Olprinone

Olprinone is an inhibitor of phosphodiesterase 3 (PDE3; IC₅₀ = 0.35 μM for human cardiac enzyme).¹ It is selective for PDE3 over PDE1 and PDE2 (IC₅₀s = 150 and 100 μM, respectively). Olprinone induces relaxation of precontracted isolated rabbit renal and carotid arterial rings (IC₅₀s = 40 and 103 nM, respectively).² It reduces infarct size and improves cardiac function in a rat model of myocardial ischemia-reperfusion injury when administered at a dose of 0.6 mg/kg twice per day.³ Olprinone (0.2 mg/kg) reduces cortical and striatal damage, as well as reduces injured cerebral tissue nitrotyrosine formation, apoptosis, and levels of inducible nitric oxide synthase (iNOS), IL-1β, and intercellular adhesion molecule 1 (ICAM-1) in a rat model of cerebral ischemia-reperfusion injury.⁴ It inhibits neutrophil infiltration into the lungs and inhibits increases in serum levels of TNF-α and IL-6 in a rat model of LPS-induced lung inflammation when administered at a dose of 0.2 mg/kg.⁵

1.Sugioka, M., Masuoka, H., Ichikawa, K., et al.Identification and characterization of isoenzymes of cyclic nucleotide phosphodiesterase in human kidney and heart, and the effects of new cardiotonic agents on these isoenzymesNaunyn. Schmiedebergs. Arch. Pharmacol.350(3)284-293(1994) 2.Minonishi, T., Ogawa, K., Tokinaga, Y., et al.Differential vasodilation response to olprinone in rabbit renal and common carotid arteriesJ. Anesth.24(1)61-66(2010) 3.Han, M.-X., Xu, X.-W., Lu, S.-Q., et al.Effect of olprinone on ischemia-reperfusion induced myocardial injury in ratsBiomed. Pharmacother.1111005-1012(2019) 4.Genovese, T., Mazzon, E., Paterniti, I., et al.Neuroprotective effects of olprinone after cerebral ischemia/reperfusion injury in ratsNeurosci. Lett.503(2)93-99(2011) 5.Koike, T., Nadeen Qutab, M., Tsuchida, M., et al.Pretreatment with olprinone hydrochloride, a phosphodiesterase III inhibitor, attenuates lipopolysaccharide-induced lung injury via an anti-inflammatory effectPulm. Pharmacol.21(1)166-171(2008)