Agomelatine-d4

Agomelatine-d4 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].

Product Specifications

CAS Number

[1079389-44-8]

Product Name Alternative

S-20098-d4

UNSPSC

12352005

Target

5-HT Receptor; Endogenous Metabolite; Isotope-Labeled Compounds; Melatonin Receptor

Type

Isotope-Labeled Compounds

Related Pathways

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

Field of Research

Neurological Disease

Solubility

10 mM in DMSO

Smiles

CC(NC([2H])([2H])C([2H])([2H])C1=CC=CC2=C1C=C(OC)C=C2)=O

Molecular Formula

C15H13D4NO2

Molecular Weight

247.33

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.