The concentrations of endogenous γ-aminobutyric acid (GABA) receptor ligands were measured in hypophysial portal plasma by a sensitive and specific radioreceptor assay. Portal plasma contained higher concentrations of GABA receptor ligands than peripheral controls, although this increase was not due to authentic GABA but an unknown low-affinity ligand. Evidence is presented to support the hypothesis that the dipeptide homocarnosine may represent at least a part of this unknown. Electrical stimulation of median eminence evoked a massive (7.8-fold) increase in the rate of release of GABA (but not the low-affinity component) into portal blood. These results suggest that GABA and possibly other low-affinity ligands such as homocarnosine could serve as factors involved in the central control of anterior pituitary function.
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