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SR 49059

Cat. No. M8178

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SR 49059 Structure
Synonym:

SR49059

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Quality Control & Documentation
Biological Activity

SR 49059 is a potent and selective Arginine Vasopressin (AVP) V1a-receptor antagonist, with a Ki vaule of 1.4 nM. AVP is a hormone that plays an important part in circulatory and water homoeostasis and is important in renal hemodynamic alterations, water retention, and cardiac remodeling in congestive heart failure (CHF). There are three AVP receptor subtypes V1a, V1b, and V2. All belong to the large rhodopsin-like G-protein-coupled receptor family. V(1a) antagonists improve water balance and cardiac hypertrophy in CHF and might be beneficial for the treatment of water retention and cardiac remodeling in CHF. SR 49059 has also shown initial positive results in the treatment of Raynaud′s disease, dysmenorrhoea, and tocolysis.

Chemical Information
Molecular Weight 620.5
Formula C28H27Cl2N3O7S
CAS Number 150375-75-0
Solubility (25°C) DMSO 80 mg/mL
Storage -20°C, sealed
References

[1] Margareta Steinwall, et al. Inhibitory effects of SR 49059 on oxytocin-and vasopressin-induced uterine contractions in non-pregnant women

[2] R Brouard, et al. Safety, tolerability, and pharmacokinetics of SR 49059, a V1a vasopressin receptor antagonist, after repeated oral administration in healthy volunteers

[3] C Serradeil-Le Gal, et al. Biochemical and pharmacological properties of SR 49059, a new, potent, nonpeptide antagonist of rat and human vasopressin V1a receptors

[4] C Serradeil-Le Gal, et al. Binding of [3H] SR 49059, a potent nonpeptide vasopressin V1a antagonist, to rat and human liver membranes

[5] C Serradeil-Le Gal, et al. Effects of SR 49059, a non-peptide antagonist of vasopressin V1a receptors, on vasopressin-induced coronary vasoconstriction in conscious rabbits

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Keywords: SR 49059, SR49059 supplier, Vasopressin Receptor, inhibitors, activators

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