Tolvaptan
Tolvaptan is an inhibitor of the vasopressin receptor subtype V2; it acts as a diuretic, inhibiting reabsorption of water in the kidney without loss of sodium. Tolvaptan is a clinically effective diuretic used in congestive heart failure (CHF) and severe chronic kidney disease that does not induce hypernatremia. This compound can also be used to treat the severe or chronic hyponatremia stemming from syndrome of inappropriate antidiuretic hormone secretion (SIADH) that occurs after traumatic brain injury.
References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18977178
Cas No. |
150683-30-0 |
---|---|
Purity |
≥98% |
Formula |
C26H25ClN2O3 |
Formula Wt. |
448.94 |
Chemical Name |
N-(4-{[(5R)-7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl}-3-methylphenyl)-2-methylbenzamide |
IUPAC Name |
N-[4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)-3-methylphenyl]-2-methylbenzamide |
Synonym |
OPC-41061 |
Melting Point |
226°C |
Appearance |
Off-white to yellow powder |
Otsuka T, Sakai Y, Ohno D, et al. The effects of tolvaptan on patients with severe chronic kidney disease complicated by congestive heart failure. Clin Exp Nephrol. 2013 Mar 13. [Epub ahead of print]. PMID: 23483323.
Graziani G, Cucchiari D, Aroldi A, et al. Syndrome of inappropriate secretion of antidiuretic hormone in traumatic brain injury: when tolvaptan becomes a life saving drug. J Neurol Neurosurg Psychiatry. 2012 May;83(5):510-2. PMID: 22323742
Gheorghiade M, Teerlink JR, Mebazaa A. Pharmacology of new agents for acute heart failure syndromes. Am J Cardiol. 2005 Sep 19;96(6A):68G-73G. PMID: 16181825.