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Description: Conivaptan HCl (formerly known as YM-087; YM087; YM 087, trade name Vaprisol), the hydrochloride salt of Conivaptan, is an orally bioavailable and non-peptide antagonist of vasopressin V1A and V2 receptors with anti-hypernatremic activity. It inhibits rat liver V1A receptor and rat kidney V2 receptor with Ki values of 0.48 and 3.04 nM, respectively. Conivaptan has been approved in 2004 for use in the treatment of euvolemic and hypervolemic hyponatremia, specifically, for hyponatremia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH), and there is some evidence it may be effective in heart failure. Conivaptan inhibits two of the three subtypes of the vasopressin receptor (V1a and V2).
References: Eur J Pharmacol. 2005 Jan 10; 507(1-3):145-51; J Hepatol. 2003 Jun; 38(6):755-61.
Related CAS#: 210101-16-9(free base)
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