Whole-body distribution and metabolism of [N-methyl-11C](R)-1- (2-chlorophenyl)-N-(1-methylpropyl)-3-isoquinolinecarboxamide in humans; An imaging agent for in vivo assessment of peripheral benzodiazepine receptor activity with positron emission tomography

European Journal of Nuclear Medicine and Molecular Imaging

Volumn 36, Issue 4, 2009, Pages 671-682

  Roivainen, Anne ^a   Någren, Kjell ^b   Hirvonen, Jussi ^a   Oikonen, Vesa ^a   Virsu, Pauliina ^a   Tolvanen, Tuula ^a   Rinne, Juha O ^a,c  

^a TURKU UNIVERSITY HOSPITAL   (Finland)

^b UNIVERSITY OF TURKU   (Finland)

^c GE Healthcare Finland Oy   (Finland)

Author keywords

Carbon 11; Human; Metabolism; PK11195; Positron emission tomography; Whole body distribution

Indexed keywords

BENZODIAZEPINE RECEPTOR; N SEC BUTYL 1 (2 CHLOROPHENYL) N METHYL 3 ISOQUINOLINECARBOXAMIDE C 11;

ADULT; AGED; ALZHEIMER DISEASE; ARTICLE; BASAL GANGLION; BLOOD SAMPLING; CEREBELLUM; CLINICAL ARTICLE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG DISTRIBUTION; DRUG METABOLISM; DRUG STRUCTURE; DRUG UPTAKE; FEMALE; GRAY MATTER; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; IN VIVO STUDY; MALE; MEDICAL ASSESSMENT; POSITRON EMISSION TOMOGRAPHY; RADIOACTIVITY; THALAMUS; THIN LAYER CHROMATOGRAPHY;

AGED; AGED, 80 AND OVER; ANTINEOPLASTIC AGENTS; CARBON RADIOISOTOPES; FEMALE; HUMANS; ISOQUINOLINES; MALE; MIDDLE AGED; POSITRON-EMISSION TOMOGRAPHY; RECEPTORS, GABA-A; REPRODUCIBILITY OF RESULTS; TIME FACTORS; TISSUE DISTRIBUTION; WHOLE BODY IMAGING;

EID: 62149146138     PISSN: 16197070     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00259-008-1000-1     Document Type: Article

References (26)

