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-120182
    GR 128107
    		Antagonist
    GR 128107 is a competitive melatonin receptor antagonist (pKi: 9.6).
    GR 128107
  • HY-113440R
    5-Methoxytryptophol (Standard)
    		Activator
    5-Methoxytryptophol (Standard) is the analytical standard of 5-Methoxytryptophol. This product is intended for research and analytical applications. 5-Methoxytryptophol is a 5-methoxyindole alcohol structurally homologous to Melatonin (HY-B0075). It is secreted by the mammalian pineal gland and exhibits an inverse circadian rhythm. 5-Methoxytryptophol regulates bone metabolism by activating the ERK1/2 pathway. It reduces the levels of pro-inflammatory cytokines TNF-α and IL-1β, as well as proteolytic enzymes MMP-1 and MMP-2, in serum and dental pulp tissues, thereby ameliorating acute pulpitis. 5-Methoxytryptophol induces rapid sleep in mice, while high doses cause respiratory depression and death. 5-Methoxytryptophol. 5-Methoxytryptophol can be used in studies related to acute pulpitis, hypnosis, and bone metabolism.
    5-Methoxytryptophol (Standard)
  • HY-101074R
    UCM 608 (Standard)
    		Agonist
    UCM 608 (Standard) is the analytical standard of UCM 608 (HY-101074). This product is intended for research and analytical applications. UCM 608 is a high affinity melatonin (MT) membrane receptor agonist. The pKi values for MT1 and MT2 are 10.7 and 10.4.
    UCM 608 (Standard)
  • 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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