Melatonin Receptor is a G protein-coupled receptor (GPCR) which binds melatonin. Three types of melatonin receptor have been cloned. The MT1 and MT2 receptor subtypes are present in humans and other mammals, while an additional melatonin receptor subtype MT3 has been identified in amphibia and birds. The MT1 subtype's expression in the pars tuberalis of the pituitary gland and suprachiamatic nuclei of the hypothalamus is indicative of melatonin's circadian and reproductive functional involvement. The MT2 subtype's expression in the retina is suggestive of melatonin's effect on the mammalian retina occurring through this receptor. Research suggests that melatonin acts to inhibit the Ca2+-dependent release of dopamine. Melatonin's action in the retina is believed to affect several light-dependent functions, including phagocytosis and photopigment disc shedding.


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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.

  • CAS Number: 896736-21-3
  • MF: C16H21NO3
  • MW: 275.34300
  • Catalog: Melatonin Receptor
  • Density: 1.199g/cm3
  • Boiling Point: 495.171ºC at 760 mmHg
  • Melting Point: 96-98ºC
  • Flash Point: 253.271ºC

7-Desmethyl-3-hydroxyagomelatine

7-Desmethyl-3-hydroxyagomelatine (3-Hydroxy-7-desmethyl agomelatine), a metabolite of Agomelatine, has less activity than Agomelatine[1]. Agomelatine is a melatonergic (MT1 and MT2) agonist and serotonergic (5HT2C) antagonist[1][2].

  • CAS Number: 166527-00-0
  • MF: C14H15NO3
  • MW: 245.2738
  • Catalog: 5-HT Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TIK-301

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[1][2][3].

  • CAS Number: 118702-11-7
  • MF: C14H17ClN2O2
  • MW: 280.750
  • Catalog: 5-HT Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 525.9±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 271.9±30.1 °C

Melatonin D5

Melatonin D5 is deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Antioxidative and anti-inflammatory properties[1][2][3]. Melatonin is a selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation[4].

  • CAS Number: 66521-38-8
  • MF: C13H12D4N2O2
  • MW: 236.30300
  • Catalog: Autophagy
  • Density: 1.196g/cm3
  • Boiling Point: 512.831ºC at 760 mmHg
  • Melting Point: 117-118ºC
  • Flash Point: 263.951ºC

DH 97

DH97 is a potent and selective antagonist of MT2 melatonin receptor, with a pKi of 8.03 for human MT2. DH97 shows 89- and 229-fold selectivity for human MT2 over human mt1 and Xenopus mel1c receptor subtypes. DH97 can inhibit melatonin-induced enhancement of electrically-evoked responses[1][2].

  • CAS Number: 220339-00-4
  • MF: C22H26N2O
  • MW: 334.455
  • Catalog: Melatonin Receptor
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 580.1±38.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 304.6±26.8 °C

Luzindole

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].

  • CAS Number: 117946-91-5
  • MF: C19H20N2O
  • MW: 292.375
  • Catalog: Melatonin Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 559.6±38.0 °C at 760 mmHg
  • Melting Point: 44-46°C
  • Flash Point: 292.2±26.8 °C

Ramelteon-d5

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].

  • CAS Number: 1134159-63-9
  • MF: C16H16D5NO2
  • MW: 264.37
  • Catalog: Melatonin Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GR 128107

GR 128107 is an antagonist of melatonin receptor.

  • CAS Number: 190328-44-0
  • MF: C16H20N2O2
  • MW: 272.34
  • Catalog: Melatonin Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Melatonin receptor agonist 1

Melatonin receptor agonist 1 (compound 20c) is a potent melatonin receptor (MT) agonist, with Ki values of 108 nM (MT2) and 1140 nM (MT1)[1].

  • CAS Number: 2411150-76-8
  • MF: C15H19N3O2
  • MW: 273.33
  • Catalog: Melatonin Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Piromelatine

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].

  • CAS Number: 946846-83-9
  • MF: C17H16N2O4
  • MW: 312.32000
  • Catalog: 5-HT Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

S26131

S26131 (compound 5) is a potent and selective MT1 melatoninergic ligand, and the Ki values are 0.5 and 112 nM for MT1 and MT2, respectively. S26131 behaves as an MT1 and MT2 antagonist[1].

