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Conivaptan hydrochloride

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Chemical Structure| 168626-94-6 同义名 : YM 087;Conivaptan (hydrochloride);Conivaptan HCl
CAS号 : 168626-94-6
货号 : A277387
分子式 : C32H27ClN4O2
纯度 : 98%
分子量 : 535.035
MDL号 : MFCD00945712
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(196.25 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Vasopressin receptor 1
描述 Conivaptan (Hydrochloride) is a non-peptide antagonist of vasopressin receptor, with Ki values of 0.48 and 3.04 nM for rat liver V1A receptor and rat kidney V2 receptor respectively. At 4 weeks after coronary occlusion, conivaptan (0.03, 0.1 and 0.3 mg/kg i.v.) dose-dependently increased urine volume and reduced urine osmolality in both myocardial infarction and sham-operated rats. 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 myocardial infarction rats. Moreover, conivaptan (0.3 mg/kg i.v.) significantly increased dP/dt(max)/left ventricular pressure[3]. 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[4]. 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[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00811486 Right Heart Failure ... 展开 >> Pulmonary Hypertension 收起 << Not Applicable Withdrawn(Only 1 patient recru... 展开 >>ited, and he withdrew) 收起 << - United States, Colorado ... 展开 >> University of Colorado at Denver and Health Sciences Center General Clinical Research Center Denver, Colorado, United States, 80262 收起 <<
NCT01954290 Acute Cerebrovascular Accident... 展开 >> Cerebral Edema 收起 << Phase 2 Withdrawn(Investigator is leav... 展开 >>ing the institution.) 收起 << - -
NCT00380575 Hyponatremia Phase 3 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.87mL

0.37mL

0.19mL

9.35mL

1.87mL

0.93mL

18.69mL

3.74mL

1.87mL
参考文献

[1]Wada K, Fujimori A, et al. Intravenous administration of conivaptan hydrochloride improves cardiac hemodynamics in rats with myocardial infarction-induced congestive heart failure. Eur J Pharmacol. 2005 Jan 10;507(1-3):145-51.

[2]Fernandez-Varo G, Ros J, et al. Effect of the V1a/V2-AVP receptor antagonist, Conivaptan, on renal water metabolism and systemic hemodynamics in rats with cirrhosis and ascites. J Hepatol. 2003 Jun;38(6):755-61.

[3]Wada K, Fujimori A, Matsukawa U, Arai Y, Sudoh K, Yatsu T, Sasamata M, Miyata K. Intravenous administration of conivaptan hydrochloride improves cardiac hemodynamics in rats with myocardial infarction-induced congestive heart failure. Eur J Pharmacol. 2005 Jan 10;507(1-3):145-51

[4]Fernández-Varo G, Ros J, Cejudo-Martín P, Cano C, Arroyo V, Rivera F, Rodés J, Jiménez W. Effect of the V1a/V2-AVP receptor antagonist, Conivaptan, on renal water metabolism and systemic hemodynamics in rats with cirrhosis and ascites. J Hepatol. 2003 Jun;38(6):755-61

[5]Yatsu T, Tomura Y, Tahara A, Wada K, Kusayama T, Tsukada J, Tokioka T, Uchida W, Inagaki O, Iizumi Y, Tanaka A, Honda K. Cardiovascular and renal effects of conivaptan hydrochloride (YM087), a vasopressin V1A and V2 receptor antagonist, in dogs with pacing-induced congestive heart failure. Eur J Pharmacol. 1999 Jul 9;376(3):239-46