Abstract
The goal of the article is to provide a clearer understanding of how melatonin and its related analogs interact with melatonin receptors with the hope of developing important tools and agents of significant clinical and scientific importance. The review provides a compilation of the currently published melatonergic ligands and their relative affinities for melatonin receptors and discusses the importance of developing reversible, high-affinity, and subtype selective melatonin receptor antagonists. In addition, the review discusses the utility of developing high-affinity charged melatonergic ligands and irreversible ligands. Finally, the review discusses some of the problems associated with the current models used to study receptor pharmacology and function. As the availability of tools increases in the melatonin receptor field, a great body of knowledge is also gained about the structure of the melatonin receptor and the role that specific melatonin receptor subtypes have in physiologic processes. Further design, synthesis, and application of melatonergic ligands will lead us to a clearer understanding of the role that melatonin and its receptors play in humans.
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