喹托司特钠 | 101193-62-8

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 喹托司特钠
• 英文名称: sodium;4-oxo-1-phenoxy-N-(1,2,4-triaza-3-azanidacyclopenta-1,4-dien-5-yl)quinolizine-3-carboxamide
• CAS: 101193-62-8
• 化学式: C17H11N6NaO3
• 分子量: 370.3
• InChiKey: CDPWRMHFRRXOQH-UHFFFAOYSA-M

物化性质

• 溶解度：
  溶于二甲基亚砜

计算性质

• 辛醇/水分配系数(LogP)：
  -1.95
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  119
• 氢给体数：
  1
• 氢受体数：
  7

制备方法与用途

生物活性

Quinotolast sodium (浓度范围为 1-100 μg/mL) 抑制组胺，LTC4 和 PGD2 释放，这种作用具有浓度依赖性。

靶点

LTC 4

PGD 2

Histamine

体外研究

Quinotolast inhibits the release of histamine and the generation of leukotriene (LT) C ₄ and prostaglandin (PG) D ₂ from dispersed human lung cells. Quinotolast (100 μg/mL) significantly inhibits PGD ₂ and LTC ₄ release. Quinotolast inhibits PGD ₂ release by 100% and LTC ₄ release by 54%. The inhibitory effect of Quinotolast on histamine release from dispersed lung cells is largely independent of the preincubation period, no tachyphylaxis being observed. Quinotolast shows a significant inhibition of inflammatory mediators from human dispersed lung cells. Quinotolast also shows strong inhibitory effects on histamine and peptide leukotrienes release from guinea pig lung fragments or mouse cultured mast cells. Quinotolast concentration-dependently inhibits pLTs release from cultured mast cells. The IC ₅₀ value for Quinotolast is 0.72 μg/mL.

体内研究

Quinotolast potently inhibits such type I allergic reactions as passive cutaneous anaphylaxis (PCA) and anaphylactic bronchoconstriction in rats by both intravenous and oral dosing. When Quinotolast is given i.v. to rats, Quinotolast, dose-dependently inhibits PCA. The doses of Quinotolast required to inhibit the reaction by 50% (ED ₅₀ ) is 0.0063 mg/kg. Given p.o., Quinotolast inhibits the reaction. ED ₅₀ value for Quinotolast is 0.0081 mg/kg. Although almost complete inhibition is observed with Quinotolast at a dose of 0.32 mg/kg, its effect is slightly attenuated at a dose of 1 mg/kg.

反应信息

• 作为产物：
  描述：

  喹托司特 生成 喹托司特钠
  参考文献：
  名称：

  KITAURA, JOSIXIKO;OKU, TEHRUO;XIRAI, XIDEHO;YAMAMOTO, TOSIXIDEH;XASIMOTO,+

  摘要：

  DOI：