Development of [11C]/[3H]THK-5351 – A potential novel carbon-11 tau imaging PET radioligand

Nuclear Medicine and Biology

Volumn 46, Issue , 2017, Pages 50-53

  Stepanov, Vladimir ^a   Svedberg, Marie ^a   Jia, Zhisheng ^a   Krasikova, Raisa ^a   Lemoine, Laetitia ^a   Okamura, Nobujuki ^b   Furumoto, Shozo ^b   Mitsios, Nicholas ^c   Mulder, Jan ^c   Långström, Bengt ^d   Nordberg, Agneta ^a   Halldin, Christer ^a  

^a KAROLINSKA INSTITUTE   (Sweden)

^b TOHOKU UNIVERSITY SCHOOL OF MEDICINE   (Japan)

^c SCIENCE FOR LIFE LABORATORY   (Sweden)

^d UPPSALA UNIVERSITY   (Sweden)

Author keywords

Autoradiography; Carbon 11; Pet; Proteinopathy; Tau imaging; Tritium

Indexed keywords

1 FLUORO 3 [2 [6 (METHYLAMINO)PYRIDIN 3 YL]QUINOLIN 6 YLOXY]PROPAN 2 OL C 11; RADIOLIGAND; TRIFLUOROACETIC ACID; TRITIUM; UNCLASSIFIED DRUG; WATER; AMINOPYRIDINE DERIVATIVE; CARBON; LIGAND; QUINOLINE DERIVATIVE; TAU PROTEIN; THK5351;

ALZHEIMER DISEASE; ARTICLE; AUTORADIOGRAPHY; CONTROLLED STUDY; DRUG PURITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENANTIOMER; HUMAN; HUMAN TISSUE; IN VITRO STUDY; POSITRON EMISSION TOMOGRAPHY; RADIOACTIVITY; BRAIN; CHEMISTRY; DIAGNOSTIC IMAGING; METABOLISM; PROCEDURES; RADIOCHEMISTRY; SYNTHESIS;

AMINOPYRIDINES; BRAIN; CARBON RADIOISOTOPES; HUMANS; LIGANDS; POSITRON-EMISSION TOMOGRAPHY; QUINOLINES; RADIOCHEMISTRY; TAU PROTEINS;

EID: 85006986052     PISSN: 09698051     EISSN: 18729614     Source Type: Journal    
DOI: 10.1016/j.nucmedbio.2016.12.004     Document Type: Article

References (20)

