| Name | OPC-51803 |
| Description | OPC-51803 is an orally available nonapeptidylpressor (AVP) V(2) receptor selective agonist for the treatment of urinary incontinence and nocturia. |
| In vitro | OPC-51803 and dDAVP displaced [(3)H]-AVP binding to human V(2)- and V(1a)-receptors with K(i) values of 91.9+/-10.8 nM (n = 6) and 3.12+/-0.38 nM (n = 6) for V(2)-receptors, and 819+/-39 nM (n = 6) and 41.5+/-9.9 nM (n = 6) for V(1a)-receptors, indicating that OPC-51803 was about nine times more selective for V(2)-receptors, similar to the selectivity of dDAVP.[5]
OPC-51803 concentration-dependently increased cyclic adenosine 3', 5'-monophosphate (cyclic AMP) production in HeLa cells expressing human V(2)-receptors with an EC(50) value of 189+/-14 nM (n = 6).[5] |
| In vivo | OPC-51803 shows antidiuretic action in dogs. OPC-51803 (0.03 to 0.3 mg/kg; oral) decreased urine volume and increased urinary osmolality in a dose-dependent manner in water-loaded dogs.[4]
OPC-51803 infusions (0.3 and 3 microg x kg(-1) x min(-1); Intravenous ) did not affect renal or systemic hemodynamics in anesthetized dogs.[4] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween-80+45% Saline : 2 mg/mL (4.41 mM), Sonication is recommended.
DMSO : 45 mg/mL (99.12 mM), Sonication is recommended.
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| Keywords | VasopressinReceptor | vasopressin V1b receptor (AVPR1B) | Vasopressin Receptor | OPC-51803 |
| Inhibitors Related | Mozavaptan | Desmopressin acetate (16679-58-6 free base) | Felypressin acetate | d[Cha4]-AVP acetate(500170-27-4 free base) | Nelivaptan | PF-184563 | Ornipressin Acetate(3397-23-7,free) | d[Leu4,Lys8]-VP acetate | E-4177 | Fuscoside | Tolvaptan | WAY-267464 |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Endocrinology-Hormone Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library |
United States
