SR 49059
Chemical Name: (2S)-1-[[(2R,3S)-5-Chloro-3-(2-chlorophenyl)-1-[(3,4-dimethoxyphenyl)sulfonyl]-2,3-dihydro-3-hydroxy-1H-indol-2-yl]carbonyl]-2-pyrrolidinecarboxamide
Purity: ≥99%
Biological Activity
SR 49059 is a 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 antagonizes arginine vasopressin-induced effects in vitro (IC50 = 3.7 nM for inhibition of human platelet aggregation) and is orally active in vivo.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Nutritional state-dependent ghrelin activation of vasopressin neurons via retrograde trans-neuronal-glial stimulation of excitatory GABA circuits.
Haam J, Halmos K, Di S, Tasker J
J Neurosci, 2014;34(18):6201-13. -
Biochemical and pharmacological properties of SR 49059, a new, potent, nonpeptide antagonist of rat and human vasopressin V1a receptors.
Serradeil-Le Gal et al.
J.Clin.Invest., 1993;92:224 -
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.
Tahtaoui et al.
J.Biol.Chem., 2003;278:40010 -
Binding of [3H]SR 49059, a potent nonpeptide vasopressin V1a antagonist, to rat and human liver membranes.
Serradeil-Le Gal et al.
Biochem.Biophys.Res.Comm., 1994;199:353
Product Datasheets
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Citations for SR 49059
The citations listed below are publications that use Tocris products. Selected citations for SR 49059 include:
6 Citations: Showing 1 - 6
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OXT functions as a spatiotemporal filter for excitatory synaptic inputs to VTA DA neurons.
Authors: Xiao Et al.
Elife 2018;7
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Biased OXTergic Modulation of Midbrain DA Systems.
Authors: Xiao Et al.
Neuron 2017;95:368
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Water deprivation induces neurovascular and cognitive dysfunction through vasopressin-induced oxidative stress.
Authors: Faraco Et al.
Acta Neurochir Suppl 2014;34:852
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Arginine vasopressin enhances cell survival via a G protein-coupled receptor kinase 2/β-arrestin1/extracellular-regulated kinase 1/2-dependent pathway in H9c2 cells.
Authors: Zhu Et al.
Mol Pharmacol 2013;84:227
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Arginine-vasopressin V1a receptor inhibition improves neurologic outcomes following an intracerebral hemorrhagic brain injury.
Authors: Manaenko Et al.
Neurochem Int 2011;58:542
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Post-treatment with SR49059 improves outcomes following an intracerebral hemorrhagic stroke in mice.
Authors: Manaenko Et al.
BMC Neurosci 2011;111:191
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