The type of mechanism(s) by which melatonin alone and/or through the intervention of other putative neurotransmitters is able to control circadian rhythms remains unresolved. Comparison of 2-[125I]iodomelatonin binding pattern in the brain of castrated and gonadally intact Japanese quail (Coturnix japonica), using quantitative receptor autoradiography, displayed that the combination of the intact gonadal condition and a long-day (16L:8D) photostimulatory schedule is responsible for major binding changes. In fact, high and low binding levels were obtained in the suprachiasmatic area and nucleus ectomamillaris (p < 0.01) and in the nucleus preopticus anterior and paleostriatum primitivum (p < 0.001), respectively. A gonadal modulatory role was not always evident in all brain areas as revealed by long-day photic cycles producing diminished (p < 0.01) binding levels in the anterior neostriatum and the nucleus rotundus of both castrated and gonadally intact animals, although elevated values were also found in the substantia grisea centralis (p < 0.05) of the same animals. Saturation binding studies revealed that gonadal and/or photic effects induce alterations in the number of binding sites, whereas the affinity constant varied only in some hypothalamic sites. Testing of GABAergic activity on 2-[125I] iodomelatonin binding levels showed that this inhibitory neurotransmitter was responsible for increasing low receptor values. Moreover, GABA-dependent influences were shown to be mediated via a GABAA receptor subtype since bicuculline (specific antagonist of this site) inhibited the elevated GABA-induced melatonin binding levels in the above brain sites of the gonadally intact quail exposed to both photoperiod cycles. Even in this case, melatonin binding changes were due to the variations in the number of binding sites. The apparent GABAergic-gonadal influence resulting in changes of the 2-[125I] iodomelatonin binding values, under the different photic conditions, provides evidences of other probable neural mechanisms that entrain circadian rhythmicity in neuroendocrine activities and in sociosexual behaviors.