Melatonin (MT) Receptor Antagonists Small Molecules and Peptides

Melatonin receptors are a group of high affinity G_i/G₀ protein-coupled receptors, which are split into two subtypes; MT₁ and MT₂. A third melatonin receptor, MT₃, was proposed to exist but it has since been shown to be the hamster homolog of human quinone reductase 2 and is therefore not considered within this GPCR classification.

MT₁ and MT₂ receptors are widely distributed with high concentrations found in the brain (especially in the suprachiasmatic nucleus) and in the retina. Lower ...