R 80123

R 80123 is the Z-isomer of R 79595, is also a highly selective phosphodiesterase inhibitor. The fuction is similar to R 80122 (HY-100615, Revizinone) . 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) is 10 fold more potent than R 79595 and nearly 100 fold more potent than R 80123 (Z-isomer) . [2] Revizinone significantly increases global LV function and systolic wall thickening in ischemic areas at doses greater than or equal to 0.16 mg/kg i.v. [3]

Product Specifications

CAS Number

[133718-30-6]

UNSPSC

12352005

Target

Phosphodiesterase (PDE)

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/R-80123.html

Purity

98.0

Solubility

10 mM in DMSO

Smiles

O=C(N(C1CCCCC1)C)CO/N=C(C2=CC=CC=C2)\C3=CC4=C(N=C(NC(C5)=O)N5C4)C=C3

Molecular Formula

C26H29N5O3

Molecular Weight

459.54

References & Citations

[1]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. https://www.ncbi.nlm.nih.gov/pubmed/ 1381769|[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. 1992 Nov;346 (5) :563-72.|[3]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.