A vasopressin V1A and V2 receptor antagonist (Kis = 0.48 and 3.04 nM for rat liver V1A and kidney V2

Conivaptan (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
168626-94-6
Storage:
4
UN-No:
Non-Hazardous - /

Conivaptan is an antagonist of the arginine vasopressin (AVP) receptors V1A and V2 (Kis = 0.48 and 3.04 nM for rat liver V1A and kidney V2, respectively).{38430} It also competitively inhibits oxytocin binding to rat uterine oxytocin receptors (Ki = 44 nM) but has no effect on AVP binding to anterior pituitary V1B receptors at concentrations up to 100 μM in a radioligand binding assay. Conivaptan suppresses AVP-induced increases in intracellular calcium in vascular smooth muscle cells (VSMCs) in vitro and the pressor response in pithed rats. Conivaptan (0.01-0.3 mg/kg, i.v.) increases urine output and decreases urine osmolality in dehydrated conscious rats in a dose-dependent manner. It also reduces brain edema and blood-brain barrier disruption in a mouse experimental stroke model.{38431}  

 

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SKU: 23728 - 5 mg Category:

Description

A vasopressin V1A and V2 receptor antagonist (Kis = 0.48 and 3.04 nM for rat liver V1A and kidney V2, respectively); competitively inhibits oxytocin binding to rat uterine oxytocin receptors (Ki = 44 nM) but has no effect on AVP binding to anterior pituitary V1B receptors at concentrations up to 100 μM in a radioligand binding assay; suppresses AVP-induced increases in intracellular calcium in VSMCs and the pressor response in pithed rats; increases urine output and decreases urine osmolality in dehydrated conscious rats in a dose-dependent manner; reduces brain edema and blood-brain barrier disruption in a mouse experimental stroke model,

Formal name: N-[4-[(4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl]-[1,1′-biphenyl]-2-carboxamide, monohydrochloride

Synonyms:  YM-087

Molecular weight: 535

CAS: 168626-94-6

Purity: ≥95%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Cardiovascular Diseases|Stroke||Research Area|Cardiovascular System|Kidney & Renal Disease||Research Area|Cardiovascular System|Vasculature|Smooth Muscle Cells||Research Area|Neuroscience|Neuroprotection|Ischemia

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