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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 |
|---|
| Melatonin
Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation. |
| Ramelteon (TAK-375)
Ramelteon (TAK-375) is a novel melatonin receptor agonist for human MT1 and MT2 receptors and chick forebrain melatonin receptors with Ki of 14 pM, 112 pM and 23.1 pM, respectively. |
| 2-Phenylmelatonin
2-Phenylmelatonin is a potent melatonin agonist. |
| Luzindole
Luzindole (N-0774) is a selective competitive melatonin MT1/MT2 antagonist with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. |
| Tasimelteon
Tasimelteon (BMS-214778) is a Dual Melatonin Receptor Agonist (DMRA) recently approved (Hetlioz) for the treatment of Non-24-hour sleep–wake disorder, a disorder primarily found in the totally blind, where a lack of normal synchronization between the 24-hour light–dark cycle and the endogenous circadian rhythm causes it to drift out of alignment with conventional sleep–wake schedules. |
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