Conivaptan hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Conivaptan (YM-087) 是一种有效的选择性非肽加压素 V1A 和 V2 受体拮抗剂，Ki 分别为 0.48 nM 和 3.04 nM。

Conivaptan (YM-087)?is a potent, selective nonpeptide vasopressin V1A and V2 receptor antagonist with Ki of 0.48 nM and 3.04 nM respectively; less potent for OT receptors and no effect on V1B receptor; blocks AVP-induced cAMP production of cultured renal epithelium cells concentration dependently and has no agonistic activities.Other Indication Approved(In Vivo):Conivaptan (0.03, 0.1 and 0.3 mg/kg, i.v.) dose-dependently increases urine volume and reduces urine osmolality in both myocardial infarction and sham-operated rats. 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. 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. 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.

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Conivaptan (0.03, 0.1 and 0.3 mg/kg, i.v.) dose-dependently increases urine volume and reduces urine osmolality in both myocardial infarction and sham-operated rats. 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. 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. 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.

YM-087

GPCR/G Protein

Vasopressin Receptor

vasopressinreceptor1a|vasopressinreceptor2

Other Indications

Other Disease

168626-94-6

535.0354

C32H27ClN4O2

>98% (HPLC)

10 mM in DMSO

O=C(NC1=CC=C(C(N2CCC(NC(C)=N3)=C3C4=CC=CC=C42)=O)C=C1)C5=CC=CC=C5C6=CC=CC=C6.[H]Cl

[1,1'-Biphenyl]-2-carboxamide, N-[4-[(4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl]-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years