Melatonin Receptors

Melatonin is a endogenous hormone that acts as an agonist at melatonin receptors MT1 and MT2.

Ramelteon is a melatonin receptor agonist with both high affinity for melatonin MT1 (IC50 =28.5 ?? 8.55 pM)and MT2 (20.1 ?? 9.25 pM)receptors and selectivity over the MT3 receptor.

Tasimelteon is a melatonin MT1 and MT2 receptor agonist.

Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1 or MT2). Ramelteon is a selective melatonin agonist.

AP1189 is a biased agonist at receptors MC1 and MC3. AP1189 reduced cytokine release, an effect reliant on both MC1 and MC3 as evident from the use of Mc1r(-/-) and Mc3r(-/-) macrophages.

ACH-000143 is a potent and peripherally preferred melatonin receptor agonist.