Positron emission tomography imaging of the 18-kDa translocator protein (TSPO) with [18F]FEMPA in Alzheimer’s disease patients and control subjects

European Journal of Nuclear Medicine and Molecular Imaging

Volumn 42, Issue 3, 2015, Pages 438-446

  Varrone, Andrea ^a,c   Oikonen, Vesa ^b   Forsberg, Anton ^a   Joutsa, Juho ^b   Takano, Akihiro ^a   Solin, Olof ^b   Haaparanta Solin, Merja ^b   Nag, Sangram ^a   Nakao, Ryuji ^a   Al Tawil, Nabil ^c   Wells, Lisa A ^d   Rabiner, Eugenii A ^d   Valencia, Ray ^e   Schultze Mosgau, Marcus ^e   Thiele, Andrea ^e   Vollmer, Sonja ^e   Dyrks, Thomas ^e   Lehmann, Lutz ^e   Heinrich, Tobias ^e   Hoffmann, Anja ^e   Nordberg, Agneta ^c   Halldin, Christer ^a   Rinne, Juha O ^b   more..

^a KAROLINSKA INSTITUTE   (Sweden)

^b UNIVERSITY OF TURKU   (Finland)

^c KAROLINSKA UNIVERSITY HOSPITAL   (Sweden)

^d Imanova Ltd   (United Kingdom)

^e BAYER PHARMA AG   (Germany)

Author keywords

Alzheimer; Dementia; Microglia; Neuroinflammation; Translocator protein

Indexed keywords

18 KDA TRANSLOCATOR PROTEIN; CARRIER PROTEIN; N [2 (2 FLUOROETHOXYL) 5 METHOXYBENZYL] N [2 (4 METHOXYPHENOXY)PYRIDINE 3 YL]ACETAMIDE F 18; RADIOLIGAND; UNCLASSIFIED DRUG; (18F)FEMPA; 4 AMINOBUTYRIC ACID RECEPTOR; FLUORINATED HYDROCARBON; PROTEIN BINDING; PYRIDINE DERIVATIVE; RADIOPHARMACEUTICAL AGENT; TSPO PROTEIN, HUMAN;

ADULT; AGED; ALZHEIMER DISEASE; ANALYSIS OF VARIANCE; ARTICLE; BINDING AFFINITY; BRAIN CORTEX; BRAIN REGION; CAUDATE NUCLEUS; CEREBELLUM; CLINICAL ARTICLE; COMPARTMENT MODEL; COMPETITIVE BINDING ASSAY; CONTROLLED STUDY; DRUG PROTEIN BINDING; FEMALE; HUMAN; IMAGE ANALYSIS; IN VITRO STUDY; KINETICS; MALE; MIDDLE AGED; MINI MENTAL STATE EXAMINATION; NUCLEAR MAGNETIC RESONANCE IMAGING; POSITRON EMISSION TOMOGRAPHY; POSTERIOR CINGULATE; PUTAMEN; RADIOACTIVITY; SUBCORTEX; TEMPORAL CORTEX; THALAMUS; CONTROLLED CLINICAL TRIAL; DIAGNOSTIC USE; METABOLISM; SCINTISCANNING;

AGED; ALZHEIMER DISEASE; FEMALE; HUMANS; HYDROCARBONS, FLUORINATED; MALE; MIDDLE AGED; POSITRON-EMISSION TOMOGRAPHY; PROTEIN BINDING; PYRIDINES; RADIOPHARMACEUTICALS; RECEPTORS, GABA;

EID: 84925496554     PISSN: 16197070     EISSN: 16197089     Source Type: Journal    
DOI: 10.1007/s00259-014-2955-8     Document Type: Article

References (23)

