PET imaging of brain 5-HT1A receptors in rat in vivo with 18F-FCWAY and improvement by successful inhibition of radioligand defluorination with miconazole

Journal of Nuclear Medicine

Volumn 47, Issue 2, 2006, Pages 345-353

  Tipre, Dnyanesh N ^a,c   Zoghbi, Sami S ^a   Liow, Jeih San ^a   Green, Michael V ^b   Seidel, Jurgen ^c   Ichise, Masanori ^a   Innis, Robert B ^a   Pike, Victor W ^a  

^a NATIONAL INSTITUTE OF MENTAL HEALTH   (United States)

^b Trident Imaging Inc   (United States)

^c NATIONAL INSTITUTES OF HEALTH   (United States)

Author keywords

5 HT1A receptors; 18F FCWAY; Defluorination; Miconazole; PET; Rat

Indexed keywords

4 FLUORO N [2 [4 (2 METHOXYPHENYL) PIPERAZIN 1 YL]ETHYL] N (2 PYRIDYL)CYCLOHEXANECARBOXAMIDE] F 18; AMIDE; CIMETIDINE; DICLOFENAC; FLUORIDE ION; MICONAZOLE NITRATE; RADIOLIGAND; SEROTONIN 1A RECEPTOR; UNCLASSIFIED DRUG; CYCLOHEXANE DERIVATIVE; DIAGNOSTIC AGENT; FLUORINE; MICONAZOLE; N (2 (4 (2 METHOXYPHENYL)PIPERAZINO)) N (2 PYRIDINYL) TRANS 4 FLUOROCYCLOHEXANECARBOXAMIDE; N-(2-(4-(2-METHOXYPHENYL)PIPERAZINO))-N-(2-PYRIDINYL) TRANS-4-FLUOROCYCLOHEXANECARBOXAMIDE; PIPERAZINE DERIVATIVE; RADIOPHARMACEUTICAL AGENT;

ANIMAL EXPERIMENT; ARTICLE; BRAIN REGION; CLINICAL RESEARCH; CONTROLLED STUDY; DEFLUORINATION; ENZYME ACTIVITY; ENZYME INHIBITION; HALF LIFE TIME; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; IN VITRO STUDY; IN VIVO STUDY; LIVER MICROSOME; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; RADIOACTIVITY; RAT; RECEPTOR BINDING; RECEPTOR DENSITY; VENOUS BLOOD; ANIMAL; BRAIN; COMPARATIVE STUDY; DRUG EFFECT; EVALUATION; IMAGE ENHANCEMENT; MALE; METABOLIC CLEARANCE RATE; METABOLISM; METHODOLOGY; SCINTISCANNING; SPRAGUE DAWLEY RAT; TISSUE DISTRIBUTION;

ANIMALS; BRAIN; CYCLOHEXANES; FLUORINE; FLUORINE RADIOISOTOPES; IMAGE ENHANCEMENT; MALE; METABOLIC CLEARANCE RATE; MICONAZOLE; PIPERAZINES; POSITRON-EMISSION TOMOGRAPHY; RADIOPHARMACEUTICALS; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR, SEROTONIN, 5-HT1A; TISSUE DISTRIBUTION;

EID: 33747627634     PISSN: 01615505     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (34)

