A review on Melatonin Binding Sites
The discovery of melatonin binding sites has been done in the year 1984 by Vakkuri and it has been achieved by the synthesis of 2 indomelatonin. It has now been used in several studies to understand the melatonin biding sites in a range of tissues and species. The discovery of this radioligand and autoradiograph studies have paved the way of many hidden insights to light. Using this radioligand both the high and low affinity binding sites has been affirmed and has been named as ML1 and ML2. and the peculiarity of the binding sites are the low affinity of expression. In humans the tissue distribution of MT1 and MT2 levels has been studied mainly in the brain. The expressions of the receptors are mainly seen in suprachiasmatic nucleus, hypothalamus, hippocampus, cerebellum and cerebral arteries. MT1 is expressed in retina, adipose tissue and the kidney tissue and MT2 is expressed in the adipose and kidney tissues as well. Another MT3 melatonin receptor has been identified as the form of human homologue of the cytoplasmic reductase. Expression of melatonin binding sites has also been found in the liver. Liver represents as the most important organ for melatonin metabolism and the hormone undergoes 6 hydroxylation followed by sulphate or glucoronide conjugation. 6 sulphatoxymelatonin is the major urinary metabolite of melatonin in humans and the measurement provides simple and important assessment of melatonin secretion.
Source:- 1. Physiological and metabolic function of melatonin, Jaione Barrenetxe, Martinez Alfred
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