1. V Papadopoulos M Baraldi TR Guilarte TB Knudsen JJ Lacapère P Lindemann 2006 Translocator protein (18 kDa): new nomenclature for the peripheral-type benzodiazepine receptor based on its structure and molecular function Trends Pharmacol Sci 27 402 409
2. P Casellas S Galiegue AS Basile 2002 Peripheral benzodiazepine receptors and mitochondrial function Neurochem Int 40 475 486
3. KE Krueger 1995 Molecular and functional properties of mitochondrial benzodiazepine receptors Biochim Biophys Acta 241 453 470
4. L Skrabanek F Campagne 2001 TissueInfo: high-throughput identification of tissue expression profiles and specificity Nucleic Acids Res 29 E102
5. L Huminiecki AT Lloyd KH Wolfe 2003 Congruence of tissue expression profiles from Gene Expression Atlas, SAGEmap and TissueInfo databases BMC Genomics 4 31
6. L Junck JM Olson BJ Ciliax RA Koeppe GL Watkins DM Jewett 1989 PET imaging of human gliomas with ligands for the peripheral benzodiazepine binding site Ann Neurol 26 752 758
7. E Vowinckel D Reutens B Becher G Verge A Evans T Owens 1997 PK11195 binding to the peripheral benzodiazepine receptor as a marker of microglia activation in multiple sclerosis and experimental autoimmune encephalomyelitis J Neurosci Res 50 345 353
8. RB Banati J Newcombe RN Gunn A Cagnin F Turkheimer F Heppner 2000 The peripheral benzodiazepine binding site in the brain in multiple sclerosis: quantitative in vivo imaging of microglia as a measure of disease activity Brain 123 2321 2337
9. MR Turner A Cagnin FE Turkheimer CC Miller CE Shaw DJ Brooks 2004 Evidence of widespread cerebral microglial activation in amyotrophic lateral sclerosis: an [11C](R)-PK11195 positron emission tomography study Neurobiol Dis 15 601 609
10. Y Ouchi E Yoshikawa Y Sekine M Futatsubashi T Kanno T Ogusu 2005 Microglial activation and dopamine terminal loss in early Parkinson's disease Ann Neurol 57 168 175
11. S Pappata M Levasseur RN Gunn R Myers C Crouzel A Syrota 2000 Thalamic microglial activation in ischemic stroke detected in vivo by PET and [11C]PK1195 Neurology 55 1052 1054
12. MA Kropholler R Boellaard A Schuitemaker BN van Berckel G Luurtsema AD Windhorst 2005 Development of a tracer kinetic plasma input model for (R)-[11C]PK11195 brain studies J Cereb Blood Flow Metab 25 842 851
13. F De Vos F Dumont P Santens G Slegers R Dierckx J De Reuck 1999 High-performance liquid chromatographic determination of [11C]-1-(2- chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinoline carboxamide in mouse plasma and tissue and in human plasma J Chromatogr B Biomed Sci Appl 736 61 66
14. P Charbonneau A Syrota C Crouzel J-M Valois C Prenant M Crouzel 1986 Peripheral-type benzodiazepine receptors in the living heart characterized by positron emission tomography Circulation 73 476 483
15. VW Pike C Halldin C Crouzel L Barré DJ Nutt S Osman 1993 Radioligands for PET studies of central benzodiazepine receptors and PK (peripheral benzodiazepine) binding sites - current status Nucl Med Biol 20 503 525
16. SK Luthra S Osman DR Turton V Vaja K Dowsett F Brady 1993 An automated system based on solid phase extraction and HPLC for the routine determination in plasma of unchanged [11C]-L-deprenyl; [11C]diprenorphine; [11C]flumazenil; [11C]raclopride; and [11C]Scherring 23390 J Labelled Compd Radiopharm 32 518 520
17. JC Debruyne J Versijpt KJ Van Laere F De Vos J Keppens K Strijckmans 2003 PET visualization of microglia in multiple sclerosis patients using [11C]PK11195 Eur J Neurol 10 257 264
18. TR DeGrado TG Turkington JJ Williams CW Stearns JM Hoffman RE Coleman 1994 Performance characteristics of a whole-body PET scanner J Nucl Med 35 1398 1406
19. AJ Montgomery MC Asselin L Farde PM Grasby 2007 Measurement of methylphenidate-induced change in extrastriatal dopamine concentration using [11C]FLB 457 PET J Cereb Blood Flow Metab 27 369 377
20. HNJM Greuter PLB van Ophemert G Luurtsema BN van Berckel EJ Franssen BD Windhorst 2005 Optimizing an online SPE-HPLC method for analysis of (R)-[11C]1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3- isoquinolinecarboxamide [(R)-[11C]PK11195] and its metabolites in humans Nucl Med Biol 32 307 312
21. EP Wala JW Sloan X Jing 2000 Pharmacokinetics of the peripheral benzodiazepine receptor antagonist, PK 11195, in rats. The effect of dose and gender Pharmacol Res 41 461 468
22. A Ferry P Jaillon B Lecocq V Lecocq C Jozefczak 1989 Pharmacokinetics and effects on exercise heart rate of PK 11195 (52028 RP), an antagonist of peripheral benzodiazepine receptors, in healthy volunteers Fundam Clin Pharmacol 3 383 392
23. MC Cleij FJ Airbirhio JC Baron JC Clark 2003 Base-promoted dechlorination of (R)-[11C]PK 11195 J Labelled Compd Radiopharm 46 S88
24. D Diorio SA Weiner RF Butterworth Mi Meaney BE Suranyi-Cadotte 1991 Peripheral benzodiazepine binding sites in Alzheimer's disease frontal and temporal cortex Neurobiol Aging 12 255 258
25. A Cagnin DJ Brooks AM Kennedy RN Gunn R Myers FE Turkheimer 2001 In-vivo measurement of activated microglia in dementia Lancet 358 461 467
26. P Virsu I Laitinen T Pöyhönen K Någren A Roivainen 2005 In vivo biodistribution, biokinetics and blood metabolism of 11C-PK11195 in rats - a PET tracer for peripheral benzodiazepine receptor Eur J Nucl Med Mol Imaging 32 P752