プルカロプリド

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

  H315：皮膚刺激

  H319：強い眼刺激

  H335：呼吸器への刺激のおそれ

  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。

  P302+P352：皮膚に付着した場合：多量の水と石鹸で洗うこと。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

プルカロプリド 価格

プルカロプリド 化学特性,用途語,生産方法

• 効能

  消化管運動改善薬, セロトニン受容体作動薬

• 説明

  Prucalopride is a potent and selective agonist of the serotonin (5-HT) receptor subtype 5-HT₄ (K_is = 2.5 and 8 nM for human 5-HT_4A and 5-HT_4B, respectively). Prucalopride is greater than 250-fold selective for 5-HT₄ over a panel of 53 overexpressed receptors, including 5-HT subtypes, but does bind to human dopamine D₄ and sigma-1 (σ₁) receptors and mouse 5-HT₃ receptors (K_is = 2.3, 3.7, and 3.8 μM, respectively). It induces contractions in guinea pig colon with an EC₅₀ value of 33 nM, an effect that is blocked by the 5-HT₄ antagonist GR113808 but not the 5-HT_2A and 5-HT₃ antagonists ketanserin and granisetron , respectively. It also facilitates non-cholinergic contractions induced by electrical stimulation. In fasted dogs, oral administration of prucalopride increases colonic motility by inhibiting distal colon contractions (ED₅₀ = 0.04 mg/kg), an effect that is blocked by pretreatment with the 5-HT₄ antagonist GR125487. Prucalopride (5-10 mg/kg, s.c.) increases acetylcholine and histamine levels in the rat prefrontal cortex by 2.4-fold and 3-fold, respectively, and increases the power of hippocampal theta oscillations. Formulations containing prucalopride have been used in the treatment of chronic idiopathic constipation.

• Biochem/physiol Actions

  In healthy male individuals, prucalopride decreases the display of esophageal acid and promotes gastric emptying. It is effective, safe and shows good tolerance for the treatment of men with chronic constipation.

• 作用機序

  Prucalopride is a high affinity, highly selective 5-HT4 agonist. Its action in the treatment of chronic constipation is to stimulate intestinal peristalsis by specifically interacting with 5-HT4 receptors in the digestive tract, resulting in the release of acetylcholine, which further constricts the muscular layer of the colon, and the relaxation of the circular muscular layer promoting the expulsion of luminal contents.

• 酵素阻害剤

  This novel enterokinetic drug (FW = 367.87 g/mol; CAS 179474-81-8), also known by the tradename Resolor? and its systematic name, 4-amino-5- chloro-N-[1-(3-methoxypropyl)piperidin-4-yl]-2,3-dihydro-1-benzofuran-7- carboxamide, is a selective, high affinity serotonin 5-HT4 receptor agonist with that stimulates colonic mass movements, which provide the main propulsive force for defecation. It exhibits high affinity to both 5-HT4 receptor isoforms, with respective pKi values of 8.60 and 8.10 for the human 5-HT4A and 5-HT4B receptors. Based on 50 other binding assays,tonly the human D4 receptor (pKi = 5.63), the mouse 5-HT3 receptor (pKi = 5.41) and the human s1 (pKi = 5.43) shown measurable affinity, resulting in >290x selectivity for 5-HT4 receptors. Prucalopride also differs from other 5-HT4 agonists, such as tegaserod and cisapride, that interact with other receptors (5-HT1B/D and cardiac human ether-a-go-go K+ or hERG channel, respectively).

プルカロプリド 生産企業

Global(227)Suppliers

プルカロプリド スペクトルデータ(¹HNMR)

179474-81-8, プルカロプリド キーワード