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-105285
    Piromelatine
    		Agonist 99.54%
    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
  • HY-103005S
    Ramelteon metabolite M-II-d3
    		Activator ≥99.0%
    Ramelteon metabolite M-II-d3 is the deuterium labeled Ramelteon metabolite M-II. Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1 or MT2). Ramelteon is a selective melatonin agonist[1][2].
    Ramelteon metabolite M-II-d<sub>3</sub>
  • HY-100908
    N-Acetyltryptamine
    		Agonist
    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
  • HY-103005
    Ramelteon metabolite M-II
    		Activator 98.24%
    Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1 or MT2). Ramelteon is a selective melatonin agonist.
    Ramelteon metabolite M-II
  • HY-B0075S2
    Melatonin-d7
    		Activator ≥98.0%
    Melatonin-d7 is the deuterium labeled Melatonin (HY-B0075). Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress.
    Melatonin-d<sub>7</sub>
  • HY-17038S1
    Agomelatine-d4
    		Agonist
    Agomelatine-d4 is the deuterium labeled Agomelatine. 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[1]. 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[2].
    Agomelatine-d<sub>4</sub>
  • HY-147542
    Melatonin receptor agonist 1
    		Agonist
    Melatonin receptor agonist 1 (compound 20c) is a potent melatonin receptor (MT) agonist, with Ki values of 108 nM (MT2) and 1140 nM (MT1).
    Melatonin receptor agonist 1
  • HY-119010
    UCM 549
    		Modulator
    UCM 549 is a melatonin MT2 receptor inverse agonist and a MT1 receptor antagonist.
    UCM 549
  • HY-101303
    5-MCA-NAT
    		Agonist
    5-MCA-NAT is a melatonin agonist that may target the melatoninMT3 receptor. 5-MCA-NAT can contract the colonic band in a concentration-dependent manner and reduce intraocular pressure (IOP) in glaucomatous monkey eyes, inhibiting the increase in IOP.
    5-MCA-NAT
  • HY-A0014S
    Ramelteon-d5
    		Agonist
    Ramelteon-d5 is deuterium labeled Ramelteon. 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[1][2].
    Ramelteon-d<sub>5</sub>
  • HY-133112
    7-Desmethyl-3-hydroxyagomelatine
    		Agonist
    7-Desmethyl-3-hydroxyagomelatine (3-Hydroxy-7-desmethyl agomelatine), a metabolite of Agomelatine, has less activity than Agomelatine. Agomelatine is a melatonergic (MT1 and MT2) agonist and serotonergic (5HT2C) antagonist.
    7-Desmethyl-3-hydroxyagomelatine
  • HY-17038S2
    Agomelatine-d3
    		Agonist ≥98.0%
    Agomelatine-d3 is the deuterium labeled Agomelatine. 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[1]. 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[2].
    Agomelatine-d<sub>3</sub>
  • HY-151951
    Antidepressant agent 4
    Antidepressant agent 4 is an orally active antidepressant agent. Antidepressant agent 4 exhibits antidepressant, anxiolytic, performance enhancing and nootropic activities.
    Antidepressant agent 4
  • 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-116930
    S-20928
    		Antagonist
    S-20928 is an antagonist for melatonin receptor through inhibition of binding of melatonin to its receptors. S-20928 enhances the 2-Deoxy-D-glucose (2DG) (HY-13966)-induced increase in blood glucose and glucagon levels in rats brain.
    S-20928
  • 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-A0014S1
    Ramelteon-d3
    		≥99.0%
    Ramelteon-d3 is a deuterium-labelled Ramelteon (HY-A0014).
    Ramelteon-d<sub>3</sub>
  • 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-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
Melatonin Receptor Isoform Comparison

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