In vivo evaluation in rats of [18F]1-(2-fluoroethyl)-4-[(4- cyanophenoxy)methyl]piperidine as a potential radiotracer for PET assessment of CNS sigma-1 receptors

Nuclear Medicine and Biology

Volumn 33, Issue 2, 2006, Pages 211-215

  Waterhouse, Rikki N ^a,b   Chang, Raymond C ^a,b   Zhao, Jun ^a,b   Carambot, Patty E ^a,b  

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

^b NEW YORK STATE PSYCHIATRIC INSTITUTE   (United States)

Author keywords

Flourine 18; PET; Radiotracer; Sigma 1 receptor

Indexed keywords

1 (FLUOROETHYL) 4 [(4 CYANOPHENOXY)METHYL]PIPERIDINE F 18; DRUG METABOLITE; PIPERIDINE DERIVATIVE; SIGMA 1 OPIATE RECEPTOR; TRACER; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BRAIN REGION; CENTRAL NERVOUS SYSTEM; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; DRUG CLEARANCE; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SCREENING; DRUG SYNTHESIS; ELECTROENCEPHALOGRAM; FRONTAL CORTEX; HIPPOCAMPUS; LIGAND BINDING; MALE; NONHUMAN; OCCIPITAL CORTEX; POSITRON EMISSION TOMOGRAPHY; RAT; RECEPTOR AFFINITY;

ANIMALS; BRAIN; DRUG EVALUATION, PRECLINICAL; FEASIBILITY STUDIES; MALE; METABOLIC CLEARANCE RATE; ORGAN SPECIFICITY; PIPERIDINES; POSITRON-EMISSION TOMOGRAPHY; RADIOPHARMACEUTICALS; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, SIGMA; TISSUE DISTRIBUTION;

EID: 33644949009     PISSN: 09698051     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.nucmedbio.2005.10.007     Document Type: Article

References (38)

