Name | Conivaptan hydrochloride |
Synonyms | Vaprisol Conivaptan HCI Conivaptan HCl Unii-75L57R6X36 Conivaptan hydrochloride Conivaptan hydrochkoride Conivaptan hydrochloride [usan] N-[4-[(4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl]-, monohydrochloride N-{4-[(2-Methyl-4,5-dihydroimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl}biphenyl-2-carboxamidhydrochlorid N-{4-[(2-methyl-4,5-dihydroimidazo[4,5-d][1]benzazépin-6(1H)-yl)carbonyl]phenyl}biphenyl-2-carboxamide chlorhydrate N-{4-[(2-methyl-4,5-dihydroimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl}biphenyl-2-carboxamide hydrochloride N-[4-[(4,5-Dihydro-2-MethyliMidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl]-[1,1'-Biphenyl]-2-carboxaMide Hydrochloride (1,1'-Biphenyl)-2-carboxamide, N-(4-((4,5-dihydro-2-methylimidazo(4,5-D)(1)benzazepin-6(1H)-yl)carbonyl)phenyl)-, monohydrochloride [1,1'-biphenyl]-2-carboxamide, N-[4-[(4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl]-, monohydrochloride |
CAS | 168626-94-6 |
EINECS | 1312995-182-4 |
InChI | InChI=1/C32H26N4O2.ClH/c1-21-33-28-19-20-36(29-14-8-7-13-27(29)30(28)34-21)32(38)23-15-17-24(18-16-23)35-31(37)26-12-6-5-11-25(26)22-9-3-2-4-10-22;/h2-18H,19-20H2,1H3,(H,33,34)(H,35,37);1H |
Molecular Formula | C32H26N4O2.HCl |
Molar Mass | 535.04 |
Melting Point | >250° |
Boling Point | 751.2°C at 760 mmHg |
Flash Point | 408.1°C |
Solubility | Soluble in DMSO (107 mg/ml at 25 °C), ethanol (7 mg/ml at 25 °C), and water (<1 mg/ |
Vapor Presure | 1.89E-22mmHg at 25°C |
Appearance | Solid |
Color | White to Off-White |
Storage Condition | under inert gas (nitrogen or Argon) at 2-8°C |
Use | A non-peptide inhibitor of antidiuretic hormone |
In vivo study | In myocardial infarction and sham-operated rats, Conivaptan(0.03,0.1, and 0.3 mg/kg, I. V.) dose-dependently increased urine output and decreased urine osmolality. In rats with myocardial infarction, Conivaptan(0.3 mg/kg, I. V.) significantly reduced right ventricular systolic pressure, left ventricular end-diastolic pressure, lung/body weight, and right atrial pressure. In rats with myocardial infarction, Conivaptan(0.3 mg/kg, I. V.) significantly increased dP/dt (Max)/left ventricular pressure. Conivaptan produces an acute increase in urine volume (UV) and a decrease in osmolality (UOSM). At the end of the treatment, V(1a)/V(2)-AVP receptor antagonist treated cirrhotic rats did not show hyponatremia or hypotonicity. Conivaptan also restored U(Na)V without affecting creatinine clearance and blood pressure. In dogs, Conivaptan(0.01 to 0.1 mg/kg, I. V.) exerts a dose-dependent diuretic effect without increasing the urinary excretion of electrolytes, inhibited the pressor effect of exogenous vasopressin in a dose-dependent manner (0.003 to 0.1 mg/kg, I. V.) and, at the highest dose (0.1 mg/kg, I. V.), it almost completely blocks the vasoconstriction induced by exogenous vasopressin. Conivaptan(0.1 mg/kg, I. V.) improves cardiac function as evidenced by a significant increase in left ventricular dP/dt Maxima, cardiac output and stroke volume. In dogs with congestive heart failure, Conivaptan (0.1 mg/kg, I. V.) reduced anteroposterior load, as evidenced by a significant decrease in left ventricular end-diastolic pressure and total peripheral vascular resistance. |
Reference Show more | 1. [IF=4.411] Xin Meng et al."Drug Repurposing for Influenza Virus Polymerase Acidic (PA) Endonuclease Inhibitor."Molecules. 2021 Jan;26(23):7326 |