Conivaptan hydrochloride 是一种口服有效的加压素 V2 和 V1A 受体拮抗剂,用于治疗高血容量性低钠血症和正常血容量。
产品描述
Conivaptan HCl is an orally active vasopressin V2 and V1A receptor antagonist, used in the therapy of hypervolemic hyponatremia and euvolemic.
体内活性
Conivaptan (0.03, 0.1 and 0.3 mg/kg i.v.) increases urine volume and reduces urine osmolality in both myocardial infarction and sham-operated rats in dose-dependent manner. Conivaptan (0.3 mg/kg i.v.) significantly reduces right ventricular systolic pressure, left ventricular end-diastolic pressure, lung/body weight and right atrial pressure in myocardial infarction rats. Conivaptan (0.3 mg/kg i.v.) significantly increases dP/dt(max)/left ventricular pressure in myocardial infarction rats. [1] Conivaptan produces an acute increase in urine volume (UV), a reduction in osmolality (UOsm) and, at the end of the investigation, cirrhotic rats receiving the V(1a)/V(2)-AVP receptor antagonist does not show hyponatremia or hypoosmolality. Conivaptan also normalizes U(Na)V without affecting creatinine clearance and arterial pressure. [2] Conivaptan (0.01 to 0.1 mg/kg i.v.) exerts a dose-dependent diuretic effect in dogs without an increase in the urinary excretion of electrolytes, inhibits 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.), almost completely blocks vasoconstriction caused by exogenous vasopressin. Conivaptan (0.1 mg/kg i.v.) improves cardiac function, as evidenced by significant increases in left ventricular dP/dtmax, cardiac output and stroke volume, and reduces preload and afterload, as evidenced by significant decreases in left ventricular end-diastolic pressure and total peripheral vascular resistance in dogs with congestive heart failure. [3]
Cas No.
168626-94-6
分子式
C32H27ClN4O2
分子量
535.04
别名
盐酸考尼伐坦;Vaprisol;Conivaptan HCl;YM 087
储存和溶解度
DMSO:99 mg/mL (185 mM)
Ethanol:7 mg/mL (13.08 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years