Determination of receptor occupancy in the presence of mass dose: [11C]GSK189254 PET imaging of histamine H3 receptor occupancy by PF-03654746
Gallezot JD, Planeta B, Nabulsi N, Palumbo D, Li X, Liu J, Rowinski C, Chidsey K, Labaree D, Ropchan J, Lin SF, Sawant-Basak A, McCarthy TJ, Schmidt AW, Huang Y, Carson RE. Determination of receptor occupancy in the presence of mass dose: [11C]GSK189254 PET imaging of histamine H3 receptor occupancy by PF-03654746. Cerebrovascular And Brain Metabolism Reviews 2016, 37: 1095-1107. PMID: 27207170, PMCID: PMC5363483, DOI: 10.1177/0271678x16650697.Peer-Reviewed Original ResearchQuantitative projection of human brain penetration of the H3 antagonist PF-03654746 by integrating rat-derived brain partitioning and PET receptor occupancy
Sawant-Basak A, Chen L, Shaffer CL, Palumbo D, Schmidt A, Tseng E, Spracklin DK, Gallezot JD, Labaree D, Nabulsi N, Huang Y, Carson RE, McCarthy T. Quantitative projection of human brain penetration of the H3 antagonist PF-03654746 by integrating rat-derived brain partitioning and PET receptor occupancy. Xenobiotica 2016, 47: 119-126. PMID: 27353353, DOI: 10.3109/00498254.2016.1166531.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBiological TransportBlood-Brain BarrierBrainCyclobutanesHistamine H3 AntagonistsHumansPyrrolidinesRats