SR 49059

Names

[ CAS No. ]:
150375-75-0

[ Name ]:
SR 49059

[Synonym ]:
reclovaptan
cis-Ned 19
INDOL-2-YLCARBONYL)-L-PROLINAMIDE
Relcovaptan
SR 49059

Biological Activity

[Description]:

SR 49059 (SR-49059) is a potent, orally active, selective vasopressin V1a antagonist with a Ki vaule of 1.4 nM[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Research Areas >> Endocrinology

Signaling Pathways >> GPCR/G Protein >> Vasopressin Receptor

[Target]

Ki: 1.4±0.3 nM (vasopressin V1a)[1].

[In Vivo]

SR 49059 (SR-49059) (2 mg/kg and 30 mg/kg; i.p.; once) shows neuroprotective effects in ischemic brain injury when injected early after occlusion of the middle cerebral artery (MCA)[2]. Animal Model: Male Wistar rats, weighing 300 to 350 g, cerebral focal ischemia model[2] Dosage: 2 mg/kg and 30 mg/kg dissolved in 10% dimethyl sulfoxide Administration: Intraperitoneal injection, once Result: Significantly reduced infarction volume measured at 48 hours after the arterial occlusion. Reduced neurological deficits and ischemic brain edema.

[References]

[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.

Chemical & Physical Properties

[ Density]:
1.499g/cm3

[ Boiling Point ]:
868ºC at 760mmHg

[ Molecular Formula ]:
C₂₈H₂₇Cl₂N₃O₇S

[ Molecular Weight ]:
620.50

[ Flash Point ]:
478.8ºC

[ Exact Mass ]:
619.09500

[ PSA ]:
147.85000

[ LogP ]:
5.08430

[ Vapour Pressure ]:
0mmHg at 25°C

[ Index of Refraction ]:
1.664

[ Storage condition ]:
2-8°C

MSDS

Click to get detail MSDS

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Articles

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...