The use of PET and knockout mice in the drug discovery process

Drug Discovery Today

Volumn 8, Issue 9, 2003, Pages 404-410

  Eckelman, William C ^a  

^a NATIONAL INSTITUTES OF HEALTH   (United States)

Author keywords

15O H2O; 18F FDG; Drug Discovery; Knockout mice; PET; Pharmaceutical Science; Pharmacology; Receptors; Techniques Methods

Indexed keywords

3 ALLYL 6 CHLORO 2,3,4,5 TETRAHYDRO 7,8 DIHYDROXY 1 PHENYL 1H 3 BENZAZEPINE; 3 METHYLSPIPERONE C 11; 8 CHLORO 2,3,4,5 TETRAHYDRO 3 METHYL 5 PHENYL 1H 3 BENZAZEPIN 7 OL HYDROGEN MALEATE C 11; ADENOVIRUS VECTOR; ALPHA (2,3 DIMETHOXYPHENYL) 1 [2 (4 FLUOROPHENYL)ETHYL] 4 PIPERIDINEMETHANOL; AMPHETAMINE; CARFENTANIL C 11; CLOMIPRAMINE; CLOZAPINE; COCAINE C 11; DOPAMINE; DOPAMINE 2 RECEPTOR; DOPAMINE 2 RECEPTOR STIMULATING AGENT; FLUORODEOXYGLUCOSE F 18; GLUCOSE 6 PHOSPHATASE; IMATINIB; LORAZEPAM; N [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] N (2 PYRIDYL)CYCLOHEXANECARBOXAMIDE C 11; NALMEFENE; NALOXONE; PACLITAXEL; PACLITAXEL F 18; PHYSOSTIGMINE; RACLOPRIDE C 11; REMOXIPRIDE; RISPERIDONE; SDZMAR 327; SEROTONIN 2A RECEPTOR; SETOPERONE F 18; TRACER; U 91356A; UNCLASSIFIED DRUG; UNINDEXED DRUG; WATER O 15;

ALZHEIMER DISEASE; DOPAMINE BRAIN LEVEL; DRUG APPROVAL; DRUG BINDING SITE; DRUG EFFECT; DRUG HALF LIFE; DRUG INDUSTRY; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG RESEARCH; DRUG RETENTION; DRUG UPTAKE; GLYCOGEN STORAGE DISEASE; HUMAN; ISOTOPE LABELING; KNOCKOUT MOUSE; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; PROTEOMICS; QUANTITATIVE ANALYSIS; RECEPTOR DENSITY; REVIEW; VALIDATION PROCESS; VIRAL GENE THERAPY;

ALZHEIMER DISEASE; ANIMALS; BINDING SITES; DRUG DESIGN; DRUG RESISTANCE, MULTIPLE; HUMANS; LIGANDS; MICE; MICE, KNOCKOUT; RADIOACTIVE TRACERS; RADIOPHARMACEUTICALS; TOMOGRAPHY, EMISSION-COMPUTED;

EID: 0037403554     PISSN: 13596446     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1359-6446(03)02678-3     Document Type: Review

References (46)