1. Wyss-Coray T, Rogers J. Inflammation in Alzheimer disease – a brief review of the basic science and clinical literature. Cold Spring Harb Perspect Med. 2012;2:a006346.
2. Rupprecht R, Papadopoulos V, Rammes G, Baghai TC, Fan J, Akula N, et al. Translocator protein (18 kDa) (TSPO) as a therapeutic target for neurological and psychiatric disorders. Nat Rev Drug Discov. 2010;9:971–88.
3. Scarf AM, Kassiou M. The translocator protein. J Nucl Med. 2011;52:677–80.
4. Bird JL, Izquierdo-Garcia D, Davies JR, Rudd JH, Probst KC, Figg N, et al. Evaluation of translocator protein quantification as a tool for characterising macrophage burden in human carotid atherosclerosis. Atherosclerosis. 2010;210:388–91.
5. Cosenza-Nashat M, Zhao ML, Suh HS, Morgan J, Natividad R, Morgello S, et al. Expression of the translocator protein of 18 kDa by microglia, macrophages and astrocytes based on immunohistochemical localization in abnormal human brain. Neuropathol Appl Neurobiol. 2009;35:306–28.
6. Kuhlmann AC, Guilarte TR. Cellular and subcellular localization of peripheral benzodiazepine receptors after trimethyltin neurotoxicity. J Neurochem. 2000;74:1694–704.
7. Venneti S, Lopresti BJ, Wiley CA. Molecular imaging of microglia/macrophages in the brain. Glia. 2013;61:10–23.
8. Cagnin A, Brooks DJ, Kennedy AM, Gunn RN, Myers R, Turkheimer FE, et al. In-vivo measurement of activated microglia in dementia. Lancet. 2001;358:461–7.
9. Edison P, Archer HA, Gerhard A, Hinz R, Pavese N, Turkheimer FE, et al. Microglia, amyloid, and cognition in Alzheimer’s disease: an [11C](R)PK11195-PET and [11C]PIB-PET study. Neurobiol Dis. 2008;32:412–9.
10. Wiley CA, Lopresti BJ, Venneti S, Price J, Klunk WE, DeKosky ST, et al. Carbon 11-labeled Pittsburgh compound B and carbon 11-labeled (R)-PK11195 positron emission tomographic imaging in Alzheimer disease. Arch Neurol. 2009;66:60–7.
11. Schuitemaker A, Kropholler MA, Boellaard R, van der Flier WM, Kloet RW, van der Doef TF, et al. Microglial activation in Alzheimer’s disease: an (R)-[11C]PK11195 positron emission tomography study. Neurobiol Aging. 2013;34:128–36.
12. Dolle F, Luus C, Reynolds A, Kassiou M. Radiolabelled molecules for imaging the translocator protein (18 kDa) using positron emission tomography. Curr Med Chem. 2009;16:2899–923.
13. Yasuno F, Ota M, Kosaka J, Ito H, Higuchi M, Doronbekov TK, et al. Increased binding of peripheral benzodiazepine receptor in Alzheimer’s disease measured by positron emission tomography with [11C]DAA1106. Biol Psychiatry. 2008;64:835–41.
14. Yasuno F, Kosaka J, Ota M, Higuchi M, Ito H, Fujimura Y, et al. Increased binding of peripheral benzodiazepine receptor in mild cognitive impairment-dementia converters measured by positron emission tomography with [11C]DAA1106. Psychiatry Res. 2012;203:67–74.
15. Varrone A, Mattsson P, Forsberg A, Takano A, Nag S, Gulyas B, et al. In vivo imaging of the 18-kDa translocator protein (TSPO) with [18F]FEDAA1106 and PET does not show increased binding in Alzheimer’s disease patients. Eur J Nucl Med Mol Imaging. 2013;40:921–31.
16. Owen DR, Howell OW, Tang SP, Wells LA, Bennacef I, Bergstrom M, et al. Two binding sites for [3H]PBR28 in human brain: implications for TSPO PET imaging of neuroinflammation. J Cereb Blood Flow Metab. 2010;30:1608–18.
17. Owen DR, Gunn RN, Rabiner EA, Bennacef I, Fujita M, Kreisl WC, et al. Mixed-affinity binding in humans with 18-kDa translocator protein ligands. J Nucl Med. 2011;52:24–32.
18. Owen DR, Yeo AJ, Gunn RN, Song K, Wadsworth G, Lewis A, et al. An 18-kDa translocator protein (TSPO) polymorphism explains differences in binding affinity of the PET radioligand PBR28. J Cereb Blood Flow Metab. 2012;32:1–5.
19. Kreisl WC, Lyoo CH, McGwier M, Snow J, Jenko KJ, Kimura N, et al. In vivo radioligand binding to translocator protein correlates with severity of Alzheimer’s disease. Brain. 2013;136:2228–38.
20. McKhann GM, Knopman DS, Chertkow H, Hyman BT, Jack CR Jr, Kawas CH, et al. The diagnosis of dementia due to Alzheimer's disease: recommendations from the National Institute on Aging-Alzheimer’s Association workgroups on diagnostic guidelines for Alzheimer’s disease. Alzheimers Dement. 2011;7:263–9.
21. Wahlund LO, Barkhof F, Fazekas F, Bronge L, Augustin M, Sjogren M, et al. A new rating scale for age-related white matter changes applicable to MRI and CT. Stroke. 2001;32:1318–22.
22. Kreisl WC, Jenko KJ, Hines CS, Lyoo CH, Corona W, Morse CL, et al. A genetic polymorphism for translocator protein 18 kDa affects both in vitro and in vivo radioligand binding in human brain to this putative biomarker of neuroinflammation. J Cereb Blood Flow Metab. 2013;33:53–8.
23. Owen DR, Guo Q, Kalk NJ, Colasanti A, Kalogiannopoulou D, Dimber R, et al. Determination of [11C]PBR28 binding potential in vivo: a first human TSPO blocking study. J Cereb Blood Flow Metab. 2014;34:989–94.