Melatonin Receptor Signaling: Finding the Path Through the Dark

Melatonin, dubbed "the hormone of darkness," is involved in relaying photoperiodic information to the organism. Not only is melatonin involved in the regulation of circadian rhythms and sleep, but it also has roles in visual, cerebrovascular, reproductive, neuroendocrine, and neuroimmunological functions. Melatonin mediates its effects through G protein-coupled receptors: MT 1 , MT 2 , and, possibly, MT 3 . Pharmacological agents have been instrumental in identifying these receptor types. Masana and Dubocovich discuss how the level of receptor expression may alter their efficacy, so that caution is necessary when extrapolating the pharmacological properties of ligands defined on recombinant systems to the receptors in the organism. With these cautions in mind, they describe the various signaling pathways and physiological roles ascribed to the three melatonin receptor types.