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Agomelatine

Cayman Chemical Item Number 13203

Valdoxan® (CAS 138112-76-2)

Agomelatine (CAS 138112-76-2)

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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.1 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).2 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.2

1 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).

2 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).

Synonyms
  • Valdoxan®
Formal Name N-​[2-​(7-​methoxy-​1-​naphthalenyl)ethyl]-​acetamide
CAS Number 138112-76-2
Molecular Formula C15H17NO2
Formula Weight 243.3
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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COc1ccc2cccc(CCNC(=O)​C)​c2c1

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).

Agomelatine is available in the following screening library:

Size Price Quantity Subtotal
5 mg $61.00 $0.00
10 mg $116.00 $0.00
50 mg $488.00 $0.00
100 mg $854.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

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Pricing updated 2012-05-26. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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