Conivaptan hydrochloride

Details:

Product Name: Conivaptan hydrochloride
Synonyms: (1,1'-Biphenyl)-2-carboxamide, N-(4-((4,5-dihydro-2-methylimidazo(4,5-D)(1)benzazepin-6(1H)-yl)carbonyl)phenyl)-, monohydrochloride;Conivaptan HCl;Conivaptan hydrochloride [usan];Unii-75L57R6X36;Vaprisol;Conivaptan hydrochkoride;[1,1'-Biphenyl]-2-carboxamide,N-[4-[(4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl]-,hydrochloride;Conivaptan hydrochloride, >=99%
CAS: 168626-94-6
MF: C32H26N4O2.HCl
MW: 535.04
EINECS: 1312995-182-4
Product Categories: Aromatics;Intermediates & Fine Chemicals;Inhibitors;Pharmaceuticals
Mol File: 168626-94-6.mol
Conivaptan hydrochloride Structure
Conivaptan hydrochloride Chemical Properties
Melting point  >250°

Conivaptan hydrochloride Usage And Synthesis
Description Arginine vasopressin is intimately involved in volume homeostasis, and elevated levels of arginine vasopressin are responsible for the pathogenesis and progression of diseases with an imbalance of sodium and water, particularly congestive heart failure. To restore homeostasis, antagonism of vasopressin receptors is a practical solution. As such, conivaptan has been developed and launched as a dual V1a and V2 vasopressin receptor antagonist. As a competitive, reversible inhibitor of both subtypes, conivaptan can modulate systemic vascular resistance through the V1a receptor (Ki 0.48 nM) distributed in vascular smooth muscle cells, cardiomyocytes, hepatocytes, and platelets and blocks the renal V2 receptor (Ki 3.04 nM) resulting in enhanced diuresis, thereby increasing serum sodium concentration and reducing total body volume. Currently, the drug is approved for the management of refractory hyponatremia and potentially lifethreatening sodium and water imbalance, but it has shown promise as a potential treatment option for other diseases, such as congestive heart failure, syndrome of antidiuretic hormone, diabetes insipidus, and liver cirrhosis.
Chemical Properties White to Off-White Solid
Originator Yamanouchi (Japan)
Uses Conivaptan is a non-peptide inhibitor of antidiuretic hormone (vasopressin receptor antagonist).
Uses Used in treatment of congestive heart failure.
Definition ChEBI: The hydrochloride salt of conivaptan. It is an antagonist for two of the three types of arginine vasopressin (AVP) receptors, V1a and V2, and is used for the treatment of hyponatraemia (low blood sodium levels) cau ed by syndrome of inappropriate antidiuretic hormone (SIADH).