretically, provide effective antihypertensive activity by diminishing the tonic influence of the sympathetic nervous system on the vasculature and myocardium. A potential advantage would be an absence of baroreceptor-mediated reflex increases in heart rate and renin release, which tend to offset the antihypertensive effects of compounds producing passive dilation by acting on specific receptors or ion channels in vascular smooth muscle. A disadvantage of this type of drug, however, is its potential for inducing nausea and vomiting, a side effect which might limit acceptability in an indication such as hypertension for which there are so many useful drugs available.

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