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Agomelatine-d3

Product Specifications

UNSPSC Description

Agomelatine-d3 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively[1]. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively[2].

Target Antigen

5-HT Receptor; Endogenous Metabolite; Melatonin Receptor

Type

Isotope-Labeled Compounds

Related Pathways

GPCR/G Protein;Metabolic Enzyme/Protease;Neuronal Signaling

Field of Research

Neurological Disease

Purity

98.0

Solubility

10 mM in DMSO

Smiles

[2H]C([2H])([2H])C(NCCC1=CC=CC2=C1C=C(OC)C=C2)=O

Molecular Weight

246.32

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. |[2]Audinot V, et al. New selective ligands of human cloned melatonin MT1 and MT2 receptors. Naunyn Schmiedebergs Arch Pharmacol. 2003 Jun;367(6):553-61.|[3]Millan MJ, 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. 2003 Sep;306(3):954-64.|[4]Aguiar CC, et al. Effects of agomelatine on oxidative stress in the brain of mice after chemically induced seizures. Cell Mol Neurobiol. 2013 Aug;33(6):825-35.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Clinical Information

No Development Reported

CAS Number

1079389-38-0

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