MT1 agonist
MT1 melatonin receptor agonist
- Suppresses the wake-promoting circadian signal → sleep initiation
- The arm most tied to falling asleep
- Promotes sleep initiation
- Modulates reproductive hormones
- Vasoconstriction
- ➔ the balance between MT1 and MT2 (vasodilation) regulates tissue perfusion
- ➔ MT1 effects dominant during sleep onset
Drugs with this mechanism (3)
- Melatonin — OTC pineal hormone used for sleep and circadian shifting.
- Ramelteon — Melatonin-receptor hypnotic with no abuse potential.
- Tasimelteon — Melatonin agonist for non-24-hour sleep-wake disorder in the blind.
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