Synthesis, in vitro and in vivo evaluation of [11C]MMTP: A potential PET ligand for mGluR1 receptors

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 12, 2010, Pages 3499-3501

  Prabhakaran, Jaya ^a   Majo, Vattoly J ^a   Milak, Matthew S ^a,b   Kassir, Suham A ^b   Palner, Mikael ^a   Savenkova, Lyudmila ^a   Mali, Pratap ^b   Arango, Victoria ^a,b   Mann, J John ^a,b   Parsey, Ramin V ^a,b   Kumar, J S Dileep ^a,b  

^a Och Spine at New York Presbyterian Hospitals   (United States)

^b NEW YORK STATE PSYCHIATRIC INSTITUTE   (United States)

Author keywords

Autoradiography; Biological imaging; Human postmortem; mGluR1 receptors; Positron emission tomography

Indexed keywords

[O METHYL CARBON 11]DIMETHYLAMINO 3(4 METHOXYPHENYL) 3H PYRIDO[3',2':4,5]THIENO[3,2 D]PYRIMIDIN 4 ONE; GLUTAMATE RECEPTOR 1; TRACER; UNCLASSIFIED DRUG;

ARTICLE; AUTOPSY; BLOOD BRAIN BARRIER; CEREBELLUM; CORPUS STRIATUM; DEMETHYLATION; HIPPOCAMPUS; HUMAN; HUMAN TISSUE; IN VITRO STUDY; IN VIVO STUDY; POSITRON EMISSION TOMOGRAPHY; PREFRONTAL CORTEX; PROTEIN EXPRESSION; PROTEIN SYNTHESIS; RADIOCHEMISTRY;

ANIMALS; BLOOD-BRAIN BARRIER; BRAIN CHEMISTRY; CARBON RADIOISOTOPES; CEREBELLUM; HUMANS; ISOTOPE LABELING; LIGANDS; PAPIO; POSITRON-EMISSION TOMOGRAPHY; PYRIMIDINONES; RADIOPHARMACEUTICALS; RECEPTORS, METABOTROPIC GLUTAMATE;

PAPIO;

EID: 77954218836     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.04.146     Document Type: Article

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15. 11C]1 in 10% ethanol-saline was analyzed to confirm the chemical and radiochemical purities.
16. The autoradiograms were quantified using a dilution series (each 1:10) of droplets (5 μL) made from the incubation solution, these were added to a TLC plate and exposed together with the autoradiograms. The pixel intensity of the droplets were fitted by a power equation using counted samples as concentration references. Individual ROI′s were thereby quantified for the total amount of compound using the specific activity.
17. 11C]1 (S.A. of 2.5 ± 0.5 Ci/μmol) was injected as an i.v. bolus and emission data were collected for 120 min in 3-D mode in a Siemens ECAT 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.