托伐普坦

• 常用名: 托伐普坦
• 英文名: Tolvaptan
• CAS号: 150683-30-0
• 分子量: 448.941
• 密度: 1.3±0.1 g/cm3
• 沸点: 594.4±50.0 °C at 760 mmHg
• 分子式: C₂₆H₂₅ClN₂O₃
• 熔点: 219-222°C
• 闪点: 313.3±30.1 °C

托伐普坦用途

Tolvaptan是精氨酸加压素受体2拮抗剂,能抑制AVP-诱导的血小板聚集,IC50为1.28μM。

托伐普坦名称

• 中文名: 托伐普坦
• 英文名: N-[4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)-3-methylphenyl]-2-methylbenzamide
• 中文别名: 托伐坦 | N-[4-[(5R)-7-氯-5-羟基-2,3,4,5-四氢-1-苯并氮杂卓-1-甲酰基]-3-甲基苯基]-2-甲基苯甲酰胺

托伐普坦生物活性

• 描述: Tolvaptan是精氨酸加压素受体2拮抗剂,能抑制AVP-诱导的血小板聚集,IC50为1.28μM。
• 相关类别:
  信号通路 >> 自噬 >> 自噬
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 血管加压素受体
  研究领域 >> 心血管疾病
• 参考文献:

  [1]. Friedman B, Cirulli J.Hyponatremia in critical care patients: Frequency, outcome, characteristics, and treatment with the vasopressin V(2)-receptor antagonist tolvaptan.J Crit Care. 2012 Aug 8.

  [2]. Inomata T.Tolvaptan (vasopressin receptor antagonist).Nihon Rinsho. 2011 Nov;69 Suppl 9:408-11.

  [3]. Vaduganathan M, Gheorghiade M, Pang PS, Konstam MA, Zannad F, Swedberg K, Grinfeld L, Burnett JC Jr, Krasa HB, Zimmer C, Blair J, Ouyang J, Maggioni AP; EVEREST investigators.Efficacy of oral tolvaptan in acute heart failure patients with hypotension and renal impairment.J Cardiovasc Med (Hagerstown). 2012 Jul;13(7):415-22.

  [4]. Y Yamamura et al. OPC-41061, a Highly Potent Human Vasopressin V2-Receptor Antagonist: Pharmacological Profile and Aquaretic Effect by Single and Multiple Oral Dosing in Rats. J. Pharmacol. Exp. Ther. 1998, 287(3), 860-867.

  [5]. RW Schrier et al. Tolvaptan, a Selective Oral Vasopressin V2-Receptor Antagonist, for Hyponatremia. N Engl J Med 2006, 355, 2099-2112.

托伐普坦物理化学性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 594.4±50.0 °C at 760 mmHg
• 熔点: 219-222°C
• 分子式: C₂₆H₂₅ClN₂O₃
• 分子量: 448.941
• 闪点: 313.3±30.1 °C
• 精确质量: 448.155365
• PSA: 69.64000
• LogP: 4.09
• 外观性状: white to tan
• 蒸汽压: 0.0±1.8 mmHg at 25°C
• 折射率: 1.664
• 储存条件: Refrigerator
• 水溶解性: DMSO: ≥15mg/mL

托伐普坦安全信息

• 危险品运输编码: NONH for all modes of transport

托伐普坦英文别名

• (±)-4'-[(7-chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-o-tolu-m-toluidide
• Tolvaptan
• UNII-21G72T1950
• olvaptan
• N-{4-[(7-Chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl}-2-methylbenzamide
• Benzamide, N-[4-[(7-chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methyl-
• Samsca
• benzazepine derivative,32
• N-[4-(9-chloro-6-hydroxy-2-azabicyclo[5.4.0]undeca-8,10,12-triene-2-carbonyl)-3-methyl-phenyl]-2-methyl-benzamide