| Identification | Back Directory | [Name]
Revizinone | [CAS]
133718-29-3 | [Synonyms]
R 80122
Revizinone
R 80122;R80122;R-80122
Acetamide, N-cyclohexyl-N-methyl-2-[[(E)-[phenyl(1,2,3,5-tetrahydro-2-oxoimidazo[2,1-b]quinazolin-7-yl)methylene]amino]oxy]- | [Molecular Formula]
C26H29N5O3 | [MDL Number]
MFCD00867129 | [MOL File]
133718-29-3.mol | [Molecular Weight]
459.54 |
| Chemical Properties | Back Directory | [Boiling point ]
627.7±65.0 °C(Predicted) | [density ]
1.33±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : ≥ 4.6 mg/mL (10.01 mM) | [form ]
Solid | [pka]
2.99±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Revizinone is a novel selective phosphodiesterase (PDE) inhibitor with IC50 values on this enzyme to 0.036 microM.
target: phosphodiesterase (PDE)[3];
IC 50: 0.036 microM; [3]
In vivo: The administration of Revizinone improved the haemodynamic profile with an increase in cardiac output, a decrease in systemic vascular resistance and a stable heart rate and mean arterial blood pressure. [1] With regard to reconstitution of contractility and cardiac function Revizinone (E-isomer) was 10 fold more potent than R 79595 and nearly 100 fold more potent than R 80123 (Z-isomer). [2] Revizinone significantly increased global LV function and systolic wall thickening in ischemic areas at doses greater than or equal to 0.16 mg/kg i.v. [4] | [References]
[1] Herregods L et al. Haemodynamic effects of R 80122 immediately after cardiopulmonary bypass; preliminary results. Anaesthesia. 1994 Aug;49(8):719-22. DOI:10.1111/j.1365-2044.1994.tb04409.x
[2] Schneider J et al. Cardiac effects of R 79595 and its isomers (R 80122 and R 80123) in an acute heart failure model. A new class of cardiotonic agents with highly selective phosphodiesterase III inhibitory properties. Naunyn Schmiedebergs Arch Pharmacol DOI:10.1007/BF00169014
[3] de Cheffoy de Courcelles D et al. Inhibition of human cardiac cyclic AMP-phosphodiesterases by R 80122, a new selective cyclic AMP-phosphodiesterase III inhibitor: a comparison with other cardiotonic compounds. J Pharmacol Exp Ther. 1992 Oct;263(1):6-14. PMID:1328613
[4] Vandeplassche GM et al. Comparative effects of R 80122, enoximone, and milrinone on left ventricular phosphodiesterase isoenzymes in vitro and on contractility of normal and stunned myocardium in vivo in dogs. J Cardiovasc Pharmacol. 1992 May;19(5):714-22 PMID:1381769 |
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