The putative dopamine autoreceptor agonist B-HT 920 decreases nigral dopamine cell firing rate and prolactin release in rat.

Recent behavioural and biochemical investigations have suggested that the alpha-2 receptor agonist B-HT 920 is also a centrally acting dopamine (DA) agonist with a selectivity for autoreceptors. It is presently demonstrated that B-HT 920, in contrast to the structurally related alpha-2 agonist B-HT 933, effectively reduces the firing rate of nigral DA neurons both after intravenous and microiontophoretic administration. Furthermore, B-HT 920, but not B-HT 933, decreases plasma levels of prolactin in reserpine pretreated rats. The electrophysiological as well as the neuroendocrine effects of the drug were antagonised by DA antagonists but not by alpha-2 receptor antagonists. The data support the contention that B-HT 920 acts as an agonist at central DA autoreceptors. Furthermore, they reinforce the hypothesis that lactotroph DA receptors are more similar to DA autoreceptors than to postsynaptic DA receptors in the brain.