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Melatonin Receptor Melatonin Receptor

Cat.No.  Name Information
M14014 S26131 S26131 (compound 5) is a potent and selective MT1 melatoninergic ligand, and the Ki values are 0.5 and 112 nM for MT1 and MT2, respectively. S26131 behaves as an MT1 and MT2 antagonist.
M14013 Agomelatine (L(+)-Tartaric acid) Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively.
M9613 4-P-PDOT 4-P-PDOT is a MT2-receptor-specific antagonist, it is >300-fold more selective for MT2 than MT1.
M6922 Luzindole Luzindole (N-0774) is a selective competitive melatonin MT1/MT2 antagonist with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively.
M6328 2-Phenylmelatonin 2-Phenylmelatonin is a potent melatonin agonist.
M5919 Ramelteon (TAK-375) Ramelteon (TAK-375) is a novel melatonin receptor agonist for human MT1 and MT2 receptors and chick forebrain melatonin receptors with Ki of 14 pM, 112 pM and 23.1 pM, respectively.
M2230 Agomelatine Agomelatine is a metabolically stable analog of melatonin that displays agonist activity for MT1 and MT2 binding with nanomolar affinity. Agomelatine is also a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
M30957 Piromelatine Piromelatine (Neu-P11) is a melatonin MT1/MT2 receptor agonist, serotonin 5-HT1A/5-HT1D agonist, and serotonin 5-HT2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.
M29376 ACH-000143  ACH-000143 is a potent and orally active melatonin receptor agonist, with EC50 values of 0.06 nM and 0.32 nM for MT1 and MT2, respectively.
M8769 Tasimelteon Tasimelteon (BMS-214778) is a Dual Melatonin Receptor Agonist (DMRA) recently approved (Hetlioz) for the treatment of Non-24-hour sleep–wake disorder, a disorder primarily found in the totally blind, where a lack of normal synchronization between the 24-hour light–dark cycle and the endogenous circadian rhythm causes it to drift out of alignment with conventional sleep–wake schedules.

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