Sulpiride and Other Benzamides as Specific Antagonists at the D2 Dopamine Receptor

Abstract

This chapter discusses sulpiride and other benzamides as specific antagonists at the D 2 dopamine receptor. Sulpiride is a substituted benzamide, and similar to metoclopramide it possesses a pronounced antiemetic activity. Sulpiride possesses strong inhibitory effects on apomorphine-induced vomiting in dogs and is a potent stimulant of prolactin release both in the laboratory animals and man. The chapter presents the in vitro and in vivo investigation of the interaction of sulpiride and other substituted benzamides with dopamine (DA) and other neurotransmitter receptors at the molecular level. The reliability of these studies has been strengthened by the use of stereoselectivity of agonist and antagonist compounds as a research tool. Brain homogenates or slices were prepared according to a standard procedure and the effect of sulpiride and some chemically-related derivatives were determined on the stimulation of cyclic adenosine monophosphate (AMP) formation elicited by DA. The chapter also presents the comparison of the ability of sulpiride with that of various dopamine agonists and antagonists to displace the specific binding of 3 H-Haloperidol from rat striatal membrane preparation..