Dopamine D3 receptor antagonists: The quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 17, 2009, Pages 5056-5059

  Bennacef, Idriss ^a   Salinas, Cristian A ^a   Bonasera, Thomas A ^a   Gunn, Roger N ^a   Audrain, Hélène ^b   Jakobsen, Steen ^b   Nabulsi, Nabeel ^c   Weinzimmer, David ^c   Carson, Richard E ^c   Huang, Yiyun ^c   Holmes, Ian ^d   Micheli, Fabrizio ^e   Heidbreder, Christian ^g   Gentile, Gabriella ^e   Rossi, Tino ^e   Laruelle, Marc ^a,f  

^a HAMMERSMITH HOSPITAL   (United Kingdom)

^b AARHUS UNIVERSITY HOSPITAL   (Denmark)

^c YALE UNIVERSITY SCHOOL OF MEDICINE   (United States)

^d Cancer Therapeutics   (Australia)

^e GSK   (Italy)

^f IMPERIAL COLLEGE LONDON   (United Kingdom)

^g Altria Client Services   (United States)

Author keywords

Antagonist; Dopamine D3; Ligand; PET

Indexed keywords

CARBON 11; CYANIDE; DOPAMINE 3 RECEPTOR; DOPAMINE 3 RECEPTOR BLOCKING AGENT; N [4 [2 (6 CYANO 1,2,3,4 TETRAHYDRO 2 ISOQUINOLINYL)ETHYL]CYCLOHEXYL] 4 QUINOLINECARBOXAMIDE; PALLADIUM; CARBON; DIAGNOSTIC AGENT; IMIDAZOLIDINE DERIVATIVE; LIGAND; PIPERIDINE DERIVATIVE; RADIOPHARMACEUTICAL AGENT;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BLOOD BRAIN BARRIER; CATALYSIS; CAUDATE NUCLEUS; CONTROLLED STUDY; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; GLOBUS PALLIDUS; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; IN VITRO STUDY; IN VIVO STUDY; LIGAND BINDING; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; PRIMATE; PUTAMEN; RADIOSYNTHESIS; RAT; SWINE; THALAMUS; ANIMAL; CHEMISTRY; DRUG ANTAGONISM; HAPLORHINI; HUMAN; METABOLISM; SYNTHESIS;

PRIMATES; SUS;

ANIMALS; CARBON RADIOISOTOPES; HAPLORHINI; HUMANS; IMIDAZOLIDINES; LIGANDS; PIPERIDINES; POSITRON-EMISSION TOMOGRAPHY; RADIOPHARMACEUTICALS; RATS; RECEPTORS, DOPAMINE D3; SWINE;

EID: 68349127060     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.07.055     Document Type: Article

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14. Data not shown.
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20. 11C] GSK981352 are shown in yellow, with progressively lower concentrations displayed in orange and red, respectively. PET images are displayed on a common scale.
21. 11C]1 in the plasma was determined by ultrafiltration.
22. ND is attributed to normal variation in a dataset with little specific binding signal.