盐酸考尼伐坦 T6453

Product Introduction
Bioactivity


英文名: Conivaptan hydrochloride

描述: Conivaptan hydrochloride (Vaprisol) 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。

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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 7 mg/mL (13.08 mM)
DMSO : 99 mg/mL (185 mM)


关键字: Vasopressin Receptor | inhibit | YM087 | Conivaptan | Conivaptan Hydrochloride | YM-087 | Inhibitor | Conivaptan hydrochloride

相关产品: Terlipressin Acetate | Fuscoside | Invopressin | Atosiban acetate | Vasopressin Dimer (parallel) (TFA) | RG7713 | Desmopressin acetate (16679-58-6 free base) | Felypressin acetate | Dp[Tyr(methyl)2,Arg8]-Vasopressin | Fedovapagon

相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | GPCR Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Orally Active Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途