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 ( K d = 21 pM) melatonin binding sites ( B max = 8.5 fmol/mg protein). The order of potency of various indole amines to inhibit 125I-melatonin binding was melatonin ⪢ N-acetyl-5-hydroxytryptamine > 5-methoxytryptamine > 5-hydroxytryptamine.

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