A melatonin receptor agonist (Kis = 0.14 and 0.41 nM for MT1 and MT2

Agomelatine – 5 mg

Brand:
Cayman
CAS:
138112-76-2
Storage:
-20
UN-No:
De Minimis - 3077 / 9

Agomelatine is an agonist of melatonin (MT) receptors and a derivative of melatonin (Item No. 14427).{53599} It binds to MT1 and MT2 receptors (Kis = 0.14 and 0.41 nM, respectively) and has an EC50 value of 0.1 nM in a [35S]GTPγS binding assay using CHO cells expressing MT2 receptors. Agomelatine is also an antagonist of the serotonin (5-HT) receptor subtypes 5-HT2B and 5-HT2C (Kis = 0.26 and 0.71 nM, respectively, for the human receptors).{16799} Agomelatine (40 mg/kg) inhibits the penile erection response induced by the 5-HT2 agonist Ro 60-0175 (Item No. 29500) in rats. It also increases extracellular levels of noradrenaline and dopamine in the frontal cortex of freely moving rats when administered at doses ranging from 20 to 80 mg/kg. Agomelatine (10 mg/kg) reduces immobility time in the forced swim test and increases the amount of time spent in the open arms of the elevated plus maze in mice, indicating antidepressant-like and anxiolytic-like activity, in a transgenic neuroendocrine model of depression.{53600} It also increases the rate of readjustment to circadian activity cycles following an induced phase shift.  

 

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Description

A melatonin receptor agonist (Kis = 0.14 and 0.41 nM for MT1 and MT2, respectively) and 5-HT2B and 5-HT2C antagonist (Kis = 0.26 and 0.71 nM, respectively); inhibits the 5-HT2-mediated penile erection response in rats at 40 mg/kg; increases extracellular levels of noradrenaline and dopamine in the frontal cortex of freely moving rats at 20-80 mg/kg; reduces immobility time in the forced swim test and increases the amount of time spent in the open arms of the elevated plus maze in mice in a transgenic neuroendocrine model of depression at 10 mg/kg

Formal name: N-[2-(7-methoxy-1-naphthalenyl)ethyl]-acetamide

Synonyms:  S20098

Molecular weight: 243.3

CAS: 138112-76-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Behavioral Neuroscience|Anxiety||Research Area|Neuroscience|Behavioral Neuroscience|Depression||Research Area|Neuroscience|Behavioral Neuroscience|Sleep & Biological Rhythms

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