Quantitative preclinical imaging of TSPO expression in glioma using N,N-diethyl-2-(2-(4-(2- 18F-fluoroethoxy) phenyl)-5,7- dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide

Journal of Nuclear Medicine

Volumn 53, Issue 2, 2012, Pages 287-294

  Tang, Dewei ^a,b   Hight, Matthew R ^a,c   McKinley, Eliot T ^a,c   Fu, Allie ^a   Buck, Jason R ^a,d   Smith, R Adam ^a,d   Tantawy, Mohammed Noor ^a,d   Peterson, Todd E ^a,b,d,e   Colvin, Daniel C ^a,d   Ansari, M Sib ^a,d   Nickels, Michael ^a,d   Manning, H Charles ^a,b,c,d,f  

^a VANDERBILT UNIVERSITY   (United States)

^b VANDERBILT UNIVERSITY SCHOOL OF MEDICINE   (United States)

^c VANDERBILT UNIVERSITY   (United States)

^d VANDERBILT UNIVERSITY MEDICAL CENTER   (United States)

^e VANDERBILT UNIVERSITY   (United States)

^f VANDERBILT INGRAM CANCER CENTER   (United States)

Author keywords

DPA 714; Glioma; Positron emission tomography; Pyrazolopyrimidine; TSPO

Indexed keywords

ACETAMIDE DERIVATIVE; CARRIER PROTEIN; DPA 714; N FLUOROACETYL N (2,5 DIMETHOXYBENZYL) 2 PHENOXYANILINE F 18; N SEC BUTYL 1 (2 CHLOROPHENYL) N METHYL 3 ISOQUINOLINECARBOXAMIDE; N SEC BUTYL 1 (2 CHLOROPHENYL) N METHYL 3 ISOQUINOLINECARBOXAMIDE H 3; N,N DIETHYL 2 (2 (4 (2 FLUOROETHOXY)PHENYL) 5,7 DIMETHYLPYRAZOLO[1,5 A]PYRIMIDINE 3 YL)ACETAMIDE; N,N DIETHYL 2 (2 (4 (2 FLUOROETHOXY)PHENYL) 5,7 DIMETHYLPYRAZOLO[1,5 A]PYRIMIDINE 3 YL)ACETAMIDE F 18; PYRAZOLOPYRIMIDINE DERIVATIVE; TRACER; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BRAIN TISSUE; CELL SPECIFICITY; CONTROLLED STUDY; DRUG ACCUMULATION; DRUG BINDING; DRUG STRUCTURE; DRUG TUMOR LEVEL; EX VIVO STUDY; FEASIBILITY STUDY; GLIOMA; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; IMAGE PROCESSING; IMAGING SYSTEM; IMMUNOHISTOCHEMISTRY; IN VITRO STUDY; ISOTOPE ANALYSIS; ISOTOPE TRACING; LIGAND BINDING; MALE; MOLECULAR IMAGING; MOLECULAR PROBE; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; PROTEIN EXPRESSION; QUANTITATIVE ANALYSIS; RAT; WESTERN BLOTTING;

ACETANILIDES; ANIMALS; BIOLOGICAL TRANSPORT; BRAIN NEOPLASMS; CARRIER PROTEINS; CELL LINE, TUMOR; FEASIBILITY STUDIES; FLUORINE RADIOISOTOPES; GENE EXPRESSION REGULATION, NEOPLASTIC; GLIOMA; MALE; POSITRON-EMISSION TOMOGRAPHY; PYRAZOLES; PYRIMIDINES; RATS; RECEPTORS, GABA-A;

EID: 84863022896     PISSN: 01615505     EISSN: None     Source Type: Journal    
DOI: 10.2967/jnumed.111.095653     Document Type: Article

References (33)

