| Identification | Back Directory | [Name]
AgoMelatine (L(+)-Tartaric acid) | [CAS]
824393-18-2 | [Synonyms]
S-20098 L(+)-TARTARIC ACID
AgoMelatine (L(+)-Tartaric acid)
Agomelatine L(+)-Tartaric acid (S-20098)
Agomelatine L( )-Tartaric acid
(S-20098 L(+)-Tartaric acid) | [Molecular Formula]
C19H23NO8 | [MOL File]
824393-18-2.mol | [Molecular Weight]
393.388 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc. | [form ]
Powder | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) 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 L(+)-Tartaric acid 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]. | [in vivo]
Agomelatine (25, 50, or 75 mg/kg; i.p.) has antioxidant activity in Strychnine (75 mg/kg, i.p.) or Pilocarpine (400 mg/kg, i.p.) induced seizure models in mice. Agomelatine dose not have any antioxidant effects on parameters of oxidative stress produced by Pentylenetetrazole (PTZ) or Picrotoxin (PTX) induced seizure models when compared to controls[3]. | Animal Model: | Female Swiss mice (20-30 g) were administered PTZ (85 mg/kg, i.p.), PTX (7 mg/kg, i.p.), strychnine (75 mg/kg, i.p.), Pilocarpine (400 mg/kg, i.p.), respectively[3] | | Dosage: | 25, 50, or 75 mg/kg | | Administration: | Administered intraperitoneally (i.p.) | | Result: | All dosages showed a significant decrease in thiobarbituric acid reactive substances (TBARS) levels and nitrite content in all brain areas when compared to controls in the Pilocarpine induced seizure model.
All dosages decreased TBARS levels in all brain areas, and at low doses (25 or 50 mg/kg) decreased nitrite contents, but only at 25 or 50 mg/kg showed a significant increase in catalase activity in three brain areas when compared to controls in the Strychnine-induced seizure model.
Did not have any antioxidant effects on parameters of oxidative stress produced by PTX- or PTZ-induced seizure models when compared to controls. |
| [IC 50]
5-HT2C Receptor: 6.4 (pKi, native porcine); 5-HT2C Receptor: 6.2 (pKi, human); hMT1: 0.1 nM (Ki, CHO Cells); hMT1: 0.06 nM (Ki, HEK Cells); hMT2: 0.12 nM (Ki, CHO Cells); hMT2: 0.27 nM (Ki, HEK Cells) | [References]
[1] 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. DOI:10.1007/s00210-003-0751-2
[2] 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. DOI:10.1124/jpet.103.051797
[3] 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. DOI:10.1007/s10571-013-9949-0 |
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SPIRO PHARMA
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InvivoChem
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