Target intelligence / Profile preview

Melatonin Receptor Type 1 (MT1)

Target
MT1
Molecular classification
G protein-coupled receptor, GPCR, Receptor
01

Overview

The Melatonin MT1 receptor is a G protein-coupled receptor that binds the neurohormone melatonin. It plays a central role in regulating circadian rhythms, sleep, and various neuroendocrine functions. Upon binding melatonin, MT1 primarily couples to Gi proteins, leading to inhibition of adenylyl cyclase and decreased intracellular cAMP levels. It is expressed in several key tissues including the suprachiasmatic nucleus (SCN) of the hypothalamus, pars tuberalis of the pituitary gland, and retina. Drugs targeting MT1 are used for treating insomnia, non–24-hour sleep-wake disorder, depression, and jet lag.

Other names
Melatonin receptor 1AMTNR1AMelatonin receptor subtype 1
02

Mechanism of action

Agonist at MT1 receptor, leading to inhibition of adenylyl cyclase and decreased cAMP levels. Activation also increases phosphorylation of MAPK/ERK pathways and enhances potassium conductance via Kir channels.

03

Biological functions

Signal transductionCircadian rhythm regulationSleep regulationNeuroendocrine regulationModulation of neuronal excitability
04

Disease associations

Sleep disordersMood disordersDepressionAnxietyNeurodegenerative diseasesDrug addiction
05

Safety considerations

DrowsinessDizzinessSomnolence
06

Interacting drugs

Melatonin

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