1. Dhermain FG, Hau P, Lanfermann H, Jacobs AH, van den Bent MJ. Advanced MRI and PET imaging for assessment of treatment response in patients with gliomas. Lancet Neurol. 2010;9:906-920.
2. van den Bent MJ, Vogelbaum MA, Wen PY, Macdonald DR, Chang SM. End point assessment in gliomas: novel treatments limit usefulness of classical Macdonald's Criteria. J Clin Oncol. 2009;27:2905-2908.
3. Papadopoulos V, Baraldi M, Guilarte TR, et al. Translocator protein (18kDa): new nomenclature for the peripheral-type benzodiazepine receptor based on its structure and molecular function. Trends Pharmacol Sci. 2006;27:402-409. (Pubitemid 44069585)
4. Papadopoulos V, Lecanu L. Translocator protein (18 kDa) TSPO: an emerging therapeutic target in neurotrauma. Exp Neurol. 2009;219:53-57.
5. Diorio D, Welner SA, Butterworth RF, Meaney MJ, Suranyi-Cadotte BE. Peripheral benzodiazepine binding sites in Alzheimer's disease frontal and temporal cortex. Neurobiol Aging. 1991;12:255-258.
6. Messmer K, Reynolds GP. Increased peripheral benzodiazepine binding sites in the brain of patients with Huntington's disease. Neurosci Lett. 1998;241:53-56. (Pubitemid 28079032)
7. Hardwick M, Fertikh D, Culty M, Li H, Vidic B, Papadopoulos V. Peripheral-type benzodiazepine receptor (PBR) in human breast cancer: correlation of breast cancer cell aggressive phenotype with PBR expression, nuclear localization, and PBR-mediated cell proliferation and nuclear transport of cholesterol. Cancer Res. 1999;59:831-842. (Pubitemid 29086736)
8. Carmel I, Fares FA, Leschiner S, Scherubl H, Weisinger G, Gavish M. Peripheral- type benzodiazepine receptors in the regulation of proliferation of MCF-7 human breast carcinoma cell line. Biochem Pharmacol. 1999;58:273-278. (Pubitemid 29255945)
9. Fafalios A, Akhavan A, Parwani AV, Bies RR, McHugh KJ, Pflug BR. Translocator protein blockade reduces prostate tumor growth. Clin Cancer Res. 2009;15:6177-6184.
10. Nagler R, Ben-Izhak O, Savulescu D, et al. Oral cancer, cigarette smoke and mitochondrial 18kDa translocator protein (TSPO): in vitro, in vivo, salivary analysis. Biochim Biophys Acta. 2010;1802:454-461.
11. Maaser K, Grabowski P, Sutter AP, et al. Overexpression of the peripheral benzodiazepine receptor is a relevant prognostic factor in stage III colorectal cancer. Clin Cancer Res. 2002;8:3205-3209. (Pubitemid 35155032)
12. Deane NG, Manning HC, Foutch AC, et al. Targeted imaging of colonic tumors in smad3-/- mice discriminates cancer and inflammation. Mol Cancer Res. 2007;5:341-349. (Pubitemid 46706996)
13. Maaser K, Hopfner M, Jansen A, et al. Specific ligands of the peripheral benzodiazepine receptor induce apoptosis and cell cycle arrest in human colorectal cancer cells. Br J Cancer. 2001;85:1771-1780. (Pubitemid 34081526)
14. Venturini I, Zeneroli ML, Corsi L, et al. Up-regulation of peripheral benzodiazepine receptor system in hepatocellular carcinoma. Life Sci. 1998;63:1269-1280. (Pubitemid 29369143)
15. Black KL, Ikezaki K, Toga AW. Imaging of brain tumors using peripheral benzodiazepine receptor ligands. J Neurosurg. 1989;71:113-118. (Pubitemid 19196561)
16. Starosta-Rubinstein S, Ciliax BJ, Penney JB, McKeever P, Young AB. Imaging of a glioma using peripheral benzodiazepine receptor ligands. Proc Natl Acad Sci USA. 1987;84:891-895. (Pubitemid 17033913)
