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托伐普坦

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。

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托伐普坦名称

[ CAS 号 ]:
150683-30-0

[ 中文名 ]:
托伐普坦

[ 英文名 ]:
Tolvaptan

[中文别名 ]:

托伐坦

[英文别名 ]:

Tolvaptan
UNII-21G72T1950
olvaptan
Samsca
benzazepine derivative,32

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.

[相关活性小分子]

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

托伐普坦合成路线

详细合成路线

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托伐普坦文献

Relation of serum uric acid levels and outcomes among patients hospitalized for worsening heart failure with reduced ejection fraction (from the efficacy of vasopressin antagonism in heart failure outcome study with tolvaptan trial).

Am. J. Cardiol. 114(11) , 1713-21, (2014)

We investigated the clinical profiles associated with serum uric acid (sUA) levels in a large cohort of patients hospitalized for worsening chronic heart failure with ejection fraction (EF) ≤40%, with...

Tolvaptan plus pasireotide shows enhanced efficacy in a PKD1 model.

J. Am. Soc. Nephrol. 26(1) , 39-47, (2015)

Autosomal dominant polycystic kidney disease (ADPKD) is a leading cause of ESRD. A central defect associated with ADPKD pathology is elevated levels of 3', 5'-cyclic AMP (cAMP). Compounds such as tolv...

Association of arginine vasopressin levels with outcomes and the effect of V2 blockade in patients hospitalized for heart failure with reduced ejection fraction: insights from the EVEREST trial.

Circ. Heart Fail. 6(1) , 47-52, (2013)

Arginine vasopressin (AVP) levels are elevated in proportion to heart failure severity and are associated with higher cardiovascular mortality in ambulatory patients. However, the relationship between...

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