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Tolvaptan, sold under the brand name Samsca among others, is an aquaretic drug that functions as a selective, competitive vasopressin receptor 2 (V 2) antagonist used to treat hyponatremia (low blood sodium levels) associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH).
Conivaptan hydrochloride is an off-white or a pale yellow power with a solubility of 0.25 mg/mL in water at 23 °C. The injectable formulation consists of 20 mg conivaptan hydrochloride, 0.4 g ethanol, 1.2 g propylene glycol and water. [2]
The "vaptan" drugs act by directly blocking the action of vasopressin at its receptors (V 1A, V 1B and V 2).These receptors have a variety of functions, with the V 1A and V 2 receptors are expressed peripherally and involved in the modulation of blood pressure and kidney function respectively, while the V 1A and V 1B receptors are expressed in the central nervous system.
Tolvaptan phosphate is a drug used for the treatment of cardiac edema. It is a prodrug of tolvaptan, [1] [2] formulated as the salt tolvaptan sodium phosphate, for intravenous administration. Tolvaptan phosphate is converted into the active drug tolvaptan in the human body following administration.
This is followed by Part 2 of the study, during which all study participants who complete Part 1 will receive lixivaptan in a single-arm, open-label phase for an additional 12 months. Part 2 will investigate whether lixivaptan's effect on kidney function continues to accrue over time.
Vasopressin receptor 2 (V2R), or arginine vasopressin receptor 2 (officially called AVPR2), is a protein that acts as receptor for vasopressin. [5] AVPR2 belongs to the subfamily of G-protein-coupled receptors. Its activity is mediated by the G s type of G proteins, which stimulate adenylate cyclase.
Spreitzer H (November 20, 2006). "Neue Wirkstoffe - Conivaptan". Österreichische Apothekerzeitung (in German) (24/2006). "Conivaptan hydrochloride". Molecule of the Month. Prous Science. November 2006. Archived from the original on 2012-02-13.
Satavaptan (INN; developmental code name SR121463, former tentative brand name Aquilda) is a vasopressin-2 receptor antagonist [1] which was investigation by Sanofi-Aventis and was under development for the treatment of hyponatremia. It was also being studied for the treatment of ascites. [2] Development was discontinued in 2009. [3]
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