| S2593 |
Tolvaptan
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Tolvaptan (OPC-41061) is an orally effective nonpeptide arginine vasopressin V2 receptor antagonist with IC50 of 3 nM, used to treat hyponatremia.
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J Immunother Cancer, 2024, 12(11)e009805
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Int Immunopharmacol, 2024, 127:111378
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Acta Physiol (Oxf), 2021, 10.1111/apha.13661
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| S2116 |
Conivaptan HCl
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Conivaptan HCl(YM 087) is an orally active, non-peptide, vasopressin V1A and V2 receptor antagonist, used in the treatment of euvolemic and hypervolemic hyponatremia.
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Sci Bull (Beijing), 2024, 69(12):1936-1953
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J Immunother Cancer, 2024, 12(11)e009805
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Cell Res, 2022, 1-17
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| S2920 |
Mozavaptan
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Mozavaptan (OPC-31260) is a novel competitive vasopressin receptor antagonist for both V1 and V2 receptors with IC50 of 1.2 μM and 14 nM, respectively.
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Life Sci, 2019, 10.1016/j.lfs.2019.05.049
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Am J Med Sci, 2019, 357(3):247-254
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| S0007 |
RO 5028442 (RG7713)
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RO 5028442 (RG7713) is a highly potent and selective Brain-Penetrant Vasopressin 1a (V1a) receptor antagonist with Kis of 1 nM for hV1a and 39 nM for mV1a.
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| S2815 |
Lixivaptan (VPA-985)
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Lixivaptan (VPA-985, CRTX 080, WAY VPA 985) is an oral, non-peptide, selective V2 receptor vasopressin antagonist with IC50s of 1.2 nM and 2.3 nM for human V2 receptor and rat V2 receptor, respectively.
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| E4957 |
Mozavaptan (hydrochloride)
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Mozavaptan hydrochloride (OPC 31260 HCl), a benzazepine derivative, is a potent, selective, competitive, and orally active antagonist of vasopressin V2 receptor with an IC50 value of 14 nM. It shows ~85-fold selectivity for V2 receptor over V1 receptor and has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment.
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