< 生产厂家价格 >

(2S)-1-[[(2r,3s)-5-氯-3-(2-氯苯基)-1-[(3,4-二甲氧基苯基)磺酰基]-2,3-二氢-3-羟基-1H-吲哚-2-基]羰基]-2-吡咯烷羧酰胺

用途

SR 49059(SR-49059)是一种有效的口服选择性加压素V1a拮抗剂,其Ki值为1.4 nM【1】。

点击显示

名称

[ CAS 号 ]:
150375-75-0

[ 中文名 ]:
(2S)-1-[[(2r,3s)-5-氯-3-(2-氯苯基)-1-[(3,4-二甲氧基苯基)磺酰基]-2,3-二氢-3-羟基-1H-吲哚-2-基]羰基]-2-吡咯烷羧酰胺

[ 英文名 ]:
SR 49059

[英文别名 ]:

reclovaptan
cis-Ned 19
INDOL-2-YLCARBONYL)-L-PROLINAMIDE
Relcovaptan
SR 49059

生物活性

[ 描述 ]:

SR 49059(SR-49059)是一种有效的口服选择性加压素V1a拮抗剂,其Ki值为1.4 nM【1】。

[ 相关类别 ]:

研究领域 >> 心血管疾病

研究领域 >> 内分泌

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 血管加压素受体

[ 靶点 ]

Ki: 1.4±0.3 nM (vasopressin V1a)[1].

[体内研究]

大脑中动脉(MCA)闭塞后早期注射SR 49059(SR-49059)(2 mg/kg和30 mg/kg；i.p.；一次)对缺血性脑损伤有神经保护作用【2】。动物模型：雄性Wistar大鼠,体重300-350 g,局灶性脑缺血模型【2】剂量：2 mg/kg和30 mg/kg溶于10%二甲基亚砜给药：腹腔注射,一次结果：动脉闭塞后48小时测得的梗死体积显著减少。减少神经功能缺损和缺血性脑水肿。

[参考文献]

[1]. Serradeil-Le Gal C, et al. Effect of SR-49059, a vasopressin V1a antagonist, on human vascular smooth muscle cells. Am J Physiol. 1995 Jan;268(1 Pt 2):H404-10.

[2]. Shuaib A, et al. Effects of nonpeptide V(1) vasopressin receptor antagonist SR-49059 on infarction volume and recovery of function in a focal embolic stroke model. Stroke. 2002 Dec;33(12):3033-7.

物理化学性质

[ 密度 ]:
1.499g/cm3

[ 沸点 ]:
868ºC at 760mmHg

[ 分子式 ]:
C₂₈H₂₇Cl₂N₃O₇S

[ 分子量 ]:
620.50

[ 闪点 ]:
478.8ºC

[ 精确质量 ]:
619.09500

[ PSA ]:
147.85000

[ LogP ]:
5.08430

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
0mmHg at 25°C

[ 折射率 ]:
1.664

[ 储存条件 ]:
2-8°C

MSDS

详细MSDS(安全技术说明书)

安全信息

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

文献

The secretion patterns and roles of cardiac and circulating arginine vasopressin during the development of heart failure.

Neuropeptides 51 , 63-73, (2015)

The aim of this study is to investigate local cardiac and circulating AVP secretion during heart failure and to determine whether AVP mediates ventricular remodeling.We assessed cardiac function and A...

Vasopressin and hydration play a major role in the development of glucose intolerance and hepatic steatosis in obese rats.

Diabetologia 58(5) , 1081-90, (2015)

High plasma copeptin, a marker of vasopressin (VP) secretion, has been shown to be associated with the metabolic syndrome and development of type 2 diabetes in humans. The present study was designed t...

Vasopressin-2 receptor antagonist attenuates the ability of the lungs to clear edema in an experimental model.

Am. J. Respir. Cell. Mol. Biol. 47(5) , 583-8, (2012)

In the last two decades, the role of the alveolar active sodium transport was extensively studied and was found to play a crucial role in regulating alveolar fluid clearance (AFC), and thus in keeping...

更多文献