A high-affinity [3H]tryptamine binding site in human brain

In vitro filtration binding revealed high-affinity specific [3H]tryptamine binding sites in human brain. These binding sites are heterogeneously distributed throughout brain, ranging from 280 fmol/mg protein in hippocampus and thalamus to approximately 90 fmol/mg protein in medulla oblongata and cerebellum. Preliminary autoradiographic studies indicate a heterogeneous distribution within layers of the frontal cortex. The observed stereoselectivity of the site, the interaction of the site with a G protein and the observed region-selective downregulation of the site in a human pathological condition, i.e. hepatic encephalopathy (Mousseau et al., 1994), suggests that this binding site is a functional [3H]tryptamine receptor. A similarity in kinetics and distribution of the [3H]tryptamine receptor in human and rat brain indicates that these two entities represent homologous structures, although the difference in pharmacological profiles suggests species variants. One cannot exclude the possibility that the rat and human [3H]tryptamine receptors do represent distinct subtypes. Finally, the suggested role for tryptamine in neuropsychiatric disorders as originally suggested by Dewhurst (1968) is supported by the present series of experiments.