17. Nagler R, Savulescu D, Krayzler E, Leschiner S, Veenman L, Gavish M. Cigarette smoke decreases salivary 18 kDa translocator protein binding affinity: in association with oxidative stress. Curr Med Chem. 2010;17:2539-2546.
18. Galiègue S, Casellas P, Kramar A, Tinel N, Simony-Lafontaine J. Immunohistochemical assessment of the peripheral benzodiazepine receptor in breast cancer and its relationship with survival. Clin Cancer Res. 2004;10:2058-2064. (Pubitemid 38375567)
19. Miettinen H, Kononen J, Haapasalo H, et al. Expression of peripheral-type benzodiazepine receptor and diazepam binding inhibitor in human astrocytomas: relationship to cell proliferation. Cancer Res. 1995;55:2691-2695.
20. Hardwick M, Rone J, Han Z, Haddad B, Papadopoulos V. Peripheral-type benzodiazepine receptor levels correlate with the ability of human breast cancer MDA-MB-231 cell line to grow in SCID mice. Int J Cancer. 2001;94:322-327. (Pubitemid 32906060)
21. Dollé F, Luus C, Reynolds A, Kassiou M. Radiolabelled molecules for imaging the translocator protein (18 kDa) using positron emission tomography. Curr Med Chem. 2009;16:2899-2923.
22. 18F-N-fluoroacetyl- N-(2,5-dimethoxybenzyl)- 2-phenoxyaniline. J Nucl Med. 2011;52:107-114.
23. Tang D, Buck JR, Hight MR, Manning HC. Microwave-assisted organic synthesis of a high-affinity pyrazolo-pyrimidinyl TSPO ligand. Tetrahedron Lett. 2010;51:4595-4598.
24. Kozikowski AP, Kotoula M, Ma D, Boujrad N, Tuckmantel W, Papadopoulos V. Synthesis and biology of a 7-nitro-2,1,3-benzoxadiazol-4-yl derivative of 2-phenylindole- 3-acetamide: a fluorescent probe for the peripheral-type benzodiazepine receptor. J Med Chem. 1997;40:2435-2439. (Pubitemid 27347006)
25. 11C-PK11195 in a rat model of acute neuroinflammation. J Nucl Med. 2009;50:468-476.
26. Cleveland WS, Devlin SJ. Locally weighted regression: an approach to regression- analysis by local fitting. J Am Stat Assoc. 1988;83:596-610.
27. Innis RB, Cunningham VJ, Delforge J, et al. Consensus nomenclature for in vivo imaging of reversibly binding radioligands. J Cereb Blood Flow Metab. 2007; 27:1533-1539. (Pubitemid 47301451)
28. Logan J, Fowler JS, Volkow ND, Wang GJ, Ding YS, Alexoff DL. Distribution volume ratios without blood sampling from graphical analysis of PET data. J Cereb Blood Flow Metab. 1996;16:834-840. (Pubitemid 26292051)
29. 18F]DPA-714 in a rat model of focal cerebral ischemia. J Cereb Blood Flow Metab. 2010;30:230-241.
30. Olson JM, Junck L, Young AB, Penney JB, Mancini WR. Isoquinoline and peripheral-type benzodiazepine binding in gliomas: implications for diagnostic imaging. Cancer Res. 1988;48:5837-5841.
31. Cornu P, Benavides J, Scatton B, Hauw JJ, Philippon J. Increase in omega 3 (peripheral-type benzodiazepine) binding site densities in different types of human brain tumours: a quantitative autoradiography study. Acta Neurochir (Wien). 1992;119:146-152. (Pubitemid 23022785)
32. Junck L, Olson JM, Ciliax BJ, et al. PET imaging of human gliomas with ligands for the peripheral benzodiazepine binding site. Ann Neurol. 1989;26:752-758. (Pubitemid 20011009)
33. Pappata S, Cornu P, Samson Y, et al. PET study of carbon-11-PK 11195 binding to peripheral type benzodiazepine sites in glioblastoma: a case report. J Nucl Med. 1991;32:1608-1610.