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ChemicalBook--->CAS DataBase List--->133718-29-3

133718-29-3

133718-29-3 Structure

133718-29-3 Structure
IdentificationBack 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 PropertiesBack 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 InformationBack 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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