The affinity of metergoline for 3H-serotonin (5HT) binding sites is regulated by guanine nucleotide.

100 microM guanine nucleotide Gpp (NH)p reduces the affinity of the serotonergic antagonist metergoline for 3H-5HT binding sites in rat cerebral cortex. This effect is present both in inhibition binding and in saturation experiments. The hypothesis that the interaction of some serotonergic antagonists with 3H-5HT binding sites is regulated by guanine nucleotides is discussed.