Author/Authors :
Ajay Purohit، نويسنده , , Richard Benetti، نويسنده , , Megan Hayes، نويسنده , , Mary Guaraldi، نويسنده , , Mikhail Kagan، نويسنده , , Padmaja Yalamanchilli، نويسنده , , Fran Su، نويسنده , , Michael Azure، نويسنده , , Mahesh Mistry، نويسنده , , Ming Yu، نويسنده , , Simon Robinson، نويسنده , , Douglas D. Dischino، نويسنده , , David Casebier، نويسنده ,
Abstract :
Several quinazoline derivatives were made as mitochondrial complex 1 inhibitors. Compound 4 showed an IC50 of 11.3 nM and was the most potent compound of this series. The 18F analog of 4, [18F] 4, was injected in the rat and showed high and rapid heart uptake, fast liver clearance, and low blood uptake. Images obtained using a μPET showed clear delineation of the myocardium in normal rats and perfusion deficit in ischemic rats. In the non-human primate, [18F] 4 showed rapid uptake and clearance from the myocardium and high liver uptake.
Keywords :
Quinazoline derivatives , MC-I inhibitors , positron emission tomography , myocardial perfusion
