|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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