| S1204 |
Melatonin
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Melatonin is a MT receptor agonist, used as a dietary supplement. This compound is a selective ATF-6 inhibitor and downregulates COX-2. It enhances mitophagy and regulates the homeostasis of apoptosis and autophagy.
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Antioxidants (Basel), 2025, 14(5)528
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Sci Rep, 2025, 15(1):8451
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Biochem Biophys Res Commun, 2025, 760:151706
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| S1259 |
Ramelteon
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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.
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Aging Cell, 2021, e13375
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Cell Cycle, 2021, 20(12):1195-1208
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Plant Cell Physiol, 2020, 10.1093/pcp/pcaa018
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| S3584 |
Luzindole
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Luzindole (N-0774, N-acetyl-2-benzyltryptamine) is a selective melatonin receptor antagonist with Kis of 179 nM for MT1 and 7.3 nM for MT2, respectively.
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Commun Biol, 2025, 8(1):396
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Aging Cell, 2021, e13375
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Int Immunopharmacol, 2021, 96:107787
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| S4281 |
Tasimelteon
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Tasimelteon (BMS 214778, VEC 162) is a selective dual melatonin receptor (MT1/MT2) agonist with 2.1-4.4 times greater affinity for the MT2 receptor believed to mediate circadian rhythm phase-shifting (Ki = 0.0692 nM and Ki = 0.17 nM in NIH-3T3 and CHOeK1 cells, respectively), than for the MT1 receptor (Ki = 0.304 nM and Ki = 0.35 nM, respectively).
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Cells, 2022, 11(21)3467
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| E6011 |
Agomelatine hydrochloride
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Agomelatine hydrochloride (S-20098 hydrochloride) 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. It is also a selective antagonist of 5-HT2C receptors with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively. Blockade of these receptors enhances adrenergic and dopaminergic transmission in the frontocortical regions.
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