2023
Investigating CNS distribution of PF‐05212377, a P‐glycoprotein substrate, by translation of 5‐HT6 receptor occupancy from non‐human primates to humans
Sawant‐Basak A, Chen L, Lockwood P, Boyden T, Doran A, Mancuso J, Zasadny K, McCarthy T, Morris E, Carson R, Esterlis I, Huang Y, Nabulsi N, Planeta B, Fullerton T. Investigating CNS distribution of PF‐05212377, a P‐glycoprotein substrate, by translation of 5‐HT6 receptor occupancy from non‐human primates to humans. Biopharmaceutics & Drug Disposition 2023, 44: 48-59. PMID: 36825693, DOI: 10.1002/bdd.2351.Peer-Reviewed Original ResearchConceptsNon-human primatesBrain penetrationPositron emission tomographyReceptor occupancyUnbound concentrationsPre-clinical evidenceVivo brain penetrationConcentration-dependent increaseP-glycoprotein substratesPlasma ECsP-gpAlzheimer's diseaseEmission tomographyRat BBBTarget engagementCumulative evidenceDependent increaseTransporter substratesCNS distributionBBBRatsDiseasePrimatesSpecies differencesHumans
2001
Analyses of [18F]altanserin bolus injection PET data. I: Consideration of radiolabeled metabolites in baboons
Price J, Lopresti B, Mason N, Holt D, Huang Y, Mathis C. Analyses of [18F]altanserin bolus injection PET data. I: Consideration of radiolabeled metabolites in baboons. Synapse 2001, 41: 1-10. PMID: 11354008, DOI: 10.1002/syn.1054.Peer-Reviewed Original ResearchConceptsBolus injectionMajor radiometabolitePositron emission tomographySerotonin 2A receptor bindingBlood-brain barrier passageReceptor-rich regionsKetanserin administrationNonspecific radioactivityReceptor blockadeInput function methodEmission tomographyPET studiesPET dataReceptor bindingRadiometabolitesVivo kineticsInjectionBBBTissue componentsHuman brainBaboonsMetabolitesRadioactivityBlockadeAntagonist