Agomelatine
Synonyms: Valdoxan ®
Formal Name: N-[2-(7-methoxy-1-naphthalenyl)ethyl]-acetamide
CAS Number: 138112-76-2
Molecular Formula: C15H17NO2
Formula Weight: 243.3[g/mol]
Stability: 2 years
Storage: -20°C
Purity: 99.0%min (HPLC)
SMILES: COc1ccc2cccc(CCNC(=O)C)c2c1
STOCK: Yes
Min Order Qty: 1KG
Price: ****/KG FOR 1KG
Description:
Melatonin, produced in the pineal gland, is an endogenous regulator of circadian rhythms. It acts through the melatonin receptors (MT1 and MT2) and has been shown to have anti-depressant activity in experimental models of clinical depression. Agomelatine is a metabolically stable analog of melatonin that displays agonist activity for MT1 and MT2 binding with nanomolar affinity. However, unlike melatonin, agomelatine is a competitive antagonist of human and porcine serotonin (5-HT2C) receptors (pKi = 6.2 and 6.4, respectively) as well as human 5-HT2B receptors (pKi = 6.6). Agomelatine abolishes 5-HT2C agonist effects both in cells and in vivo. It also dose dependently increases extracellular levels of noradrenaline and dopamine in frontal cortex of freely moving rats.
Background Reading:
Yous, S., Andrieux, J., Howell, H.E., et al. Novel naphthalenic ligands with high affinity for the melatonin receptor. J Med Chem 35(8) 1484-1486(1992).
Millan, M.J., Gobert, A., Lejeune, F., et al. The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways. J Pharmacol Exp Ther 306(3)954-964 (2003)
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