| Identification | Back Directory | [Name]
3H-1,2,4-Triazol-3-one, 5-(4-chlorophenyl)-2-[[1-(3-chlorophenyl)-5-[(1S)-1-hydroxyethyl]-1H-1,2,4-triazol-3-yl]methyl]-2,4-dihydro-4-[(2S)-3,3,3-trifluoro-2-hydroxypropyl]- | [CAS]
1914998-56-3 | [Synonyms]
Pecavaptan
3H-1,2,4-Triazol-3-one, 5-(4-chlorophenyl)-2-[[1-(3-chlorophenyl)-5-[(1S)-1-hydroxyethyl]-1H-1,2,4-triazol-3-yl]methyl]-2,4-dihydro-4-[(2S)-3,3,3-trifluoro-2-hydroxypropyl]- | [Molecular Formula]
C22H19Cl2F3N6O3 | [MOL File]
1914998-56-3.mol | [Molecular Weight]
543.33 |
| Hazard Information | Back Directory | [Uses]
Pecavaptan is an orally active and dual antagonist of V1a/V2 receptor (Ki=0.5 nM and 0.6 nM for human, respectively). Pecavaptan promotes an increase in urine production, which reduces the associated symptoms of water retention and edema[1]. | [in vivo]
Pecavaptan (0.01, 0.03, 0.1 and 0.3 mg/kg; IV; single dose) protects from arginine vasopressin (AVP)-mediated cardiac output (CO) in canine tachypacing-induced model of heart failure (HF)[1].
| [IC 50]
human V1a Receptor: 3.6 nM (IC50); canine V1a Receptor: 4.4 nM (IC50); human V2 Receptor: 1.7 nM (IC50); canine V2 Receptor: 1.3 nM (IC50) | [References]
[1] Mondritzki T, et al. Cardiac output improvement by pecavaptan: a novel dual-acting vasopressin V1a/V2 receptor antagonist in experimental heart failure. Eur J Heart Fail. 2021 May;23(5):743-750. DOI:10.1002/ejhf.2001 |
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