Selective vasopressin V1A receptor antagonist. Inhibits vasopressin and oxytocin-induced increases in intracellular calcium concentrations in vitro (IC50 values are 5 and 30 nM respectively). Exhibits potent and prolonged antivasopressor activity and induces anxiolytic-like effects in the dorsal, but not ventral, hippocampus in vivo.
(Modifications: Tyr-1 = Pmp-Tyr(Me), Gly-8 = C-terminal amide)
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solubility||Soluble to 2 mg/ml in water|
Preparing Stock Solutions
The following data is based on the product molecular weight 1151.38. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||0.87 mL||4.34 mL||8.69 mL|
|5 mM||0.17 mL||0.87 mL||1.74 mL|
|10 mM||0.09 mL||0.43 mL||0.87 mL|
|50 mM||0.02 mL||0.09 mL||0.17 mL|
References are publications that support the products' biological activity.
Kruszynski et al (1980) [1-(β-mercapto-β,β-cyclopentamethylenepropionic acid),2-(O-methyl)tyrosine]arginine-vasopressin and [1-(β-mercapto-β,β-cyclopentamethylenepropionic acid)]arginine-vasopressin, two highly potent antagonists of the vas J.Med.Chem. 23 364 PMID: 6892930
Spath et al (1996) Arginine vasopressin and oxytocin increase intracellular calcium and cAMP in human glomerular epithelial cells in culture. Kidney Blood Press.Res. 19 81 PMID: 8871886
Tsuchiya et al (2002) Vasopressin inhibits sarcolemmal ATP-sensitive K+ channels via V1 receptors activation in the guinea pig heart. Circ.J. 66 277 PMID: 11922278
Engin and Treit (2008) Dissociation of the anxiolytic-like effects of Avpr1a and Avpr1b receptor antagonists in the dorsal and ventral hippocampus. Neuropeptides 42 411 PMID: 18508119
If you know of a relevant reference for (d(CH2)51,Tyr(Me)2,Arg8)-Vasopressin, please let us know.
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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.