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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.

PD 0332992