Melatonin Receptor

6-Chloromelatonin is a potent melatonin receptor agonist, a 5-methoxyindole compound that competes for the same presynaptic melatonin receptor sites in the rabbit retina and inhibits the calcium-dependent release of [3H]dopamine with a higher metabolic stability than melatonin. Chloromelatonin competes for [3H]melatonin binding to MT2 receptors (pKi=9.77) and may be used to study insomnia and sleep disorders associated with depression.

2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, it is more 5-fold selective for MT1 over MT2. 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues.

Melatonin (Melatonine) is a biogenic amine that is found in animals and plants. In mammals, melatonin is produced by the PINEAL GLAND. Its secretion increases in darkness and decreases during exposure to light. Melatonin is implicated in the regulation of SLEEP, mood, and REPRODUCTION. Melatonin is also an effective antioxidant.

ACH-000143 have been identified as a novel agonist of the melatonin receptors MT1 and MT2.

Tasimelteon (BMS-214778) is a melatonin receptor agonist that is used for the treatment of non-24 hour sleep-wake disorder in blind individuals.

Agomelatine (Valdoxan) is structurally closely related to melatonin. Agomelatine is a potent agonist at melatonin receptors and an antagonist at serotonin-2C (5-HT2C) receptors, tested in an animal model of depression.

Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole inhibits experimental autoimmune encephalomyelitis and exerts antidepressant-like activity. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively.

4-P-PDOT (4-phenyl-2- propionamidotetralin) is a potent, selective and affinity Melatonin receptor (MT2) antagonist.

Ramelteon (TAK-375) is a Melatonin Receptor Agonist. The mechanism of action of ramelteon is as a Melatonin Receptor Agonist.

N-ACETYLTRYPTAMINE is a partial agonist for melatonin receptors in the retina. Also used for determination of serotonin N-acetyl transferase.