Red deer display characteristic seasonal changes in appetite, growth,
and reproduction which are mediated by the pineal hormone, melatonin,
which provides a direct neuroendocrine transduction of the ambient pho
toperiod. To identify potential central sites of action for this hormo
ne, [2-I-125]iodomelatonin binding sites were localized and characteri
zed within the cervine brain and pituitary by in vitro autoradiography
. Specific binding was distributed over a number of discrete regions o
f the brain, including the cortex, septum, putamen, hippocampus, cereb
ellum, and superior colliculus. The choroid plexus, the pars tuberalis
, and the pars distalis of the pituitary were also specifically labele
d. Specific binding was completely abolished in the presence of 10(-7)
M melatonin and inhibited in the presence of 10(-4) M GTP gamma S (gu
anosine-5-O-(3-thiotriphosphate)), a nonhydrolysable analogue of GTP,
in the pars tuberalis, pars distalis, choroid plexus, and all neuronal
regions examined apart from the hippocampus and layer III of the cere
bral cortex. Inhibition of [2-I-125]iodomelatonin binding by GTP gamma
S is indicative that binding is representative of a G-protein-coupled
receptor. Characterization studies showed that [2-I-125]iodomelatonin
binding was time-dependent and saturable with a dissociation constant
(K-d) in the low picomolar range (approximately 10 pM). Competition s
tudies with iodomelatonin, melatonin, and N-acetylserotonin gave IC50
values similar to those previously characterized for the melatonin rec
eptor in the ovine pars tuberalis. (C) 1996 Academic Press, Inc.