1. X. Guitart, X. Codony, and X. Monroy Sigma receptors: biology and therapeutic potential Psychopharmacology 174 2004 301 319
2. T. Maurice, A. Urani, V.L. Phan, and P. Romieu The interaction between neuroactive steroids and the sigma1 receptor function: behavioral consequences and therapeutic opportunities Brain Res Brain Res Rev 37 2001 116 132
3. T. Maurice, R. Martin-Fardon, P. Romieu, and R.R. Matsumoto Sigma(1) (sigma(1)) receptor antagonists represent a new strategy against cocaine addiction and toxicity Neurosci Biobehav Rev 26 2002 499 527
4. T. Maurice Neurosteroids and sigma1 receptors, biochemical and behavioral relevance Pharmacopsychiatry 37 2004 S171 S182
5. M. Takebayashi, T. Hayashi, and T.P. Su A perspective on the new mechanism of antidepressants: neuritogenesis through sigma-1 receptors Pharmacopsychiatry 37 Suppl 3 2004 S208 S213
6. T.P. Su, and T. Hayashi Understanding the molecular mechanism of sigma-1 receptors: towards a hypothesis that sigma-1 receptors are intracellular amplifiers for signal transduction Curr Med Chem 10 2003 2073 2080
7. S.J. Nuwayhid, and L.L. Werling Sigma1 receptor agonist-mediated regulation of N-methyl-d-aspartate-stimulated [3H]dopamine release is dependent upon protein kinase C J Pharmacol Exp Ther 304 2003 364 369
8. S. Chaki, S. Okuyama, S. Ogawa, and K. Tomisawa Regulation of NMDA-induced [3H]dopamine release from rat hippocampal slices through sigma-1 binding sites Neurochem Int 33 1998 29 34
9. D.T. Ault, and L.L. Werling Neuropeptide Y-mediated enhancement of NMDA-stimulated [3H]dopamine release from rat prefrontal cortex is reversed by sigma1 receptor antagonists Schizophr Res 31 1998 27 36
10. G.A. Gudelsky Effects of sigma receptor ligands on the extracellular concentration of dopamine in the striatum and prefrontal cortex of the rat Eur J Pharmacol 286 1995 223 228
11. G.M. Gonzalez-Alvear, and L.L. Werling sigma1 receptors in rat striatum regulate NMDA-stimulated [3H]dopamine release via a presynaptic mechanism Eur J Pharmacol 294 1995 713 719
12. J.K. Weatherspoon, G.M. Gonzalez-Alvear, and L.L. Werling Regulation of [3H]norepinephrine release from guinea pig hippocampus by sigma2 receptors Eur J Pharmacol 326 1997 133 138
13. G.M. Gonzalez-Alvear, and L.L. Werling Sigma receptor regulation of norepinephrine release from rat hippocampal slices Brain Res 673 1995 61 69
14. M. Nakagawara, and Y. Sato Neuropeptide Y: psychopharmacological and clinical aspects Yakubutsu Seishin Kodo 14 1994 117 127
15. T. Hayashi, and T. Su Sigma-1 receptor ligands: potential in the treatment of neuropsychiatric disorders CNS Drugs 18 2004 269 284
16. W. Bowen Sigma receptors: recent advances and new clinical potentials Pharm Acta Helv 74 2000 211 218
17. T.L. Collier, R. Lecomte, T.J. McCarthy, S. Meikle, T.J. Ruth, and F. Scopinaro Assessment of cancer-associated biomarkers by positron emission tomography: advances and challenges Dis Markers 18 2002 211 247
18. C.S. John, W.D. Bowen, T. Saga, S. Kinuya, B.J. Vilner, and J. Baumgold A malignant melanoma imaging agent: synthesis, characterization, in vitro binding and biodistribution of iodine-125-(2-piperidinylaminoethyl)4-iodobenzamide J Nucl Med 34 1993 2169 2175
19. J.M. Musacchio The psychotomimetic effects of opiates and the sigma receptor Neuropsychopharmacology 3 1990 191 200
20. G. Skuza, and K. Wedzony Behavioral pharmacology of sigma-ligands Pharmacopsychiatry 37 2004 S183 S188
21. G. Debonnel Current hypotheses on sigma receptors and their physiological role: possible implications in psychiatry J Psychiatr Neurosci 18 1993 157 172
22. B. Wang, R. Rouzier, C.T. Albarracin, A. Sahin, P. Wagner, and Y. Yang Expression of sigma 1 receptor in human breast cancer Breast Cancer Res Treat 87 2004 205 214
23. Y.-W. Ding, F.S. Fowler, S.L. Dewey, A.P. Wolf, J. Logan, and S.J. Gatley Synthesis and PET studies of fluorine-18-BMY 14802: a potential antipsychotic drug J Nucl Med 34 1993 246 254
24. Y.W. Jung, K.A. Frey, G.K. Mulholland, R. del Rosario, P.S. Sherman, and D.M. Raffel Vesamicol receptor mapping of brain cholinergic neurons with radioiodine-labeled positional isomers of benzovesamicol J Med Chem 39 1996 3331 3342
25. A.S. Kimes, A.A. Wilson, U. Scheffel, B.G. Campbell, and E.D. London Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3- (1-adamantyl)guanidine, a ligand for sigma binding sites J Med Chem 35 1992 4683 4689
26. D.J. Schlyer, N.D. Volkow, J.S. Fowler, A.P. Wolf, C.-Y. Shiue, and S.L. Dewey Regional distribution and kinetics of haloperidol binding in human brain: a pet study with [18F]haloperidol Synapse 11 1992 10 19
27. J. Musachio, U. Scheffel, M. Stathis, H. Ravert, W. Mathews, and R. Dannals (+)-[C-11]-cis-N-benzyl-normetazocine: a selective ligand for sigma receptors in vivo Life Sci 55 1994 225
28. S.M. Ametamey, S. Samnick, K.L. Leenders, P. Vontobel, G. Quack, and C.G. Parsons Fluorine-18 radiolabelling, biodistribution studies and preliminary PET evaluation of a new memantine derivative for imaging the NMDA receptor J Recep Signal Transduct Res 19 1999 129 141
29. K. Ishiwata, and M. Senda In vivo binding of [11C]nemonapride to sigma receptors in the cortex and cerebellum Nucl Med Biol 26 1999 627 631
30. K. Ishiwata, J. Noguchi, S. Ishii, K. Hatano, K. Ito, and T. Nabeshima Synthesis and preliminary evaluation of [11C]NE-100 labeled in two different positions as a PET sigma receptor ligand Nucl Med Biol 25 1998 195 202
31. P. Elsinga, K. Kawamura, T. Kobayashi, H. Tsukada, M. Senda, and W. Vaalburg Synthesis and evaluation of [18F]fluoroethyl SA4503 as a PET ligand for the sigma receptor Synapse 43 2002 259 267
32. K. Kawamura, K. Ishiwata, H. Tajima, S. Ishii, K. Matsuno, and Y. Homma In vivo evaluation of [(11)C]SA4503 as a PET ligand for mapping CNS sigma(1) receptors Nucl Med Biol 27 2000 255 261
33. R.N. Waterhouse, and T.L. Collier In vivo evaluation of [18F]1-(3-fluoropropyl)-4-(4-cyanophenoxymethyl)piperidine: a selective sigma-1 receptor radioligand for PET Nucl Med Biol 24 1997 127 134
34. R.N. Waterhouse, M.G. Stabin, and J.G. Page Preclinical acute toxicity studies and rodent-based dosimetry estimates of the novel sigma-1 receptor radiotracer [(18)F]FPS Nucl Med Biol 30 2003 555 563
35. R.N. Waterhouse, M. Slifstein, P. Talbot, F. Dumont, A. Sultana, and Y. Sudo Development of [18F]1-(3-fluoropropyl)-4-[(4-cyanomethoxy)methyl]piperidine ([18F]FPS): an effective PET tracer for imaging sigma-1 receptors in the primate CNS Mol Imaging Biol 4 2002 S35 S36
36. J. Zhao, R. Chang, P. Carambot, and R.N. Waterhouse Radiosynthesis and in vivo study of [18F]1-(2-flouroethyl)-4-[(4-cyanophenoxy)methyl]piperidine as a novel sigma-1 receptor ligand J Label Compd Radiopharm 48 2005 547 555
37. A. van Waarde, A.R. Buursma, G.A. Hospers, K. Kawamura, T. Kobayashi, and K. Ishii Tumor imaging with 2 sigma-receptor ligands, 18F-FE-SA5845 and 11C-SA4503: a feasibility study J Nucl Med 45 1939 1939 1945
38. M.L Leitner, A.G. Hohmann, S.L. Patrick, and J.M. Walker Regional variation in the ratio of sigma 1 to sigma 2 binding in rat brain Eur J Pharmacol 259 1994 65 69