2072803-95-1
Chemical Structure
Olprinone hydrochloride hydrate
Synonym(s): Loprinone hydrochloride hydrate
- CAS No.: 2072803-95-1
- Formula:C14H13ClN4O2
- Molecular Weight:304.73
InChIKey: BFZDXWYVGHGCMK-UHFFFAOYSA-N
SMILES: CC(N1)=C(C=C(C#N)C1=O)C2=CN3C(C=C2)=NC=C3.Cl.O
Biological Activity: Olprinone (Loprinone) hydrochloride hydrate is a potent and selective phosphodiesterase 3 (PDE3) inhibitor, with IC50 values of 150, 100, 0.35, and 14 μM against PDE1, PDE2, PDE3, and PDE4, respectively. Olprinone hydrochloride hydrate exerts comprehensive protective effects including anti-inflammatory, antioxidant, and anti-apoptotic activities by elevating intracellular cAMP levels and inhibiting the NF-κB and MAPK signaling pathways. Olprinone hydrochloride hydrate can be used in studies related to lung injury, spinal cord injury, heart failure, myocardial ischemia-reperfusion injury, and cerebral ischemic injury[1][2][3][4][5][6][7].
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Olprinone hydrochloride hydrate | Olprinone (Loprinone) hydrochloride hydrate is a potent and selective phosphodiesterase 3 (PDE3) inhibitor, with IC50 values of 150, 100, 0.35, and 14 μM against PDE1, PDE2, PDE3, and PDE4, respectively. Olprinone hydrochloride hydrate exerts comprehensive protective effects including anti-inflammatory, antioxidant, and anti-apoptotic activities by elevating intracellular cAMP levels and inhibiting the NF-κB and MAPK signaling pathways. Olprinone hydrochloride hydrate can be used in studies related to lung injury, spinal cord injury, heart failure, myocardial ischemia-reperfusion injury, and cerebral ischemic injury. | |||||||||||||||||||||
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Olprinone hydrochloride solution | Olprinone hydrochloride solution is mainly composed of Olprinone hydrochloride hydrate (HY-14254B). Olprinone hydrochloride hydrate is a potent phosphodiesterase (PDE) 3 inhibitor, with IC50s of 150, 100, 0.35 and 14 μM for PDE1, PDE2, PDE3 and PDE4, respectively. Olprinone hydrochloride hydrate has anti-inflammatory activity, and is used for the research of heart failure due to its positive inotropic and vasodilative effects. Anti-inflammatory activity | |||||||||||||||||||||
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References
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[1]. Sugioka M, 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 isoenzymes. Naunyn Schmiedebergs Arch Pharmacol. 1994 Sep;350(3):284-93.
[Content Brief] - [2]. Koike T, et al. Pretreatment with olprinone hydrochloride, a phosphodiesterase III inhibitor, attenuates lipopolysaccharide-induced lung injury via an anti-inflammatory effect. Pulmonary pharmacology & therapeutics. 2008;21(1):166-71. [Content Brief]
- [3]. Esposito E, et al. Olprinone attenuates the acute inflammatory response and apoptosis after spinal cord trauma in mice. PloS one. 2010 Sep 07;5(9):e12170.
- [4]. Mokra D, et al. Selective phosphodiesterase 3 inhibitor olprinone attenuates meconium-induced oxidative lung injury. Pulmonary pharmacology & therapeutics. 2012 Jun;25(3):216-22. [Content Brief]
- [5]. Di Paola R, et al. Olprinone, a PDE3 inhibitor, modulates the inflammation associated with myocardial ischemia-reperfusion injury in rats. European journal of pharmacology. 2011 Jan 15;650(2-3):612-20. [Content Brief]
- [6]. Genovese T, et al. Neuroprotective effects of olprinone after cerebral ischemia/reperfusion injury in rats. Neuroscience letters. 2011 Oct 03;503(2):93-9. [Content Brief]
- [7]. Mizushige K, et al. Olprinone: a phosphodiesterase III inhibitor with positive inotropic and vasodilator effects. Cardiovasc Drug Rev. 2002 Fall;20(3):163-74.
