Olprinone (hydrochloride)

Olprinone is an inhibitor of phosphodiesterase 3 (PDE3, IC50 = 0.35 µM for human cardiac enzyme). 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). 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. 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-1beta, and intercellular adhesion molecule 1 (ICAM-1) in a rat model of cerebral ischemia-reperfusion injury. It inhibits neutrophil infiltration into the lungs and inhibits increases in serum levels of TNF-alpha and IL-6 in a rat model of LPS-induced lung inflammation when administered at a dose of 0.2 mg/kg.Formal Name: 1,2-dihydro-5-imidazo[1,2-a]pyridin-6-yl-6-methyl-2-oxo-3-pyridinecarbonitrile, monohydrochloride. CAS Number: 119615-63-3. Synonyms: Loprinone. Molecular Formula: C14H10N4O . HCl. Formula Weight: 286.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. lambdamax: 219, 262, 345 nm. SMILES: O=C1C(C#N)=CC(C2=CN3C(C=C2)=NC=C3)=C(C)N1.Cl. InChi Code: InChI=1S/C14H10N4O.ClH/c1-9-12(6-11(7-15)14(19)17-9)10-2-3-13-16-4-5-18(13)8-10,/h2-6,8H,1H3,(H,17,19),1H. InChi Key: PWTBMBAQRAOAFF-UHFFFAOYSA-N.