アゴメラチン

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H400：水生生物に強い毒性

• 注意書き

  P273：環境への放出を避けること。

アゴメラチン 価格

アゴメラチン 化学特性,用途語,生産方法

• 外観

  白色～ほとんど白色粉末～結晶

• 溶解性

  エタノール

• 効能

  抗うつ薬, セロトニン受容体拮抗薬, メラトニン受容体拮抗薬

• 説明

  Agomelatine is an agonist of melatonin (MT) receptors and a derivative of melatonin . It binds to MT₁ and MT₂ receptors (K_is = 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-HT_2B and 5-HT_2C (K_is = 0.26 and 0.71 nM, respectively, for the human receptors). Agomelatine (40 mg/kg) inhibits the penile erection response induced by the 5-HT₂ agonist Ro 60-0175 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. It also increases the rate of readjustment to circadian activity cycles following an induced phase shift.

• 化学的特性

  White Solid

• 使用

  Agomelatine is a melatoninergic agonist and selective antagonist of 5-HT2C receptors, and has been shown to be active in several animal models of depression. Agomelatine (S20098) displayed pKi values of 6.4 and 6.2 at native (porcine) and cloned, human (h)5-hydroxytryptamine (5-HT)2C receptors, respectively.

アゴメラチン 上流と下流の製品情報

アゴメラチン 生産企業

Global(597)Suppliers

アゴメラチン スペクトルデータ(¹HNMR)

138112-76-2, アゴメラチン キーワード