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
2011
P3‐431: Translational receptor occupancy for the 5‐HT4 partial agonist PF‐04995274 in rats, non‐human primates and healthy volunteers
Grimwood S, Drummond E, Zasadny K, Skaddan M, Brodney M, Coffman K, Nicholas T, Duvvuri S, Raunig D, Leurent C, Rowinski C, Park Y, Ogden A, Sawant A, Miller E, Rapp T, Wang Y, Planeta‐Wilson B, Ropchan J, Carson R, Morris E, Ding Y, Katz E. P3‐431: Translational receptor occupancy for the 5‐HT4 partial agonist PF‐04995274 in rats, non‐human primates and healthy volunteers. Alzheimer's & Dementia 2011, 7: s653-s653. DOI: 10.1016/j.jalz.2011.05.1875.Peer-Reviewed Original Research