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MT Receptor

Melatonin receptors are G protein-coupled receptors (GPCR) which bind melatonin. Three types of melatonin receptors have been cloned. The MT1 (or Mel1A or MTNR1A) and MT2 (or Mel1B or MTNR1B) receptor subtypes are present in humans and other mammals, while an additional melatonin receptor subtype MT3 (or Mel1C or MTNR1C) has been identified in amphibia and birds. The receptors are crucial in the signal cascade of melatonin. In the field of chronobiology, melatonin has been found to be a key player in the synchrony of biological clocks. Melatonin secretion by the pineal gland has circadian rhythmicity regulated by the suprachiasmatic nucleus (SCN) found in the brain. The SCN functions as the timing regulator for melatonin; melatonin then follows a feedback loop to decrease SCN neuronal firing. The receptors MT1 and MT2 control this process. Melatonin receptors are found throughout the body in places such as the brain, the retina of the eye, the cardiovascular system, the liver and gallbladder, the colon, the skin, the kidneys, and many others.

  • Agomelatine hydrochloride
    T605231176316-99-6In house
    Agomelatine hydrochloride (S-20098 hydrochloride) (S-20098 hydrochloride) is a specific MT1 and MT2 receptor agonist with Ki of 0.1 nM for CHO-hMT1, 0.06 nM for HEK-hMT1, 0.12 nM for CHO-hMT2, and 0.27 nM for HEK-hMT2, respectively [1]. Agomelatine hydrochloride is a selective antagonist of a 5-HT2C receptor with pKis of 6.4 and 6.2 for native (porcine) and cloned, human 5-HT2C receptors, respectively [2].
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  • glycine
    T2O272856-40-6
    glycine (2-Aminoacetic acid) is a non-essential amino acid. It is found primarily in gelatin and silk fibroin and used therapeutically as a nutrient. It is also a fast inhibitory neurotransmitter.
    • $41
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  • ACH-000143
    T91932225836-30-4
    ACH-000143 have been identified as a novel agonist of the melatonin receptors MT1 and MT2.
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  • Tasimelteon
    T3495609799-22-6
    Tasimelteon (BMS-214778) is a melatonin receptor agonist that is used for the treatment of non-24 hour sleep-wake disorder in blind individuals.
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  • Luzindole
    T15795117946-91-5
    Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole inhibits experimental autoimmune encephalomyelitis and exerts antidepressant-like activity. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively.
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  • 4-P-PDOT
    T14042134865-74-0
    4-P-PDOT (4-phenyl-2- propionamidotetralin) is a potent, selective and affinity Melatonin receptor (MT2) antagonist.
    • $31
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  • 8-M-PDOT
    T10198134865-70-6
    8-M-PDOT (AH-002) is a selective and potent melatonin MT2 receptor agonist that also inhibits MT1 receptors.8-M-PDOT has anxiolytic activity and may be used to study MT2-induced neuropathic pain.
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  • Ramelteon
    T1463196597-26-9
    Ramelteon (TAK-375) is a Melatonin Receptor Agonist. The mechanism of action of ramelteon is as a Melatonin Receptor Agonist.
    • $37
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  • S26131
    T16834296280-56-3
    S26131 (N-[2-[7-[3-[8-(2-acetamidoethyl)naphthalen-2-yl]oxypropoxy]naphthalen-1-yl]ethyl]acetamide) behaves as an antagonist on MT1 and MT2 receptors with Ki of 0.5 and 112 nM respectively.
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  • Piromelatine
    T34081946846-83-9
    Piromelatine is an agonist of melatonin MT1/MT2 receptors, 5-HT1A and 5-HT1D, and an antagonist of 5-HT2B.Piromelatine has antinociceptive activity with inhibitory effects on P2X3, TRPV1, and Nav1.7 channels, and can be used in studies of sleep-promoting, pain-relieving, anti-neurodegenerative, and antidepressant diseases. diseases, and can be used to improve memory deficits associated with chronic mild stress-induced lack of pleasure in rats.
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