Agomelatine hydrochloride
Others
Agomelatine hydrochloride is a antidepressant, which is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor.IC50 value: 6.2 (pKi, 5-HT2c); 6.6 (pKi, 5-HT2b)Target: 5-HT 2c receptorAgomelatine hydrochloride is an antidepressant drug. It is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor. Activation of 5-HT2C receptors by serotonin inhibits dopamine and norepinephrine release. Antagonism of 5-HT2C results in an enhancement of DA and NE release and activity of frontocortical dopaminergic and adrenergic pathways [1].A total of 42 rats were divided into 7 groups as each composed of 6 rats: (1) intact, (2) 40 mg/kg agomelatine, (3) 140 mg/kg N-acetylcysteine (NAC), (4) 2 g/kg paracetamol, (5) 2 g/kg paracetamol + 140 mg/kg NAC, (6) 2 g/kg paracetamol + 20 mg/kgagomelatine, and (7) 2 g/kg paracetamol + 40 mg/kg agomelatine groups. Paracetamol-induced hepatotoxicity was applied and liver and blood samples were analyzed histopathologically and biochemically. There were statistically significant increases in the activities of aspartate aminotransferase, alanine aminotransferase, levels of tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6) and 8-iso-prostane, and decreases in the activity of superoxide dismutase and level of glutathione in the group treated with paracetamol. Administration of agomelatine and NAC separately reversed these changes significantly [2].Clinical indications: Depression; Obsessive compulsive disorderFDA Approved Date: October 2011Toxicity: Hyperhidrosis; Abdominal pain; Nausea; Vomiting; Diarrhoea; Constipation; Back pain; Fatigue
279.76
Formulation:
279.76
Source:
Usage:
Agomelatine hydrochloride
The product is for non-human research only. Not for therapeutic or veterinary use.
Catalog Number: BT-253104
CAS Number: 1176316-99-6
Molecular Formula: C15H18ClNO2
Molecular Weight: 279.76
Purity: ≥ 99%
Inventory: In Stock
| Size | SKU | Price | |
|---|---|---|---|
| 5mg | bt-253104-5mg | $301.85 | |
| 10mg | bt-253104-10mg | $468.31 |
| CAS Number | 1176316-99-6 |
|---|---|
| Product Name | Agomelatine hydrochloride |
| Molecular Formula | C15H18ClNO2 |
| Molecular Weight | 279.76 |
| InChI | InChI=1S/C15H17NO2.ClH/c1-11(17)16-9-8-13-5-3-4-12-6-7-14(18-2)10-15(12)13;/h3-7,10H,8-9H2,1-2H3,(H,16,17);1H |
| IUPAC Name | N-[2-(7-methoxynaphthalen-1-yl)ethyl]acetamide;hydrochloride |
| Description | Agomelatine hydrochloride is a antidepressant, which is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor.IC50 value: 6.2 (pKi, 5-HT2c); 6.6 (pKi, 5-HT2b)Target: 5-HT 2c receptorAgomelatine hydrochloride is an antidepressant drug. It is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor. Activation of 5-HT2C receptors by serotonin inhibits dopamine and norepinephrine release. Antagonism of 5-HT2C results in an enhancement of DA and NE release and activity of frontocortical dopaminergic and adrenergic pathways [1].A total of 42 rats were divided into 7 groups as each composed of 6 rats: (1) intact, (2) 40 mg/kg agomelatine, (3) 140 mg/kg N-acetylcysteine (NAC), (4) 2 g/kg paracetamol, (5) 2 g/kg paracetamol + 140 mg/kg NAC, (6) 2 g/kg paracetamol + 20 mg/kgagomelatine, and (7) 2 g/kg paracetamol + 40 mg/kg agomelatine groups. Paracetamol-induced hepatotoxicity was applied and liver and blood samples were analyzed histopathologically and biochemically. There were statistically significant increases in the activities of aspartate aminotransferase, alanine aminotransferase, levels of tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6) and 8-iso-prostane, and decreases in the activity of superoxide dismutase and level of glutathione in the group treated with paracetamol. Administration of agomelatine and NAC separately reversed these changes significantly [2].Clinical indications: Depression; Obsessive compulsive disorderFDA Approved Date: October 2011Toxicity: Hyperhidrosis; Abdominal pain; Nausea; Vomiting; Diarrhoea; Constipation; Back pain; Fatigue |
| SMILES | CC(=O)NCCC1=CC=CC2=C1C=C(C=C2)OC.Cl |
| Synonyms | (Z)-N-(2-(7-methoxynaphthalen-1-yl)ethyl)acetimidic acid hydrochloride |
| Reference | [1]. Chenu F, et al. Role of melatonin, serotonin 2B, and serotonin 2C receptors in modulating the firing activity of rat dopamine neurons. J Psychopharmacol. 2013 Nov 4. [2]. Karakus E, et al. Agomelatine: an antidepressant with new potent hepatoprotective effects on paracetamol-induced liver damage inrats. Hum Exp Toxicol. 2013 Aug;32(8):846-57. |
| PubChem Compound | Agomelatine hydrochloride |
| Last Modified | May 15 2022 |