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My CartCAS：168626-94-6
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to yellow Solid
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| CAS | 168626-94-6 |
| Name | Conivaptan Hydrochloride |
| Molecular Formula | C32H26N4O2·HCl |
| Molecular Weight | 535.04 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 1312995-182-4 |
| MDL | MFCD00945712 |
| SMILES | O=C(C1=CC=CC=C1C2=CC=CC=C2)NC3=CC=C(C(N4CCC(N=C(C)N5)=C5C6=CC=CC=C64)=O)C=C3.Cl |
| Target Point | Vasopressin Receptor |
| Passage | GPCR & G Protein |
| Background | It is a non-peptide vasopressin receptor antagonist. |
| Biological Activity | Conivaptan hydrochloride 是一种非肽段类的 vasopressin receptor 拮抗剂，能够抑制大鼠肝脏的 V1A 受体 和 肾脏的 V2 受体，Ki 值分别为 0.48 和 3.04 nM。[1-3] |
| In Vivo | Conivaptan(0.03，0.1和0.3 mg / kg，iv)剂量依赖性地增加尿量并降低心肌梗塞和假手术大鼠的尿渗透压。 Conivaptan(0.3 mg / kg iv)显著降低心肌梗塞大鼠的右心室收缩压，左心室舒张末压，肺/体重和右心房压。 Conivaptan(0.3 mg / kg iv)显著增加心肌梗死大鼠的dP / dt(max)/左心室压力[1]。 Conivaptan产生尿量(UV)急剧增加，渗透压降低(UOsm)，并且在研究结束时，接受V(1a)/ V(2)-AVP受体拮抗剂的肝硬化大鼠不显示低钠血症或hypoosmolality。 Conivaptan也使U(Na)V正常化而不影响肌酐清除率和动脉压[2]。 Conivaptan(0.01至0.1 mg / kg，iv)在狗中发挥剂量依赖性利尿作用而不增加电解质的尿排泄，以剂量依赖性方式抑制外源性加压素的升压作用(0.003至0.1 mg / kg)iv)并且，在最高剂量(0.1mg / kg静脉注射)下，几乎完全阻断由外源性血管加压素引起的血管收缩。 Conivaptan(0.1 mg / kg，iv)改善心脏功能，左心室dP / dtmax，心输出量和每搏输出量显著增加，并减少预负荷和后负荷，左心室舒张末期压力显著降低和充血性心力衰竭犬的总外周血管阻力[3]。 |
| Animal Experiment | 手术后4周，39只心肌梗死大鼠存活。随机选择30例无偏倚，分为5组，使组间梗死面积和体重的分布相似，给予载体，conivaptan(0.03，0.1和0.3 mg / kg)或SR121463A(0.3 mg / kg)静脉给药。假大鼠也被分成四组，并通过静脉内给药给予载体或conivaptan(0.03，0.1和0.3mg / kg)。然后将大鼠单独置于代谢笼中并收集尿液3小时。使用渗透压计通过冰点降低法测量尿渗透压。 |
| Data Literature Source | [1]. Wada K，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. Epub 2005 Jan 1. [2]. Fernandez-Varo G，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]. Yatsu T，et al. 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 |
| Unit | Bottle |
| Specification | 10mg 10mM*1mL in DMSO 25mg |
一种非肽段类的 vasopressin receptor 拮抗剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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