There is now evidence for more than one site of action for the hormone
melatonin (N-acetyl-5-methoxytryptamine). Recent pharmacological and
molecular advances are providing the tools to address the characteriza
tion of melatonin receptor subtypes. The development of novel melatoni
n receptor agonists and antagonists, high-affinity radioligands, quant
itative bioassays, and the recent cloning of melatonin receptors are f
urthering our understanding of native and recombinant melatonin recept
ors. In this article, Margarita Dubocovich discusses the properties of
melatonin receptors, and the basis for their classification into at l
east two subtypes, the ML(1) and ML(2).