ピトリサント塩酸塩

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 注意書き

  P201：使用前に取扱説明書を入手すること。

  P308+P313：暴露または暴露の懸念がある場合：医師の診断/手当てを 受けること。

ピトリサント塩酸塩 価格

ピトリサント塩酸塩 化学特性,用途語,生産方法

• 効能

  向知性薬, H3受容体逆作動薬/拮抗薬

• 説明

  Pitolisant hydrochloride, a first-in-class inverse agonist of the histamine H3 receptor, was approved in the EU for the treatment of excessive daytime sleepiness (EDS) in adults with narcolepsy with or without cataplexy. The drug, which was developed by Bioprojet and has orphan drug designation in the EU and US, enhances wakefulness by increasing histaminergic neuron activity. With once daily oral administration in the morning, patients taking pitolisant exhibited significantly reduced EDS versus placebo but not versus modafinil. Plasma levels of the drug are reduced at the end of the day such that its waking effect is minimized at night (plasma t1/2 10-12 h). Several articles have been published detailing the discovery of pitolisant.

• 合成

  The most likely scale preparation of pitolisant hydrochloride consists of only four synthetic steps starting with the mesylation of commercial 3-(4-chlorophenyl)propan-1-ol (132). Displacement of the mesylate with the sodium salt of commercial 3-(piperidin-1-yl)propan-1-ol (133) in warm DMA assembled the parent drug in 97% yield over two steps. Salt formation was affected by pH adjustment to 3-4 using HCl gas in EtOAc. Recrystallization from ethyl acetate and isopropanol provided pitolisant hydrochloride (XII) on kilogram scale in 78% overall yield across the short four-step protocol.

ピトリサント塩酸塩 生産企業

Global(99)Suppliers

ピトリサント塩酸塩 スペクトルデータ(¹HNMR)

903576-44-3, ピトリサント塩酸塩 キーワード