Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3, 5-dione: A novel agonist 5-HT1A receptor PET ligand

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 8, 2006, Pages 2101-2104

  Prabhakaran, Jaya ^a   Parsey, Ramin V ^a,b   Majo, Vattoly J ^a   Hsiung, Shu Chi ^b   Milak, Matthew S ^a   Tamir, Hadassah ^a,b   Simpson, Norman R ^a   Van Heertum, Ronald L ^a,b   Mann, J John ^a,b   Dileep Kumar, J S ^a,b  

^a New York State Psychiatric Institute ^*  (United States)

^b NEW YORK STATE PSYCHIATRIC INSTITUTE   (United States)

Author keywords

11C MMT; Agonism; Positron emission tomography; Radiotracer

Indexed keywords

GUANOSINE 5' O (3 THIOTRIPHOSPHATE); O METHYL 2 [4 [4 (3 METHOXYPHENYL)PIPERAZIN 1 YL]BUTYL] 4 METHYL 2H [1,2,4]TRIAZINE 3,5 DIONE C 11; RADIOLIGAND; SEROTONIN 1 AGONIST; SEROTONIN 1A RECEPTOR; TRACER; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; BABOON; BLOOD BRAIN BARRIER; CHEMICAL ANALYSIS; CONTROLLED STUDY; DRUG BINDING; DRUG CLEARANCE; DRUG SYNTHESIS; ISOTOPE LABELING; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; RADIOACTIVITY;

ANIMALS; BRAIN; CHO CELLS; CRICETINAE; DITERPENES; LIGANDS; MAGNETIC RESONANCE IMAGING; PAPIO; POSITRON-EMISSION TOMOGRAPHY; RADIOLIGAND ASSAY; RECEPTOR, SEROTONIN, 5-HT1A; TRIAZINES;

ANIMALIA; PAPIO HAMADRYAS;

EID: 33644796770     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.01.052     Document Type: Article

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17. 11C]5 in 10% ethanol-saline was analyzed to confirm the chemical and radiochemical purities.
18. 11C]5 (S.A. of 1400 ± 300 Ci/mmol) was injected as an iv bolus and emission data were collected for 120 min in 3-D mode in a SiemensECAT EXACT HR+ (CPS/Knoxville, TN). The head was positioned at the center of the field of view as defined by imbedded laser lines. Regions of interest drawn on the animal's MRI scan were transferred to co-registered (AIR) frames of PET data.
19. 11C]5 in the plasma at different time points.