1. Chatziioannou A., et al. Detector development for μPET II: a 1 μl resolution PET scanner for small animal imaging. Phys. Med. Biol. 46:2001;2899-2910.
2. Eckelman W.C., et al. Theory and practice of imaging saturable sites. Invest. Radiol. 37:2002;101-106.
3. Hunter J.R., et al. How FDA expedites evaluation of drugs for AIDS and other life-threatening illnesses. Wellcome Prog. Pharm. January:1993;CE2-CE12.
4. Wagner J.G. Fundamentals of Clinical Pharmacokinetics. 1981;Drug Intelligence, Hamilton, IL.
5. 15O]water be used to evaluate drugs? J. Clin. Pharmacol. (Suppl), 11S-20S.
6. McCulloch J. Mapping functional alterations in the CNS with [14C]deoxyglucose. Handbook of Psychopharmacology. 15:1982;321-410 Plenum Press.
7. Demetri G.D., et al. Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors. New. Engl. J. Med. 347:2002;472-480.
8. Vera D.R., Eckelman W.C. Receptor 1980 and Receptor 2000: twenty years of progress in receptor- binding radiotracers. Nucl. Med. Biol. 28:2001;475-476.
9. Offord, S.J. et al. (1999) The role of positron emission tomography in the drug development of M100907, a putative antipsychotic with a novel mechanism of action. J. Clin. Pharmacol. (Suppl.), 17S-24S.
10. Breier A., et al. Schizophrenia is associated with elevated amphetamine-induced synaptic dopamine concentrations: evidence from a novel positron emission tomography method. Proc. Natl. Acad. Sci. U. S. A. 94:1997;2569-2574.
11. 18F]FP- TZTP: control and competition studies. J. Cereb. Blood Flow Metab. 18:1998;1130-1142.
12. Lee Z., et al. Mapping PET-measured triamcinolone acetonide (TAA) aerosol distribution into deposition by airway generation. Int. J. Pharm. 199:2000;7-16.
13. Eckelman W.C., et al. Receptor binding radiotracers: a class of potential radiopharmaceuticals. J. Nucl. Med. 20:1979;350-357.
14. Katzenellenbogen J.A., et al. In vitro and in vivo steroid receptor assays in the design of estrogen radiopharmaceuticals. Eckelman W. In Receptor Binding Radiotracers. 1:1982;93-126 CRC Press.
15. Ma Y., et al. Identification of metabolites of fluorine-18-labeled M2 muscarinic receptor agonist, 3-(3-[(3-fluoropropyl)thio]-1,2,5-thiadiazol-4-yl)-1,2,5,6-tetrahydro-1- methylpyridine, produced by human and rat hepatocytes. J. Chromatogr. B Analyt. Technol. Biomed. Life Sci. 766:2002;319-329.
16. Ma Y., et al. Liquid chromatography-tandem mass spectrometry identification of metabolites of two 5-HT1A antagonists, N-[2-[4-(2-methoxylphenyl)piperazino]ethyl]-N-(2-pyridyl) trans- and cis-4-fluorocyclohexanecarboxamide, produced by human and rat hepatocytes. J. Chromatogr. B Biomed. Sci. Appl. 755:2001;47-56.
17. Vera C.R., et al. Kinetic sensitivity of a receptor-binding radiopharmaceutical: technetium-99m galactosyl-neoglycoalbumin. J. Nucl. Med. 30:1989;1519-1530.
18. Slifstein M., Laruelle M. Models and methods for derivation of in vivo neuroreceptor parameters with PET and SPECT reversible radiotracers. Nucl. Med. Biol. 28:2001;595-608.
19. St. George-Hyslop P. Molecular genetics of Alzheimer's Disease. Biol. Psychiatary. 47:2000;183-199.
20. Bacskai B.J., et al. Imaging amyloid-beta deposits in vivo. J. Cereb. Blood Flow Metab. 22:2002;1035-1041.
21. Aubert I., et al. Comparative alterations of nicotinic and muscarinic binding sites in Alzheimer's and Parkinson's diseases. J. Neurochem. 58:1992;529-541.
22. Quirion, R. et al. (1989). Muscarinic receptor subtypes in human neurodegenerative disorders; focus on Alzheimer's disease. In Trends in Pharmacol. Sci. (Suppl.) 80-84.
23. Rodriguez-Puertas R., et al. Autoradiographic distribution of M1, M2, M3 and M4 muscarinic receptor subtypes in alzheimer's disease. Synapse. 26:1997;341-350.
