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Mozavaptan (OPC-31260) is a novel, orally effective, nonpeptide vasopressin V2 receptor antagonist. The V2 receptor subtype is important in water retention, cardiac remodeling in congestive heart failure (CHF), and renal hemodynamic alterations, and is considered a target for polysystic kidney disease. Mozavaptan (OPC-31260) inhibited the antidiuretic action of exogenously administered AVP in water-loaded, alcohol-anaesthetized rats in a dose-dependent manner. Mozavaptan (OPC-31260) caused a competitive displacement of [3H]-AVP binding to both V1 and V2 receptors with IC50 values of 1.2 ± 0.2 × 10-6 M and 1.4 ± 0.2 × 10-8 M, respectively.
| Molecular Weight | 427.53 |
| Formula | C27H29N3O2 |
| CAS Number | 137975-06-5 |
| Solubility (25°C) | DMSO 5 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[4] Carles Villabona. Vasopressin receptor antagonists: the vaptans
| Related Vasopressin Receptor Products |
|---|
| Conivaptan hydrochloride
Conivaptan hydrochloride is a non-peptide vasopressin receptor antagonist, which can inhibit V1A receptor in rat liver and V2 receptor in kidney with Ki values of 0.48 and 3.04 nM, respectively. |
| Atosiban Acetate
Atosiban (RW22164; Tractocile) Acetate is a nonapeptide, desamino-oxytocin analogue, and a competitive vasopressin/oxytocin receptor antagonist (VOTra). Atosiban inhibits the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane. |
| L-371,257
L-371,257 is a potent and selective oxytocin receptor antagonist. |
| Antagonist G
Antagonist G is an anticancer peptide and it is also a potent vasopressin antagonist. |
| Argipressin Acetate
Argipressin (Arg8-vasopressin) binds to vascular arginine vasopressin receptors V1, V2 and V3, and its Kd value against V1 in A7r5 rat aortic smooth muscle cells is 1.31 nM. |
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