  • CAS Number: 296280-56-3
  • MF: C31H34N2O4
  • MW: 498.61
  • Catalog: Melatonin Receptor
  • Density: 1.168±0.06 g/cm3(Predicted)
  • Boiling Point: 804.6±65.0 °C(Predicted)
  • Melting Point: N/A
  • Flash Point: N/A

S-22153

S-22153 is a potent melatonin receptor antagonist with EC50 values of 19 nM, 4.6 nM for hMT1 and hMT2 melatonin receptor, respectively. S-22153 has Ki values of 8.6 nM (CHO cells) and 16.3 nM (HEK cells) for hMT1, and 6.0 nM (CHO cells) and 8.2 nM (HEK cells) for hMT2. S-22153 is a specific ligand of MT1 and MT2 melatonin receptors subtypes[1][2].

  • CAS Number: 180304-07-8
  • MF: C14H17NOS
  • MW: 247.35600
  • Catalog: Melatonin Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GR 196429

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.

  • CAS Number: 170729-12-1
  • MF: C14H18N2O2
  • MW: 246.3
  • Catalog: Melatonin Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Melatonine

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.

  • CAS Number: 73-31-4
  • MF: C13H16N2O2
  • MW: 232.278
  • Catalog: Autophagy
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 459.8±55.0 °C at 760 mmHg
  • Melting Point: 116.5-118 °C(lit.)
  • Flash Point: 231.9±31.5 °C

Ramelteon

Ramelteon is a highly potent and selective melatonin receptor agonist with Ki values of 14 and 112 pM for human melatonin1 and melatonin2.

  • CAS Number: 196597-26-9
  • MF: C16H21NO2
  • MW: 259.343
  • Catalog: Melatonin Receptor
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 455.3±24.0 °C at 760 mmHg
  • Melting Point: 113-115ºC
  • Flash Point: 229.2±22.9 °C

Agomelatine D6

Agomelatine D6 (S-20098 D6) is deuterium labeled Agomelatine. Agomelatine is a specific agonist of MT1 and MT2 receptors[1] .

  • CAS Number: 1079389-42-6
  • MF: C15H11D6NO2
  • MW: 249.33800
  • Catalog: 5-HT Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-Iodomelatonin

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].

  • CAS Number: 93515-00-5
  • MF: C13H15IN2O2
  • MW: 358.17500
  • Catalog: Melatonin Receptor
  • Density: 1.63g/cm3
  • Boiling Point: 574.5ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 301.3ºC

6-Chloromelatonin

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)[1][2].

  • CAS Number: 63762-74-3
  • MF: C13H15ClN2O2
  • MW: 266.72300
  • Catalog: Melatonin Receptor
  • Density: 1.272g/cm3
  • Boiling Point: 536.7ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 278.4ºC

UCM 608

UCM 608 is a high affinity melatonin (MT) membrane receptor agonist. The pKi values for MT1 and MT2 are 10.7 and 10.4[1][2].

  • CAS Number: 151889-03-1
  • MF: C19H20N2O2
  • MW: 308.37
  • Catalog: Melatonin Receptor
  • Density: 1.172g/cm3
  • Boiling Point: 612.4ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 324.2ºC

8-M-PDOT

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[1][2].

  • CAS Number: 134865-70-6
  • MF: C14H19NO2
  • MW: 233.30600
  • Catalog: Melatonin Receptor
  • Density: 1.09g/cm3
  • Boiling Point: 447.8ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 224.6ºC

Tasimelteon

Tasimelteon is a melatonin MT1 and MT2 receptor agonist.Target: melatonin receptorTasimelteon is a novel circadian regulator, is the first product for the treatment of Non-24-hour Sleep-Wake Disorder (Non-24) approved by either the FDA or the European Medicines Agency (EMA). Tasimelteon is a potent and specific melatonin (MT1 and MT2) receptor agonist with 2 - 4 times greater affinity for the MT2 receptor.

  • CAS Number: 609799-22-6
  • MF: C15H19NO2
  • MW: 245.317
  • Catalog: Melatonin Receptor
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 442.6±24.0 °C at 760 mmHg
  • Melting Point: 78°C(lit.)
  • Flash Point: 221.4±22.9 °C

4-P-PDOT

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].

  • CAS Number: 134865-74-0
  • MF: C19H21NO
  • MW: 279.37600
  • Catalog: Melatonin Receptor
  • Density: 1.11g/cm3
  • Boiling Point: 480.1ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 292ºC