Target intelligence / Profile preview

Melatonin Receptor MT1 (MT1)

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

Overview

The human Melatonin Receptor MT1 is a GPCR crucially involved in regulating circadian rhythms—especially REM sleep—and modulating mood through inhibitory signaling pathways primarily mediated by Gi proteins. Its distinct anatomical distribution underlies its specialized physiological roles. Ongoing research aims at developing selective drugs targeting this receptor subtype for improved treatment outcomes across multiple neuropsychiatric conditions.

Other names
Melatonin receptor type 1MTNR1AMelatonin receptor 1A
02

Mechanism of action

Agonist binding inhibits adenylate cyclase activity, leading to decreased intracellular cAMP levels and subsequent downstream effects.

03

Biological functions

Signal transductionCircadian rhythm regulationSleep regulationInhibition of adenylate cyclaseRegulation of potassium conductance
04

Disease associations

InsomniaDepressionAnxiety DisordersAlzheimer's disease (possible)Huntington's disease (possible)Addiction (possible)
05

Safety considerations

Potential for limited efficacy of mixed MT1/MT2 ligands due to opposing roles between subtypes.Age-related decrease in expression may impact therapeutic efficacy.
06

Interacting drugs

Melatonin

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