1. Phelps ME, Mazziotta JC, Schelbert HR. Positron Emission Tomography and Autoradiography, Principles and Applications for the Brain and Heart. New York, NY: Raven Press; 1986.
2. Jones T. The imaging science of positron emission tomography. Eur J Nucl Med. 1996;23:807-813.
3. Jones T. The role of positron emission tomography within the spectrum of medical imaging. Eur J Nucl Med. 1996;23:207-211.
4. Fowler JS, Wolf AP. Working against time: rapid radiotracer synthesis and imaging the human brain. Acc Chem Res. 1997;30:181-188.
5. Halldin C, Gulyas B, Langer O, et al. Brain radioligands: state of the art and new trends. Q J Nucl Med. 2001;45:139-152.
6. Elsinga PH. Radiopharmaceutical chemistry for positron emission tomography. Methods. 2002;27:208-217.
7. Sedvall G. PET scanning as a tool in clinical psychopharmacology. Triangle. 1991;30:11-12.
8. Burns HD, Hamill TG, Eng W, et al. Positron emission tomography neuroreceptor imaging as a tool in drug discovery, research and development. Curr Opin Chem Biol. 1999;3:388-394.
9. Comar D, ed. PET for Drug Development and Evaluation. Boston, MA: Kluwer Academic Publishers; 1995.
10. Farde L. The advantage of using positron emission tomography in drug research. Trends Neurosci. 1996;19:211-214.
11. 1A antagonists. J Med Chem. 1999;42:1576-1586.
12. Drevets WC, Frank E, Price JC, et al. PET imaging of serotonin 1A receptor binding in depression. Biol Psychiatry. 1999;46:1375-1387.
13. 1A receptor binding in patients with temporal lobe epilepsy. Neurology. 2003;60:749-756.
14. 18F]FCWAY [abstract]. Neuroimage. 2000;11(suppl):S45.
15. Kharasch ED, Thummel KE. Identification of cytochrome P450 2E1 as the predominant enzyme catalyzing human liver microsomal defluorination of sevoflurane, isoflurane, and methoxyflurane. Anesthesiology. 1993;79:795-807.
16. Yin H, Anders MW, Jones JP. Metabolism of 1,2-dichloro-1-fluoroethane and 1-fluoro-1,2,2-trichloroethane: electronic factors govern the regioselectivity of cytochrome P450-dependent oxidation. Chem Res Toxicol. 1996;9:50-57.
17. Seidel J, Vaquero JJ, Green MV. Resolution uniformity and sensitivity of the NIH ATLAS small animal PET scanner: comparison to simulated LSO scanners without depth-of-interaction capability. IEEE Trans Nucl Sci. 2003;50:1347-1350.
18. Johnson CA, Seidel J, Vaquero JJ, et al. Exact positioning for OSEM reconstructions on the ATLAS depth-of-interaction small animal scanner [abstract]. Mol Imaging Biol. 2002;4(suppl):S22.
19. Liow JS, Johnson CA, Toyama H, et al. A single slice rebinning/2D exact positioning OSEM reconstruction for the NIH ATLAS small animal PET scanner [abstract]. J Nucl Med. 2003;44(suppl):163P.
20. George P, Watson C. The Rat Brain in Stereotaxic Coordinates. 4th ed. San Diego, CA: Academic Press; 1998.
21. Piel G, Evrard B, Van Hees T, et al. Comparison of the IV pharmacokinetics in sheep of miconazole-cyclodextrin solutions and a micellar solution. Int J Pharm. 1999;180:41-45.
22. Fujimaki Y, Arai N, Inaba T. Identification of cytochromes P450 involved in human liver microsomal metabolism of ecabapide, a prokinetic agent. Xenobiotica. 1999;29:1273-1282.
23. 2- receptor antagonists. Clin Pharmacol Ther. 1999;65:369-376.
24. 2-receptor antagonists involving cytochrome P450 (CYPs) enzymes: from the laboratory to the clinic. Croat Med J. 1999;40:357-367.
25. Zweers-Zeilmaker WM, Horbach GJ, Witkamp RF. Differential inhibitory effects of phenytoin, diclofenac, phenylbutazone and a series of sulfonamides on hepatic cytochrome P4502C activity in vitro, and correlation with some molecular descriptors in the dwarf goat (Caprus hircus aegagrus). Xenobiotica. 1997;27:769-780.
26. Tassaneeyakul W, Birkett DJ, Miners JO. Inhibition of human hepatic cytochrome P4502E1 by azole antifungals, CNS-active drugs and non-steroidal anti-inflammatory agents. Xenobiotica. 1998;28:293-301.
27. Maurice M, Pichard L, Daujat M, et al. Effects of imidazole derivatives on cytochromes P450 from human hepatocytes in primary culture. FASEB J. 1992;6:752-758.
28. Denner K, Vogel R, Schmalix W, et al. Cloning and stable expression of the human mitochondrial cytochrome P45011B1 cDNA in V79 Chinese hamster cells and their application for testing of potential inhibitors. Pharmacogenetics. 1995;5:89-96.
29. Chang TK, Gonzalez FJ, Waxman DJ. Evaluation of triacetyloleandomycin, alpha-naphthoflavone and diethyldithiocarbamate as selective chemical probes for inhibition of human cytochromes P450. Arch Biochem Biophys. 1994;311:437-442.
30. Graybill JR, Craven PC. Antifungal agents used in systemic mycoses: activity and therapeutic use. Drugs. 1983;25:41-62.
31. Heel RC, Brogden RN, Pakes GE, et al. Miconazole: a preliminary review of its therapeutic efficacy in systemic fungal infections. Drugs. 1980;19:7-30.
32. 1A receptor antagonist, WAY-100635. Nucl Med Biol. 2000;27:493-497.
33. 1A receptors in rat brain. Eur J Pharmacol. 1994;271:515-523.
34. Hume SP, Gunn RN, Jones T. Pharmacological constraints associated with positron emission tomographic scanning of small laboratory animals. Eur J Nucl Med. 1998;25:173-176.