Melatonin receptors are present in the ferret pars tuberalis and pars distalis, but not in brain.

The pineal hormone melatonin regulates reproductive function in seasonally breeding mammals. Recent studies using 125I-labeled 2-iodomelatonin (I-MEL) reveal that the distribution of putative melatonin receptors is species-specific; only the hypophysial pars tuberalis (PT) is a consistent site of I-MEL binding in all photoperiodic species examined. In the present study, we used in vitro autoradiography to examine the distribution of I-MEL binding in the ferret brain and pituitary. We report that I-MEL binding is restricted to the PT and pars distalis (PD) of the pituitary; I-MEL binding is absent from brain. I-MEL binds in the PT and PD with high affinity (Kd values ca. 40 pM) and the rank order of potency for inhibition of I-MEL binding (6-chloromelatonin = melatonin greater than 6-hydroxymelatonin greater than N-acetylserotonin greater than serotonin) is the same as that observed for high-affinity melatonin receptors from other species. The consistent presence of high affinity melatonin receptors in the PT of a variety of photoperiodic species suggests that the PT plays a major role in mediating the effects of melatonin on neuroendocrine function.