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Nonpeptide vasopressin V1 receptor antagonist. Displays greater affinity for rat V1 than human V1 (Ki values are 25 and 8800 nM respectively). Exhibits 1000-fold selectivity for V1 receptors over V2 receptors. Orally active.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 449.54. Batch specific molecular weights may vary from batch to batch due to the degree 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||2.22 mL||11.12 mL||22.24 mL|
|5 mM||0.44 mL||2.22 mL||4.45 mL|
|10 mM||0.22 mL||1.11 mL||2.22 mL|
|50 mM||0.04 mL||0.22 mL||0.44 mL|
References are publications that support the biological activity of the product.
Yamamura et al (1991) OPC-21268, an orally effective, nonpeptide vasopressin V1 receptor antagonist. Science 252 572 PMID: 1850553
Imaizumi et al (1992) Effects of OPC-21268, an orally effective vasopressin V1 receptor antagonist in humans. Hypertension 20 54 PMID: 1319959
Thibonnier et al (2000) A molecular model of agonist and nonpeptide antagonist binding to the human V1 vascular vasopressin receptor. J.Pharmacol.Exp.Ther. 294 195 PMID: 10871312
If you know of a relevant reference for OPC 21268, please let us know.
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Keywords: OPC 21268, OPC 21268 supplier, OPC21268, vasopressin, v1, v1r, avp, arginine, Vasopressin, Receptors, 3924, Tocris Bioscience
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Literature in this Area
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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.