1129433-63-1
Chemical Structure
Conivaptan-d4
Synonym(s): YM 087-d4
- CAS No.: 1129433-63-1
- Formula:C32H22D4N4O2
- Molecular Weight:502.60
IUPAC Name: N-(4-(2-methyl-1,4,5,6-tetrahydrobenzo[b]imidazo[4,5-d]azepine-6-carbonyl)phenyl-2,3,5,6-d4)-[1,1'-biphenyl]-2-carboxamide
InChIKey: IKENVDNFQMCRTR-OCOLLXALSA-N
SMILES: O=C(C1=C([2H])C([2H])=C(NC(C2=C(C3=CC=CC=C3)C=CC=C2)=O)C([2H])=C1[2H])N4C5=CC=CC=C5C6=C(N=C(C)N6)CC4
Biological Activity: Conivaptan-d4 (YM 087-d4) is the deuterated-labeled Conivaptan (HY-18347). 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-d4 | Conivaptan-d4 (YM 087-d4) is the deuterated-labeled Conivaptan (HY-18347). 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.
