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Abstract
125I-Melatonin was used to localize and characterize the melatonin receptor sites
in the rat hypothalamus. Autoradiography revealed that displaceable 125I-melatonin
binding occurred in suprachiasmatic nuclei and median eminence only. Further studies
performed on crude membrane fractions from median eminences revealed high affinity
(Kd = 21 pM) melatonin binding sites (Bmax = 8.5 fmol/mg protein). The order of potency
of various indole amines to inhibit 125I-melatonin binding was melatonin much greater
than N-acetyl-5-hydroxytryptamine greater than 5-methoxytryptamine greater than 5-hydroxytryptamine.