Sander, Kerstin; Galante, Eva; Gendron, Thibault; Yiannaki, Elena; Patel, Niral; Kalber, Tammy L.; Badar, Adam; Robson, Mathew; Johnson, Sean P.; Bauer, Florian; Mairinger, Severin; Stanek, Johann; Wanek, Thomas; Kuntner, Claudia; Kottke, Tim; Weizel, Lilia; Dickens, David; Erlandsson, Kjell; Hutton, Brian F.; Lythgoe, Mark F.; Stark, Holger; Langer, Oliver; Koepp, Matthias; Arstad, Erik published the artcile< Development of Fluorine-18 Labeled Metabolically Activated Tracers for Imaging of Drug Efflux Transporters with Positron Emission Tomography>, SDS of cas: 128577-47-9, the main research area is fluorine 18 PET tracer imaging drug efflux transporter.
Increased activity of efflux transporters, e.g., P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), at the blood-brain barrier is a pathol. hallmark of many neurol. diseases, and the resulting multiple drug resistance represents a major clin. challenge. Noninvasive imaging of transporter activity can help to clarify the underlying mechanisms of drug resistance and facilitate diagnosis, patient stratification, and treatment monitoring. We have developed a metabolically activated radiotracer for functional imaging of P-gp/BCRP activity with positron emission tomog. (PET). In preclin. studies, the tracer showed excellent initial brain uptake and clean conversion to the desired metabolite, although at a sluggish rate. Blocking with P-gp/BCRP modulators led to increased levels of brain radioactivity; however, dynamic PET did not show differential clearance rates between treatment and control groups. Our results provide proof-of-concept for development of prodrug tracers for imaging of P-gp/BCRP function in vivo but also highlight some challenges associated with this strategy.
Journal of Medicinal Chemistry published new progress about ATP-binding cassette transporter ABCG2 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 128577-47-9 belongs to class bromides-buliding-blocks, and the molecular formula is C9H8BrFO2, SDS of cas: 128577-47-9.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary