2014
Phosphodiesterase 10A PET Radioligand Development Program: From Pig to Human
Plisson C, Weinzimmer D, Jakobsen S, Natesan S, Salinas C, Lin SF, Labaree D, Zheng MQ, Nabulsi N, Marques TR, Kapur S, Kawanishi E, Saijo T, Gunn RN, Carson RE, Rabiner EA. Phosphodiesterase 10A PET Radioligand Development Program: From Pig to Human. Journal Of Nuclear Medicine 2014, 55: 595-601. PMID: 24614221, DOI: 10.2967/jnumed.113.131409.Peer-Reviewed Original ResearchConceptsMP-10Primate brainRadioligand candidatesBaseline PET studyFirst human administrationTissue kineticsNonhuman primate brainRegional binding potentialSelective PDE10A inhibitorDose-dependent mannerOutcome measuresPreclinical studiesBrain regionsFurther evaluationPET studiesPig brainPET tracersPDE10A inhibitorsBrainVivo studiesReference tissueHuman administrationHuman brainAdministrationGood radiochemical yield
2008
Preclinical Characterization of Selective Phosphodiesterase 10A Inhibitors: A New Therapeutic Approach to the Treatment of Schizophrenia
Schmidt C, Chapin D, Cianfrogna J, Corman M, Hajos M, Harms J, Hoffman W, Lebel L, McCarthy S, Nelson F, Proulx-LaFrance C, Majchrzak M, Ramirez A, Schmidt K, Seymour P, Siuciak J, Tingley F, Williams R, Verhoest P, Menniti F. Preclinical Characterization of Selective Phosphodiesterase 10A Inhibitors: A New Therapeutic Approach to the Treatment of Schizophrenia. Journal Of Pharmacology And Experimental Therapeutics 2008, 325: 681-690. PMID: 18287214, DOI: 10.1124/jpet.107.132910.Peer-Reviewed Original ResearchConceptsTreatment of schizophreniaPharmacological toolsPDE10A inhibitorsCyclic nucleotide phosphodiesterase 10ABasal ganglia functionNew pharmacological approachesMedium spiny neuronsNew therapeutic approachesNew pharmacological toolsInhibition of PDE10AImportant new targetSelective phosphodiesterase 10A inhibitorsCorticostriatothalamic circuitGanglia functionSpiny neuronsSystemic administrationTherapeutic approachesPharmacological approachesTherapeutic utilityPreclinical characterizationMammalian striatumPhosphodiesterase 10A inhibitorsPhosphodiesterase 10ARelated disordersPoor potency
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