24. 18F-labeled muscarinic agonist with M2 selectivity. J. Med. Chem. 38:1995;5-8.
25. Kiesewetter D.O., et al. In vivo muscarinic binding of 3-(alkylthio)-3-thiadiazolyl tetrahydropyridines. Synapse. 31:1999;29-40.
26. 18F]FP-TZTP, is decreased in M2 knockout mice, but not in M1, M3, or M4 knockout mice. Neuropharmacology (in press).
27. Eckelman W.C. Mechanism of target specific uptake using examples of muscarinic rceptor binding radiotacers. Welch M.J. Handbook of Radiopharmaceuticals: Radiochemistry and Applications. 2003;John Wiley & Sons.
28. Zingone A., et al. Monitoring the correction of glycogen storage disease type 1a in a mouse model using [(18)F]FDG and a dedicated animal scanner. Life Sci. 71:2002;1293-1301.
29. Kiesewetter D.O., et al. Fluoro-, bromo-, and iodopaclitaxel derivatives: synthesis and biological evaluation. Nucl. Med. Biol. 30:2003;11-24.
30. 18F]Paclitaxel. J. Nucl. Med. (in press).
31. Piwnica-Worms, D. and Marmion, M. (1999) Characterization of drug specificity by pharmacokinetic analysis in gene knockout mice. J. Clin. Pharmacol. (Suppl.) 30S-33S.
32. Slapak, C.A. et al. (2001) Reversal of multidrug resistance with LY335979: functional analysis of P-glycoprotein-mediated transport activity and its modulation in vivo. J. Clin. Pharmacol. (Suppl.) 29S-38S.
33. Hendrikse, N.H. et al. (2001) P-glycoprotein at the blood-brain barrier and analysis of drug transport with positron-emission tomography. J. Clin. Pharmacol. (Suppl.) 48S-54S.
34. Eckelman W.C. Accelerating drug discovery and development through in vivo imaging. Nucl. Med. Biol. 8:2002;777-782.
35. Klimas M.T. Positron emission tomography and drug discovery: contributions to the understanding of pharmacokinetics, mechanism of action and disease state characterization. Molecular Imaging and Biology. 4:2002;311-337.
36. Burns H.D., et al. Positron emission tomography neuroreceptor imaging as a tool in drug discovery, research and development. Curr. Opin. Chem. Biol. 3:1999;388-394.
37. Halldin C., et al. PET studies with carbon-11 radioligands in neuropsychopharmacological drug development. Curr. Pharm. Des. 7:2001;1907-1929.
38. Kegeles L.S., et al. NMDA antagonist effects on striatal dopamine release: positron emission tomography studies in humans. Synapse. 43:2002;19-29.
39. Farde L., et al. PET-Determination of robalzotan (NAD-299) induced 5-HT(1A) receptor occupancy in the monkey brain. Neuropsychopharmacology. 22:2000;422-429.
40. Nyberg S., et al. Suggested minimal effective dose of risperidone based on PET-measured D2 and 5-HT2A receptor occupancy in schizophrenic patients. Am. J. Psychiatry. 156:1999;869-875.
41. Farde L., et al. Positron emission tomography studies on D2 and 5-HT2 receptor binding in risperidone-treated schizophrenic patients. J. Clin. Psychopharmacol. 15:1995;19S-23S.
42. Christian B.T., et al. Positron emission tomographic analysis of central dopamine D1 receptor binding in normal subjects treated with the atypical neuroleptic, SDZ MAR 327. Int. J. Mol. Med. 1:1998;243-247.
43. Volkow N.D., et al. Relationship between subjective effects of cocaine and dopamine transporter occupancy. Nature. 386:1997;827-830.
44. Kim S., et al. Longer occupancy of opioid receptors by nalmefene compared to naloxone as measured in vivo by a dual-detector system. J. Nucl. Med. 38:1997;1726-1731.
45. 18F]-setoperone during depressive illness and antidepressant treatment with clomipramine. Biol. Psychiatry. 45:1999;180-186.
46. Farde L., von Bahr C. Distribution of remoxipride to the human brain and central D2-dopamine receptor binding examined in vivo by PET. Acta. Psychiatr. Scand. Suppl. 358:1990;67-71.