210101-16-9
Chemical Structure
Conivaptan
Synonym(s): YM 087 free base
- CAS No.: 210101-16-9
- Formula:C32H26N4O2
- Molecular Weight:498.57
IUPAC Name: N-(4-(2-methyl-1,4,5,6-tetrahydrobenzo[b]imidazo[4,5-d]azepine-6-carbonyl)phenyl)-[1,1'-biphenyl]-2-carboxamide
InChIKey: IKENVDNFQMCRTR-UHFFFAOYSA-N
SMILES: O=C(C1=C(C2=CC=CC=C2)C=CC=C1)NC3=CC=C(C(N4C5=C(C6=C(CC4)N=C(C)N6)C=CC=C5)=O)C=C3
Biological Activity: Conivaptan (YM 087 free base) is an orally active dual vasopressin V1a/V2 receptor antagonist with Ki values of 0.48 nM and 3.04 nM for vasopressin V1a receptor and V2 receptor, respectively. Conivaptan competitively and reversibly blocks vasopressin-mediated antidiuresis, vasoconstriction, and cellular hypertrophy, while inhibiting CYP3A4. Conivaptan inhibits vasopressin-induced intracellular calcium, cAMP, and mitogen-activated kinase activation in vascular smooth muscle cells and cardiomyocytes. Conivaptan induces water diuresis while improving hemodynamics in heart failure models, reducing left ventricular end-diastolic pressure, vascular resistance, and organ weight. Conivaptan is used for research on hyponatremia and congestive heart failure[1][2].
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Conivaptan | Conivaptan (YM 087 free base) is an orally active dual vasopressin V1a/V2 receptor antagonist with Ki values of 0.48 nM and 3.04 nM for vasopressin V1a receptor and V2 receptor, respectively. Conivaptan competitively and reversibly blocks vasopressin-mediated antidiuresis, vasoconstriction, and cellular hypertrophy, while inhibiting CYP3A4. Conivaptan inhibits vasopressin-induced intracellular calcium, cAMP, and mitogen-activated kinase activation in vascular smooth muscle cells and cardiomyocytes. Conivaptan induces water diuresis while improving hemodynamics in heart failure models, reducing left ventricular end-diastolic pressure, vascular resistance, and organ weight. Conivaptan is used for research on hyponatremia and congestive heart failure. | |||||||||||||||||||||
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References
- [1]. Ali F, et al. Conivaptan: A Dual Receptor Vasopressin V1a/V2 Antagonist. Cardiovascular Drug Reviews, 2007, 25(3): 261-279.
- [2]. Wada K, et al. Effect of the vasopressin receptor antagonist conivaptan in rats with heart failure following myocardial infarction. European journal of pharmacology. 2002 Aug 23;450(2):169-77.
