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Agomelatine is an extremely potent agonist at both melatonin receptors (MT1 and MT2), with additional antagonism at 5HT2C. Agomelatine is a novel antidepressant with many desired in vivo properties, including neuroprotection and neurogenesis in depression-sensitive brain areas. Agomelatine abolishes 5-HT2C agonist effects both in cells and in vivo.
Agomelatine also dose dependently increases extracellular levels of noradrenaline and dopamine in frontal cortex of freely moving rats. Agomelatine (25, 50, or 75 mg/kg; i.p.) has antioxidant activity in Strychnine (75 mg/kg, i.p.) or Pilocarpine (400 mg/kg, i.p.) induced seizure models in mice. Agomelatine dose not have any antioxidant effects on parameters of oxidative stress produced by Pentylenetetrazole (PTZ) or Picrotoxin (PTX) induced seizure models when compared to controls.
| Molecular Weight | 243.3 |
| Formula | C15H17NO2 |
| CAS Number | 138112-76-2 |
| Solubility (25°C) | DMSO 60 mg/mL Ethanol 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Melatonin Receptor Products |
|---|
| DH97
DH97 is a potent and selective antagonist of MT2 melatonin receptor, with a pKi of 8.03 for human MT2. |
| 8-M-PDOT
8-M-PDOT (AH-002) is a selective melatonin MT2 receptor agonist. |
| 6-Chloromelatonin
6-Chloromelatonin is a potent melatonin receptor agonist with greater metabolic stability than melatonin. |
| Melatonin-d4
Melatonin-d4 |
| 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. |
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