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西他塞坦钠

西他塞坦钠用途

Sitaxsentan sodium 是一种有效的，选择性的 endothelin A receptor 拮抗剂。

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西他塞坦钠名称

[ CAS 号 ]:
210421-74-2

[ 中文名 ]:
司他生坦钠

[ 英文名 ]:
Sitaxentan sodium

[中文别名 ]:

西他塞坦钠

[英文别名 ]:

Thelin
Sitax
Sitaxsentan sodium
Sitaxentan sodium [USAN]
Sitaxentan sodium
Sitaxsentan (sodium)

西他塞坦钠生物活性

[ 描述 ]:

Sitaxsentan sodium 是一种有效的,选择性的 endothelin A receptor 拮抗剂。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 内皮素受体

研究领域 >> 心血管疾病

[体外研究]

西他生坦和波生坦在较高浓度下减弱NTCP转运,并抑制人肝转运蛋白,这为在临床环境中观察到的这些药物的肝毒性增加提供了潜在的机制。只有sitaxsentan减少了OATP转运(52％)[1]。西他生坦和西他生坦联合西地那非完全阻止内皮素-1和ETB受体的表达增加。单独的西他生坦可部分恢复BMPR-1A和BMPR-2的表达。西地那非和西他生坦的组合进一步恢复了BMPR-1A和BMPR-2的表达,然而,与对照组相比,BMPR-1A和BMPR-2的表达降低[3]。

[体内研究]

西他生坦(在缺氧发作前10分钟静脉注射5mg/kg)完全阻断缺氧诱导的血管收缩,该组与空气对照没有差异。西他生坦的口服给药显着减弱了MPAP的增加,而西他生坦对暴露于正常氧水平的大鼠的给药对MPAP没有影响[2]。西他生坦单独限制分流诱导的MT增加。西他生坦联合西地那非可以更有效地防止这种重塑,然而,与对照相比,这种重塑往往会增加[3]。

[动物实验]

在最初2周的低氧暴露期（10％O 2）后，在持续暴露于缺氧期间，给予西他生坦（在饮用水中每天15或30mg / kg体重）4周。在4周的缺氧期结束时，进行股动脉和肺动脉插管以及MPAP，MSAP和HR的测量。

[参考文献]

[1]. Hartman JC, et al. Evaluation of the endothelin receptor antagonists ambrisentan, darusentan, bosentan, and sitaxsentan as substrates and inhibitors of hepatobiliary transporters in sandwich-cultured human hepatocytes. Can J Physiol Pharmacol. 2010 Jun;88

[2]. Tilton RG, et al. Attenuation of pulmonary vascular hypertension and cardiac hypertrophy with sitaxsentan sodium, an orally active ET(A) receptor antagonist. Pulm Pharmacol Ther. 2000;13(2):87-97.

[3]. Rondelet B, et al. Sildenafil added to sitaxsentan in overcirculation-induced pulmonary arterial hypertension. Am J Physiol Heart Circ Physiol. 2010 Oct;299(4):H1118-23. Epub 2010 Aug 6.

[相关活性小分子]

西他塞坦钠物理化学性质

[ 分子式 ]:
C₁₈H₁₄ClN₂NaO₆S₂

[ 分子量 ]:
476.88600

[ 精确质量 ]:
475.98800

[ PSA ]:
135.56000

[ LogP ]:
4.90080

[ 外观性状 ]:
white to beige

[ 储存条件 ]:
room temp

[ 水溶解性 ]:
H2O: soluble10mg/mL (clear solution)

西他塞坦钠安全信息

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

[ RTECS号 ]:
XN0296600

西他塞坦钠文献

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