Target intelligence / Profile preview

Melatonin Receptor MT2 (MT2)

Target
MT2
Molecular classification
G protein-coupled receptor, GPCR, Receptor
01

Overview

The melatonin receptor MT2 is a G protein-coupled receptor (GPCR) that binds the neurohormone melatonin. It plays a crucial role in regulating circadian rhythms, sleep, mood, and other physiological processes. MT2 primarily couples to Gi proteins, inhibiting adenylyl cyclase and decreasing cAMP levels. It is expressed in the retina, skin, osteoblasts, and reticular thalamus, and its activation regulates processes such as circadian phase-shifting, NREM sleep, retinal adaptation, bone metabolism, and glucose homeostasis. MT2 is a therapeutic target for drugs treating insomnia, non-24-hour sleep-wake disorder, depression, and pain.

Other names
Melatonin receptor type 2Melatonin receptor 1BMTNR1B
02

Mechanism of action

Agonism (Ramelteon, Tasimelteon, Agomelatine) leading to Gi protein activation, inhibition of adenylyl cyclase, decreased cAMP, and PKC activation.

03

Biological functions

Signal transductionCircadian rhythm regulationSleep regulationRetinal functionBone metabolismVasodilationGlucose homeostasisNeuromodulation
04

Disease associations

InsomniaNon-24-hour sleep-wake disorderDepressionType 2 Diabetes MellitusPain
05

Safety considerations

Potential side effects related to altered circadian rhythms or sleep patternsIndividual variability in response to MT2-targeting drugs
06

Interacting drugs

Ramelteon

2 more in the full profile.

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