Pharmacologic agents show effect through the melatonergic system

Pharmacologic agentMechanism of actionApproved indicationsResearch areasReferences
RamelteonMT1 and MT2 agonismInsomnia

Alzheimer’s disease

Delirium

Cancer

[94106]
Agomelatine

MT1 and MT2 agonism

5HT2C antagonism

Major depressive disorder

Anxiety disordersAlzheimer’s disease

Cancer

Endothelial dysfunction

[107133]
Tasimelteon

MT1 and MT2 agonism

SCN pacemaker regulation

Non-24-h sleep-wake disorder

Alzheimer’s disease

Sleep quality

Jet lag

[134136]
Neu-P11/Piromelatine

MT1 and MT2 receptor agonism

5HT1A/1D receptor agonism

None

Sleep disorders

Depression

Anxiety

Alzheimer’s disease

Insulin resistance type 2 diabetes

[137145]
M6B, M7CMT1 and MT2 agonismNone

Panic disorders

Epilepsy

[139, 146]
UCM765Selective MT2 agonismNone

Non-REM sleep disorders

Anxiety

[137, 147, 148]
TIK-301

MT1 and MT2 agonism

5HT2B/5HT2C antagonism

Orphan drug status for circadian rhythm sleep disorders in blind individuals without retinal light exposure

Depression

Epilepsy

[139, 149]