| Description | Agomelatine hydrochloride (S-20098 hydrochloride) (S-20098 hydrochloride) is a specific MT1 and MT2 receptor agonist with Ki of 0.1 nM for CHO-hMT1, 0.06 nM for HEK-hMT1, 0.12 nM for CHO-hMT2, and 0.27 nM for HEK-hMT2, respectively [1]. Agomelatine hydrochloride is a selective antagonist of a 5-HT2C receptor with pKis of 6.4 and 6.2 for native (porcine) and cloned, human 5-HT2C receptors, respectively [2]. |
| In vitro | Agomelatine（S 20098）作为MT1和MT2受体的全激动剂，对在CHO或HEK细胞膜中表达的hΜΤ1和hΜΤ2受体的EC50值分别为1.6±0.4、0.10±0.04 nM，[1]。Agomelatine（S20098）还与h5-HT2B受体（6.6）发生作用，但在天然（大鼠）/克隆的人类5-HT2A受体（<5.0/5.3）和5-HT1A受体（<5.0/5.2）表现出低亲和力，对其他5-HT受体的亲和力更是微乎其微（<5.0）[2]。 |
| In vivo | Agomelatine（25、50或75 mg/kg；i.p.）在小鼠Strychnine（75 mg/kg，i.p.）或Pilocarpine（400 mg/kg，i.p.）引发的癫痫模型中具有抗氧化活性。与对照组[3]相比，Agomelatine在Pentylenetetrazole（PTZ）或Picrotoxin（PTX）诱导的癫痫模型上对氧化应激参数没有任何抗氧化效果。 |
| Synonyms | S-20098 hydrochloride |
| molecular weight | 279.76 |
| Molecular formula | C15H18ClNO2 |
| CAS | 1176316-99-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 0.1 mg/mL (insoluble) DMSO: 90 mg/mL (321.7 mM) |
| 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. 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. 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. |