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-106136
    TIK-301
    		Agonist
    TIK-301 (PD-6735) is a chlorinated melatonin derivative and a potent, high-affinity and orally active melatonin MT1 and MT2 receptors agonist with Kis of 0.081 nM and 0.042 nM, respectively. TIK-301 is also a 5-HT2B/5-HT2C receptors antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment.
    TIK-301
  • HY-131947
    DH97-7
    		Antagonist
    DH97 is a potent melatonin receptor 2 (MT2) antagonist with Ki values of 252 nM and 1100 nM for MT2 and MT1, respectively.
    DH97-7
  • HY-100940
    6-Chloromelatonin
    		Agonist
    6-Chloromelatonin is a potent melatonin receptor agonist with greater metabolic stability than melatonin. 6-Chloromelatonin compete for [3H]-melatonin and 2-[125I]-iodomelatonin binding to MT1 receptors (pKi=8.9 and 9.1, respectively). 6-Chloromelatonin compete for [3H]-melatonin binding to MT2 receptors (pKi=9.77).
    6-Chloromelatonin
  • HY-151950
    Antidepressant agent 3
    Antidepressant agent 3 is an orally active antidepressant agent. Antidepressant agent 3 exhibits antidepressant, anxiolytic, performance enhancing and nootropic activities.
    Antidepressant agent 3
  • HY-W744883
    Methyl-d3 Linolenate
    Methyl-d3 Linolenate is the deuterium labeled Methyl linolenate (HY-21268). Methyl linolenate is a polyunsaturated fattly acid (PUFA). Methyl linolenate has an anti-melanogenesis activity with an IC50 of 60 μM. Methyl linolenate can also be used for studies of the mechanisms and prevention of oxidation/peroxidation of unsaturated fatty acids.
    Methyl-d<sub>3</sub> Linolenate
  • HY-116046
    GR 196429
    		Agonist
    GR 196429 is a melatonin receptor agonist with some selectivity for the MT1 subtype. GR 196429 produces both sleep-promoting effects and alterations of circadian rhythm, as well as stimulating melatonin release in mice.
    GR 196429
  • HY-176436S
    GW-117
    GW-117 is a 5-HT2C receptor antagonist and a melatonin (MT1/MT2) receptor agonist. GW-117 shows antidepressant-like and anxiolytic-like effects.
    GW-117
  • 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.
    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. N-Acetyltryptamine is also used for determination of serotonin N-acetyl transferase activity.
    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-101358R
    8-M-PDOT (Standard)
    		Agonist
    8-M-PDOT (Standard) is the analytical standard of 8-M-PDOT (HY-101358). This product is intended for research and analytical applications. 8-M-PDOT (AH-002) is a selective melatonin MT2 receptor agonist. 8-M-PDOT is 5.2-fold selective for MT2 over MT1 receptors. 8-M-PDOT binds human recombinant MT2 and MT2 receptors with pKi values of 8.23 and 8.95 respectively. 8-M-PDOT has anxiolytic-like activity.
    8-M-PDOT (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).
    Tasimelteon-d<sub>5</sub>
  • 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.
    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).
    4-P-PDOT (Standard)
  • HY-A0014S1
    Ramelteon-d3
    		99.0%
    Ramelteon-d3 (TAK-375-d3) is a deuterium-labelled Ramelteon (HY-A0014). 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-d<sub>3</sub>
  • 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. 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues.
    2-Iodomelatonin (Standard)
  • HY-17038AR
    Agomelatine hydrochloride (Standard)
    		Agonist
    Agomelatine (hydrochloride) (Standard) is the analytical standard of Agomelatine (hydrochloride). This product is intended for research and analytical applications. 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. Agomelatine hydrochloride 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 hydrochloride (Standard)
Melatonin Receptor Isoform Comparison

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