Blocking of efflux transporters in rats improves translational validation of brain radioligands
Shalgunov V, Xiong M, L’Estrade E, Raval NR, Andersen IV, Edgar FG, Speth NR, Baerentzen SL, Hansen HD, Donovan LL, Nasser A, Peitersen ST, Kjaer A, Knudsen GM, Syvänen S, Palner M, Herth MM. Blocking of efflux transporters in rats improves translational validation of brain radioligands. EJNMMI Research 2020, 10: 124. PMID: 33074370, PMCID: PMC7572968, DOI: 10.1186/s13550-020-00718-x.Peer-Reviewed Original ResearchP-gp inhibitionBrain uptakePET tracersEfflux transportersDopamine D2/3 receptorsRat dataBackgroundPositron emission tomographyLow brain uptakeInitial preclinical evaluationD2/3 receptorsRat brainPreclinical evaluationMolecular imaging techniquesP-gpVivo pharmacologyEmission tomographyP-glycoproteinTranslational validationRodent dataPET radiotracersHigh expressionRatsDisease modelsTarget-specific bindingReceptors