Virtual discovery of melatonin receptor ligands to modulate circadian rhythms.

ABSTRACT: The neuromodulator melatonin synchronizes circadian rhythms and related physiological functions through the actions of two G-protein-coupled receptors: MT₁ and MT₂. Circadian release of melatonin at night from the pineal gland activates melatonin receptors in the suprachiasmatic nucleus of the hypothalamus, synchronizing the physiology and behaviour of animals to the light-dark cycle^1-4. The two receptors are established drug targets for aligning circadian phase to this cycle in disorders of sleep^5,6 and depression^1-4,7-9. Despite their importance, few in vivo active MT₁-selective ligands have been reported^2,8,10-12, hampering both the understanding of circadian biology and the development of targeted therapeutics

SUBMITTER: Stein RM 

PROVIDER: S-EPMC7134359 | biostudies-literature | 2020 Mar

REPOSITORIES: biostudies-literature