procainium acetate

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: procainium acetate
• 英文别名: Acetic acid;2-(diethylamino)ethyl 4-aminobenzoate
• 化学式: C₂H₄O₂*C₁₃H₂₀N₂O₂
• 分子量: 296.367
• InChiKey: PQNKBCQYPSDAMZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.86
• 重原子数：
  21
• 可旋转键数：
  7
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  92.9
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  溶剂黄146 、 普鲁卡因 反应 12.0h， 生成 procainium acetate
  参考文献：
  名称：

  Procainium Acetate Versus Procainium Acetate Dihydrate: Irreversible Crystallization of a Room-Temperature Active Pharmaceutical-Ingredient Ionic Liquid upon Hydration

  摘要：

  Anhydrous procainium acetate is a room temperature ionic liquid (T-g = -25 degrees C); however, in the presence of water, this salt forms a crystalline dihydrate (T-m = 52 degrees C) that cannot be dehydrated without decomposition. Unintended crystallization of any active pharmaceutical ingredient can dramatically alter its solubility and bioavailability, making it essential that ionic liquid APIs be carefully studied for their crystallization behavior.

  DOI：

  10.1021/cg400686e

文献信息

• Pharmaceutical preparation of ascorbic acid derivatives for medical treatment of cancer
  申请人：SHOWA DENKO KABUSHIKI KAISHA

  公开号：EP0875246A1

  公开（公告）日：1998-11-04

  A pharmaceutical preparation comprising at least one L-ascorbic acid derivative and at least one antimalignant tumor agent, wherein said L-ascorbic acid derivative provides, on culturing zooblast for 20 hours in a culture medium containing the L-ascorbic acid derivative in a concentration of 5 µM, an L-ascorbic acid intracellular cumulative amount equal to or greater than that obtained by culturing the zooblast, in a culture medium containing magnesium L-ascorbic acid-2-phosphate in a concentration of 50 µM. Also disclosed is a pharmaceutical preparation, for inhibiting cancer metastasis, which comprises the L-ascorbic acid derivative. Also disclosed is a method of treating cancer which comprises administering to a person in need of such treatment a dosage effective amount of the pharmaceutical preparation.

  一种药物制剂，包含至少一种L-抗坏血酸衍生物和至少一种抗恶性肿瘤剂，其中所述L-抗坏血酸衍生物在含有浓度为5微摩尔的L-抗坏血酸衍生物的培养基中培养动物细胞20小时后，细胞内的L-抗坏血酸累积量等于或大于在含有浓度为50微摩尔的L-抗坏血酸-2-磷酸镁的培养基中培养动物细胞所获得的L-抗坏血酸累积量。还公开了一种药物制剂，用于抑制癌症转移，其中包含L-抗坏血酸衍生物。还公开了一种治疗癌症的方法，该方法包括向需要这种治疗的人施用一定剂量有效量的药物制剂。
• PHARMACEUTICAL PREPARATION AND METHOD FOR TREATING CANCER
  申请人：——

  公开号：US20020010210A1

  公开（公告）日：2002-01-24

  A pharmaceutical preparation comprising at least one L-ascorbic acid derivative and at least one antimalignant tumor agent, wherein said L-ascorbic acid derivative provides, on culturing zooblast for 20 hours in a culture medium containing the L-ascorbic acid derivative in a concentration of 5 &mgr;M, an L-ascorbic acid intracellular cumulative amount equal to or greater than that obtained by culturing the zooblast in a culture medium containing magnesium L-ascorbic acid-2-phosphate in a concentration of 50 &mgr;M. Also disclosed is a method of inhibiting cancer metastasis which comprises administering to a person in need of such treatment a dosage effective amount of the L-ascorbic acid derivative. Also disclosed is a method of treating cancer which comprises administering to a person in need of such treatment a dosage effective amount of the pharmaceutical preparation.

  一种药物制剂，包括至少一种L-抗坏血酸衍生物和至少一种抗恶性肿瘤剂，其中所述L-抗坏血酸衍生物在含有浓度为5&mgr；M的L-抗坏血酸衍生物培养20小时后，细胞内L-抗坏血酸累积量等于或大于在含有浓度为50&mgr;M的L-抗坏血酸-2-磷酸镁的培养基中培养动物细胞所获得的L-抗坏血酸累积量。还公开了一种抑制癌症转移的方法，该方法包括向需要这种治疗的人施用一定剂量有效量的L-抗坏血酸衍生物。还公开了一种治疗癌症的方法，该方法包括向需要这种治疗的人施用一定剂量有效量的药物制剂。
• US5276032A
  申请人：——

  公开号：US5276032A

  公开（公告）日：1994-01-04
• US5563153A
  申请人：——

  公开号：US5563153A

  公开（公告）日：1996-10-08
• US8232265B2
  申请人：——

  公开号：US8232265B2

  公开（公告）日：2012-07-31