Agomelatine-d4
Product Specifications
UNSPSC Description
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].
Target Antigen
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 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.
Shipping Conditions
Room temperature
Clinical Information
No Development Reported
CAS Number
1079389-44-8
Available Sizes
Curated Selection
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