Mozavaptan-d₆  (Synonyms: OPC-31260-d₆)

Mozavaptan-d6 (OPC-31260-d6) is the deuterium labeled Mozavaptan. Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V₂ receptor antagonist with an IC₅₀ of 14 nM. Mozavaptan shows ~85-fold selectivity for V₂ receptor over V₁ receptor (IC₅₀ of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment^[1][2].

1. This compound can be used as a tracer.
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

433.58

C₂₇H₂₃D₆N₃O₂

2750534-83-7

137975-06-5

O=C(C1=CC=C(C=C1)NC(C2=C(C=CC=C2)C)=O)N3C4=CC=CC=C4C(CCC3)N(C([2H])([2H])[2H])C([2H])([2H])[2H]

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.  [Content Brief]

  [2]. Yamamura Y, et al. Characterization of a novel aquaretic agent, OPC-31260, as an orally effective, nonpeptide vasopressin V2 receptor antagonist. Br J Pharmacol. 1992 Apr;105(4):787-91.  [Content Brief]

  [3]. Yamaguchi K, et al. Clinical implication of the antidiuretic hormone (ADH) receptor antagonist mozavaptan hydrochloride in patients with ectopic ADH syndrome. Jpn J Clin Oncol. 2011 Jan;41(1):148-52.  [Content Brief]