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Category:
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7TM Receptors Peptides (Hypothalamic/Pituitary Hormones)Vasopressin and Oxytocin Receptors
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Cat.No.
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Product Name
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2310 |
SR 49059
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| Alternative name(s): |
Relcovaptan |
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Price and Availability
Click here for full price details of
SR 49059
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Chemical Name:
(2S)-1-[[(2R,3S)-5-Chloro-3-(2-chlorophenyl)-1-[(3,4-di
methoxyphenyl)sulfonyl]-2,3-dihydro-3-hydroxy-1H-indol-
2-yl]carbonyl]-2-pyrrolidinecarboxamide |
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Biological Activity:
Potent and selective non-peptide vasopressin V1a
receptor antagonist; devoid of agonist activity. Displays high affinity and
efficacy at both rat (Ki = 1.6 nM) and human (Ki =
1.1-6.3 nM) V1a receptors. Potently antagonises arginine vasopressin-induced
effects in vitro (IC50 = 3.7 nM for inhibition of human platelet
aggregation) and is orally active in vivo.
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
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References:
Serradeil-Le
Gal et al (1993)
Biochemical and pharmacological properties of SR 49059, a new, potent,
nonpeptide antagonist of rat and human vasopressin V1a receptors.
J.Clin.Invest. 92 224. Serradeil-Le Gal et al
(1994) Binding of [3H]SR 49059, a potent nonpeptide vasopressin V1a
antagonist, to rat and human liver membranes. Biochem.Biophys.Res.Comm. 199
353. Tahtaoui et al (2003) Identification of the binding sites of
the SR 49059 nonpeptide antagonist into the V1a vasopressin receptor
using sulfydryl-reactive ligands and cysteine mutants as chemical sensors.
J.Biol.Chem. 278 40010.
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or by Research Area
Keywords: SR 49059, Peptides (Hypothalamic / Pituitary Hormones), Selective, Orally Active Vasopressin V1a Receptor Antagonist, Relcovaptan, SR49059, Tocris Bioscience
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