Sander, Kerstin published the artcileDevelopment of Fluorine-18 Labeled Metabolically Activated Tracers for Imaging of Drug Efflux Transporters with Positron Emission Tomography, Recommanded Product: 3-Hydroxydihydrofuran-2(3H)-one, the publication is Journal of Medicinal Chemistry (2015), 58(15), 6058-6080, database is CAplus and MEDLINE.
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 19444-84-9. 19444-84-9 belongs to tetrahydrofurans, auxiliary class Tetrahydrofuran,Ester,Alcohol, name is 3-Hydroxydihydrofuran-2(3H)-one, and the molecular formula is C4H6O3, Recommanded Product: 3-Hydroxydihydrofuran-2(3H)-one.
Referemce:
https://en.wikipedia.org/wiki/Tetrahydrofuran,
Tetrahydrofuran | (CH2)3CH2O – PubChem