An in vitro assay for predicting successful imaging radiotracers

Molecular Imaging and Biology

Volumn 5, Issue 2, 2003, Pages 65-71

  Patel, Shil ^a   Hamill, Terence ^a   Hostetler, Eric ^a   Burns, H Donald ^a   Gibson, Raymond E ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

specific binding; Brain sections; PET tracer; Radioligand binding

Indexed keywords

3 METHYLSPIPERONE; 4 (2' METHOXYPHENYL) 1 [2' [N (2''PYRIDINYL) 4 FLUOROBENZAMIDO]ETHYL] PIPERAZINE; 4 IODO 2,5 DIMETHOXYAMPHETAMINE; BRAIN RECEPTOR; CARBON 11; CITALOPRAM; FLUMAZENIL; FLUORINE 18; IODINE 123; IOMAZENIL; METHYLSCOPOLAMINE; N [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] N (2 PYRIDYL)CYCLOHEXANECARBOXAMIDE; PAROXETINE; RACLOPRIDE; RADIOLIGAND; TRACER; UNCLASSIFIED DRUG;

ANALYTIC METHOD; ANIMAL TISSUE; ARTICLE; BINDING ASSAY; BRAIN; CLINICAL PRACTICE; CLINICAL PROTOCOL; CONTROLLED STUDY; DRUG EFFICACY; DRUG SCREENING; DRUG SPECIFICITY; DRUG TARGETING; FRONTAL CORTEX; IMAGING SYSTEM; IN VITRO STUDY; IN VIVO STUDY; INCUBATION TIME; IODINATION; ISOTOPE LABELING; MONKEY; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; PREDICTION; PRIORITY JOURNAL; PUTAMEN; RADIOASSAY; RAT; RECEPTOR BINDING; RECEPTOR DENSITY; TIME; TISSUE SECTION; TITRIMETRY;

ANIMALS; BRAIN; CEREBRAL CORTEX; FLUMAZENIL; GABA MODULATORS; KINETICS; MACACA; MODELS, ANIMAL; PIPERAZINES; PYRIDINES; RADIOPHARMACEUTICALS; RATS; SEROTONIN ANTAGONISTS; TOMOGRAPHY, EMISSION-COMPUTED;

RODENTIA;

EID: 0038618858     PISSN: 15361632     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1536-1632(03)00041-6     Document Type: Article

References (30)

1. Saleem A. Aboagye E.O. Price P.M. In vivo monitoring of drugs using radiotracer techniques Adv. Drug Deliv. Rev. 41 2000 21-39
2. Ito H. Goto R. Koyama M. et al. A simple method for the quantification of benzodiazepine receptors using iodine-123 iomazenil and single-photon emission tomography Eur. J. Nucl. Med. 23 1996 782-791
3. 11C]N-methylspiperone Nucl. Med. Biol. 26 2002 627-631
4. 1A receptors with PET Nucl. Med. Biol. 27 2000 467-471
5. 11C]nicotine in Rhesus monkeys Nucl. Med. Biol. 26 1999 633-640
6. 18F-MEM): a potential radioligand for mapping the NMDA-receptor complex Nucl. Med. Biol. 25 1998 323-330
7. 18F]fluoronorchloroepibatidine in rodent and human brain Nucl. Med. Biol. 25 1998 449-454
8. Hand K.S. Baird V.S. Van Paesschen W. et al. Central benzodiazepine receptor autoradiography in hippocampal sclerosis Brit. J. Pharmacol. 122 1997 358-364
9. 3H]atipamezole Eur. J. Pharmacol. 224 1992 27-38
10. 3H]raclopride binding to brain tissue from subjects with schizophrenia: methodological aspects Neuropharmacology 36 6 1997 779-786
11. 3H]p-MPPF Synapse 23 1996 344-346
12. 3H]8-OH-DPAT and demonstration of increased binding in the frontal cortex in schizophrenia Neurochem. Int. 30 1997 565-574
13. 18F]SPA-RQ: a novel tracer for substance P receptor quantitation Neuroimage 16 3 2002 S5
14. 11C]WAY-100635 in psychotropic drug development Nucl. Med. Biol. 27 2000 515-521
15. 11C]WAY-100635 Brain Res. 745 1997 96-108
16. 1A receptors in living monkey Nucl. Med. Biol. 28 2001 177-185
17. 1A receptor autoradiography and hypothermic responses in rats bred for differences in 8-OH-DPAT sensitivity Brain Res. 782 1998 1-10
18. Volkow N.D. Ding Y.-S. Fowler J.S. Gatley S. Imaging brain cholinergic activity with positron emission tomography: its role in the evaluation of cholinergic treatments in Alzheimer's dementia Biol. Psychiatry 49 2001 211-220
19. Weinberger D.R. Jones D. Reba R.C. et al. A comparison of FDG PET and IQNB SPECT in normal subjects and in patients with dementia J. Neuropsychiatry Clin. Neurosci. 4 1992 239-248
20. Freedman S.B. Harley E.A. Patel S. Direct measurement of muscarinic agents in the central nervous system of mice using ex vivo binding Eur. J. Pharmacol. 174 1989 253-260
21. + channels Eur. J. Pharmacol. 255 1994 25-32
22. 1) in the living human brain using positron emission tomography J. Clin. Psychiatry 63 suppl 1 2002 18-24
23. Laurelle M. Slifstein M. Huang Y. Positron emission tomography: imaging and quantification of neurotransporter availability Methods 27 2002 287-299
24. 2A/2C serotonin agonist Nuc. Med. Biol. 29 2002 575-583
25. Freedman S.B. Harley E.A. Iversen L.L. Relative affinities of drugs acting at cholinoreceptors in displacing agonist and antagonist radioligands: the NMS/OXO-M ratio as an index of efficacy at cortical muscarinic receptors Br. J. Pharmacol. 93 1988 437-445
26. 3H]flumazenil binding in the human hippocampal formation, frontal cortex and cerebellum detected by high-resolution phosphor-imaging Brain Res. 926 2002 27-32
27. Le Bars D. Lemaire C. Ginovart N. et al High yield radiosynthesis and preliminary in vivo evaluation of p-MPPF, a fluoro analog of WAY100-635 Nucl. Med. Bio. 25 1998 343-350
28. 2 serotonin receptors in cerebral cortex J. Neurosci. 6 1986 2941-2949
29. 125I]RTI-55 J. Pharamacol. Exp. Ther. 270 1994 296-309
30. 11C]Raclopride binding to D2-doapmine receptors in the monkey brain Synpase 25 1997 321-325