Home Neuronal Signaling 5-HT Receptor antagonist Agomelatine (S20098)

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Agomelatine (S20098) 5-HT Receptor antagonist

Cat.No.S1243

Agomelatine (Valdoxan, Melitor, Thymanax, S20098) is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor.
Agomelatine (S20098) 5-HT Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 243.3

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Quality Control

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK 293 Function assay Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand, Ki=6e-05 μM
CHO cells Function assay 120 mins Displacement of [125I]iodomelatonin form human MT1 receptor expressed in CHO cells after 120 mins, Ki=0.1 nM
CHO-Galpha16 cells Function assay 20 mins Binding affinity to rat MT1 receptor expressed in CHO-Galpha16 cells assessed as Ca2+ mobilization after 20 mins by FLIPR assay, EC50=2.1 nM
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Chemical Information, Storage & Stability

Molecular Weight 243.3 Formula

C15H17NO2

 Storage (From the date of receipt)
CAS No. 138112-76-2 Download SDF Storage of Stock Solutions

Synonyms Valdoxan, Melitor, Thymanax,S20098 Smiles CC(=O)NCCC1=CC=CC2=C1C=C(C=C2)OC

Solubility

In vitro
Batch:

DMSO : 48 mg/mL ( (197.28 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 48 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
5-HT2C [1]
In vitro

In rats subjected to chronic footshock stress, Agomelatine (S20098) completely normalizes stress-affected cell survival and partly reverses reduced doublecortin expression in the hippocampus. [1]
In vivo

Agomelatine (S20098) is effective in reversing the transgenic mouse behavioural changes noted in the Porsolt forced swim test as well as in the elevated plus maze. It also markedly accelerates readjustment of circadian cycles of temperature and activity following an induced phase shift. [2] This compound enhances cell proliferation and neurogenesis in the ventral hippocampus (VH) of adult rats, a region pertinent to mood disorders. It increases the ratio of mature vs immature neurons and enhances neurite outgrowth of granular cells in adult rats, suggesting an acceleration of maturation. Agomelatine also activates several cellular signals (extracellular signal-regulated kinase1/2, protein kinase B, and glycogen synthase kinase 3beta) known to be modulated by antidepressants and implicated in the control of proliferation/survival. [3] It enhances the time devoted to active social interaction in unfamiliar pairs of rats exposed to a novel environment. [4] The compound increases cell proliferation and neurogenesis in the ventral dentate gyrus of rats, a region notably implicated in response to emotion, which is consistent with its antidepressant-anxiolytic properties. It increases survival of newly formed neurons in the entire dentate gyrus of rats. [5]
References
  • https://pubmed.ncbi.nlm.nih.gov/15289999/
  • https://pubmed.ncbi.nlm.nih.gov/16499883/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06120543 Not yet recruiting
Polymorphism Genetic|Depression|CYP1A2 Polymorphism|CYP2C9 Polymorphism|Polymerase Chain Reaction|Plasma Concentration
Affiliated Hospital of Nantong University
 October 31 2023 --
NCT05323994 Recruiting
Depression|COVID-19
Servier Russia
 April 19 2022 --
NCT03977441 Unknown status
Parkinson Disease|Depression|Sleep Disorders|Circadian Rhythm Disorders
Second Affiliated Hospital of Soochow University
 July 2019 Phase 4
NCT00463242 Completed
Major Depressive Disorder
Novartis
 March 2007 Phase 3

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