2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Melatonin Receptor

Melatonin Receptor

Melatonin Receptor

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Melatonin receptors belong to the G protein-coupled receptor superfamily, which preferentially couple to Gαi/o proteins. The melatonin receptor subfamily is composed of three members in mammals: MT1 and MT2, which are both binding to the neurohormone melatonin with high affinity, and GPR50, which shows high sequence homology to MT1 and MT2 but does not bind to melatonin or any other known ligand.

MT1 and MT2 are involved in various biological functions including the regulation of biological rhythms, sleep, pain, retinal, neuronal and immune functions. Alteration of melatonin receptor function or expression in humans is associated with depression, Alzheimer’s disease and type 2 diabetes.

Melatonin Receptor Isoform Specific Products:

Melatonin Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-101254R
    Luzindole (Standard)
    		Antagonist
    Luzindole (Standard) is the analytical standard of Luzindole. This product is intended for research and analytical applications. Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity[1][2][3].
    Luzindole (Standard)
  • HY-100908R
    N-Acetyltryptamine (Standard)
    		Agonist
    N-Acetyltryptamine (Standard) is the analytical standard of N-Acetyltryptamine. This product is intended for research and analytical applications. N-Acetyltryptamine is a partial agonist for melatonin receptors in the retina[1]. N-Acetyltryptamine is also used for determination of serotonin N-acetyl transferase activity[2].
    N-Acetyltryptamine (Standard)
  • HY-A0014R
    Ramelteon (Standard)
    		Agonist
    Ramelteon (Standard) is the analytical standard of Ramelteon. This product is intended for research and analytical applications. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation.
    Ramelteon (Standard)
  • HY-103005R
    Ramelteon metabolite M-II (Standard)
    		Activator
    Amlodipine (maleate) (Standard) is the analytical standard of Amlodipine (maleate). This product is intended for research and analytical applications. Amlodipine maleate is a dihydropyridine calcium channel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer.
    Ramelteon metabolite M-II (Standard)
  • HY-17038B
    Agomelatine (L(+)-Tartaric acid)
    		Agonist 99.82%
    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. Agomelatine L(+)-Tartaric acid is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
    Agomelatine (L(+)-Tartaric acid)
  • HY-14803S
    Tasimelteon-d5
    		Agonist
    Tasimelteon-d5 is the deuterium labeled Tasimelteon. Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24)[1][2].
    Tasimelteon-d<sub>5</sub>
  • HY-P2092
    Cyclo(L-leucyl-L-tryptophyl)
    		Agonist
    Cyclo(L-leucyl-L-tryptophyl) (Cyclo(-Leu-Trp)) is a cyclic dipeptide that inhibits a various of bacteria and fungi. Cyclo(L-leucyl-L-tryptophyl) is a melatonin receptor agonist and is also used as a bitter ligand.
    Cyclo(L-leucyl-L-tryptophyl)
  • HY-17038R
    Agomelatine (Standard)
    		Agonist
    Agomelatine (Standard) is the analytical standard of Agomelatine. This product is intended for research and analytical applications. Agomelatine (S-20098) 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. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
    Agomelatine (Standard)
  • HY-I0603
    (R)-Ramelteon
    		Control
    (R)-Ramelteon ((R)-TAK-375) is an orally active inactive isomer of the melatonin receptor 1 and 2. (R)-Ramelteon is promising for research of regulating sleep.
    (R)-Ramelteon
  • HY-105285R
    Piromelatine (Standard)
    		Agonist
    Piromelatine (Standard) is the analytical standard of Piromelatine. This product is intended for research and analytical applications. 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[1][2][3].
    Piromelatine (Standard)
  • HY-100609R
    4-P-PDOT (Standard)
    		Antagonist
    4-P-PDOT (Standard) is the analytical standard of 4-P-PDOT. This product is intended for research and analytical applications. 4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity)[1][2][3][4].
    4-P-PDOT (Standard)
  • HY-107628
    N-Pentanoyl 2-benzyltryptamine
    		Antagonist
    N-Pentanoyl 2-benzyltryptamine is a potent and selective antagonist of MT2 melatonin receptor, with a pKi of 8.03 for human MT2. N-Pentanoyl 2-benzyltryptamine shows 89- and 229-fold selectivity for human MT2 over human mt1 and Xenopus mel1c receptor subtypes. N-Pentanoyl 2-benzyltryptamine can inhibit melatonin-induced enhancement of electrically-evoked responses.
    N-Pentanoyl 2-benzyltryptamine
  • HY-101176R
    2-Iodomelatonin (Standard)
    		Agonist
    2-Iodomelatonin (Standard) is the analytical standard of 2-Iodomelatonin. This product is intended for research and analytical applications. 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[1]. 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues[1].
    2-Iodomelatonin (Standard)
  • HY-120182
    GR 128107
    		Antagonist
    GR 128107 is a competitive melatonin receptor antagonist (pKi: 9.6).
    GR 128107
  • HY-14803R
    Tasimelteon (Standard)
    		Agonist
    Tasimelteon (Standard) is the analytical standard of Tasimelteon. This product is intended for research and analytical applications. Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24).
    Tasimelteon (Standard)
  • HY-159848
    Nedemelteon
    		Agonist
    Nedemelteon is a melatonin receptor agonist.
    Nedemelteon
  • HY-U00271
    Pareptide monohydrochloride
    Pareptide monohydrochloride is a melanotropin-inhibiting factor (MIF) metabolically stable analogue.
    Pareptide monohydrochloride
Melatonin Receptor Isoform Comparison

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