Melatonin receptor binding

Melatonin produces its effects via the GPCR, ML-1. A second lower affinity form, ML-2, has been described on the basis of binding data. Activation of melatonin receptors can inhibit DA release in the retina. 

Identification of melatonin in plants DC094 and its effects on plasma melatonin levels and binding to melatonin receptors in the verterbrates Biochem Mol... 

J Nutr 1994 124(9) 1678-1684. Hattori, A., H. Migitaka, M. ligo, et al. Identification of melatonin in plants and its effects on plasma melatonin levels and binding to melatonin receptors in vertebrates. Biochem Mol Biol Int 1995 35(3) 527-634. 

SAR studies on melatonin analogues showed that methoxy and amido moieties are important for binding to melatonin receptors various substituents on the 2nd position of the indole ring enhance the binding affinity [52-54]. The conformational flexibility of the C-3 ethylamido side chain is probably responsible for the broad spectrum of biological activities. As a powerful antioxidant melatonin was shown to have significantly broader actions including oncostatic effects [55], immune system stimulation [56], and antiinflammatory functions [57,58]. 

Spadoni G, Balsamlnl C, Diamantini G, et al. Conformatlonally restrained melatonin analogues synthesis, binding affinity for the melatonin receptor, evaluation of the biological activity, and molecular modeling study. J Med Chem 1997 40 1990-2002. 

In addition to its interaction with central BZD receptors, pharmacological concentrations of melatonin can also bind to the peripheral-type BZ receptors (PBRs), which are involved in neurosteroidogenesis (Garcia-Ovejero et al. 2005). PBRs are primarily localized on the outer mitochondrial membrane these sites are therefore also referred to as mitochondrial BZD receptors. Using the isoquinoline carboxamide, PK14105, for photoaffinity labelling, an 18 kDa isoquinoline... 

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