1. [1] Hardy, J., Selkoe, D.J., The amyloid hypothesis of Alzheimer's disease: progress and problems on the road to therapeutics. Science 297 (2002), 353–356.
2. [2] Selkoe, D.J., Hardy, J., The amyloid hypothesis of Alzheimer's disease at 25 years. EMBO Mol Med, 2016, 10.15252/emmm.201606210.
3. [3] Haass, C., Selkoe, D.J., Soluble protein oligomers in neurodegeneration: lessons from the Alzheimer's amyloid beta-peptide. Nat Rev Mol Cell Biol 8 (2007), 101–112.
4. [4] Guillozet, A.L., Weintraub, S., Mash, D.C., Mesulam, M.M., Neurofibrillary tangles, amyloid, and memory in aging and mild cognitive impairment. Arch Neurol, 60, 2003, 729-3.
5. [5] Grundke-Iqbal, I., Iqbal, K., Tung, Y.C., Quinlan, M., Wisniewski, H.M., Binder, L.I., Abnormal phosphorylation of the microtubule-associated protein tau (tau) in Alzheimer cytoskeletal pathology. Proc Natl Acad Sci U S A 83 (1986), 4913–4917.
6. [6] Arriagada, P.V., Growdon, J.H., Hedley-Whyte, E.T., Hyman, B.T., Neurofibrillary tangles but not senile plaques parallel duration and severity of Alzheimer's disease. Neurology 42 (1992), 631–639.
7. [7] Jack, C.R. Jr., Knopman, D.S., Jagust, W.J., Petersen, R.C., Weiner, M.W., Aisen, P.S., et al. Tracking pathophysiological processes in Alzheimer's disease: an updated hypothetical model of dynamic biomarkers. Lancet Neurol 12 (2013), 207–216.
8. [8] Young, A.L., Oxtoby, N.P., Daga, P., Cash, D.M., Fox, N.C., Ourselin, S., et al. A data-driven model of biomarker changes in sporadic Alzheimer's disease. Brain 137 (2014), 2564–2577.
9. [9] Dani, M., Brooks, D.J., Edison, tau Imaging in neurodegenerative diseases. Eur J Nucl Med Mol Imaging 43 (2016), 1139–1150.
10. [10] Shoghi-Jadid, K., Small, G.W., Agdeppa, E.D., Kepe, V., Ercoli, L.M., Siddarth, P., et al. Localization of neurofibrillary tangles and beta-amyloid plaques in the brains of living patients with Alzheimer disease. Am J Geriatr Psychiatry 10 (2002), 24–35.
11. [11] Okamura, N., Harada, R., Furumoto, S., Arai, H., Yanai, K., Kudo, Y., Tau PET imaging in Alzheimer's disease. Curr Neurol Neurosci Rep 14 (2014), 500–507.
12. [12] Hashimoto, H., Kawamura, K., Igarashi, N., Takei, M., Fujishiro, T., Aihara, Y., et al. Radiosynthesis, photoisomerization, biodistribution, and metabolite analysis of 11C-PBB3 as a clinically useful PET probe for imaging of tau pathology. J Nucl Med 55 (2014), 1532–1538.
13. [13] Wooten, D., Guehl, N.J., Verwer, E.E., Shoup, T.M., Yokell, D.L., Zubcevik, N., et al. Pharmacokinetic evaluation of the tau PET radiotracer [18F]T807 ([18F]AV-1451) in human subjects. J Nucl Med, 2016 [pii: jnumed.115.170910].
14. [14] Saint-Aubert, L., Almkvist, O., Chiotis, K., Almeida, R., Wall, A., Nordberg, A., Regional tau deposition measured by [18F]THK5317 positron emission tomography is associated to cognition via glucose metabolism in Alzheimer's disease. Alzheimers Res Ther, 8, 2016, 38.
15. [15] Okamura, N., Furumoto, S., Harada, R., Tago, T., Yoshikawa, T., Fodero-Tavoletti, M., et al. Novel 18F-labeled arylquinoline derivatives for noninvasive imaging of tau pathology in Alzheimer disease. J Nucl Med 54 (2013), 1420–1427.
16. [16] Villemagne, V.L., Fodero-Tavoletti, M.T., Masters, C.L., Rowe, C.C., Tau imaging: early progress and future directions. Lancet Neurol 14 (2015), 114–124.
17. [17] Tago, T., Furumoto, S., Okamura, N., Harada, R., Adachi, H., Ishikawa, Y., et al. Structure–activity relationship of 2-Arylquinolines as PET imaging tracers for tau pathology in Alzheimer disease. J Nucl Med 57 (2016), 608–614.
18. [18] Harada, R., Okamura, N., Furumoto, S., Furukawa, K., Ishiki, A., Tomita, N., et al. 18F-THK5351: a novel PET radiotracer for imaging neurofibrillary pathology in Alzheimer disease. J Nucl Med 57 (2016), 208–214.
19. [19] Harada, R., Okamura, N., Furumoto, S., Furukawa, K., Ishiki, A., Tomita, N., et al. [(18)F]THK-5117 PET for assessing neurofibrillary pathology in Alzheimer's disease. Eur J Nucl Med Mol Imaging 42 (2015), 1052–1061.
20. [20] Andersson, J., Truong, P., Halldin, C., In-target produced [11C]methane: increased specific radioactivity. Appl Radiat Isot 67 (2009), 106–110.