Browse > Article

[ ${\beta}-Amyloid$ ] Imaging Probes  

Jeong, Jae-Min (Department of Nuclear Medicine, Seoul National University College of Medicine)
Publication Information
Nuclear Medicine and Molecular Imaging / v.41, no.2, 2007 , pp. 112-117 More about this Journal
Abstract
Imaging distribution of ${\beta}-amyloid$ plaques in Alzheimer's disease is very important for early and accurate diagnosis. Early trial of the ${\beta}-amyloid$ plaques includes using radiolabeled peptides which can be only applied for peripheral ${\beta}-amyloid$ plaques due to limited penetration through the blood brain barrier (BBB). Congo red or Chrysamine G derivatives were labeled with Tc-99m for imaging ${\beta}-amyloid$ plaques of Alzheimer patient's brain without success due to problem with BBB penetration. Thioflavin T derivatives gave breakthrough for ${\beta}-amyloid$ imaging in vivo, and a benzothiazole derivative [C-11]6-OH-BTA-1 brought a great success. Many other benzothiazole, benzoxazole, benzofuran, imidazopyridine, and styrylbenzene derivatives have been labeled with F-18 and I-123 to improve the imaging quality. However, [C-11]6-OH-BTA-1 still remains as the best. However, short half-life of C-11 is a limitation of wide distribution of this agent. So, it is still required to develop an Tc-99m, F-18 or I-123 labeled agent for ${\beta}-amyloid$ imaging agent.
Keywords
${\beta}-amyloid$; alzheimer's; disease; PET;
Citations & Related Records
연도 인용수 순위
  • Reference
1 McKhann G., Drachman D, Folstein M, Katzman R, Price D, Stadlan EM. Clinical diagnosis of Alzheimer's disease: a report of the NINCDS-ADRDA Work Group, Department of Health and Human Services Task Force on Alzheimer's Disease. Neurology 1984;34:939-44   DOI
2 Schaadt BK, Hendel HW, Gimsing P, Jonsson V, Pedersen H, Hesse $^{99m}Tc$-Aprotinin scintigraphy in amylodosis. J Nucl Med 2003;44:177-83
3 Klunk WE, Debnath ML, Pettegrew JW. Chrysamine-G binding to Alzheimer and control brain: Autopsy study of a new amyloid probe. Neurobiol Aging 1995;16:541-8   DOI   ScienceOn
4 Han H, Cho C-G, Lansbury PT Jr. Technetium complexes for the quantitation of brain amyloid. J Am Chem Soc 1996;118:4506-7   DOI   ScienceOn
5 Kung HF, Molnar M, Billings J, Blau M. Synthesis and biodistribution of neutral lipid-soluble Tc-99m complexes that cross the blood-brain barrier. J Nucl Med 1984;25:326-32
6 Dezutter NA, de Groot TJ, Busson RH, Janssen GA, Verbruggen AM. Preparation of Tc-99m-$N2_S_2$ conjugates of chrysamine G, potential probes for the beta-amyloid protein of Alzheimer's disease. J Label Cmpd Radiopharm 1999;42:309-24   DOI   ScienceOn
7 Wischik CM, Harrington CR, Rickard JE, Horsley D. Neurofibrillary labels. 2002 PCT WO 02/075318 A2
8 Mathis CA, Holt DP, Wang Y, Huang GF, Debmath ML, Klunk WE. Lipophilic 11C-labelled thioflavin-T analogues for imaging amyloid plaques in Alzheimer's disease. J Label Compd Radiopharm 2001;44:S26-S8   DOI   ScienceOn
9 Marshall JR, Stimson ER, Ghilardi JR, Vinters HV, Mantyh PW, Maggio JE. Noninvasive imaging of peripherally injected Alzheimer's disease type synthetic ATEX>$\beta$ amyloid in vivo. Bioconjugate Chem 2002;13:276-84   DOI   ScienceOn
10 Ono M, Kung M-P, Hou C, Kung HF. Benzofuran derivatives as A $\beta$-aggregate-specific imaging agents for Alzheimer's disease. Nucl Med Biol 2002;29:633-42   DOI   ScienceOn
11 Oya S, Plössl K, Kung M-P, Stevenson DA, Kung HF. Small and neutral TcVO BAT, bisaminoethanthiol ($N_2S_2$) complexes for developing new brain imaging agents. Nucl Med Biol 1998;25: 135-40   DOI   ScienceOn
12 Weiner MF. Alzheimer's disease: diagnosis and treatment. Harvard Rev. Psychiatry 1997;4:306-16   DOI   ScienceOn
13 Bornebroek M, Verzijlbergen JF, Haan J, Van Scheyen EJ, Verhoeff NPLG, Pauwels EKJ, et al. Potential for imaging cerebral amyloid deposits using $ ^{123}I$-labelled serum amyloid P component and SPET. Nucl Med Commun 1996;17:929-33   DOI   ScienceOn
14 Mathis CA, Wang Y, Holt DP, Huang GF, Debnath ML, Klunk WE. Synthesis and Evaluation of 11C-Labeled 6-Substituted 2- Arylbenzothiazoles as Amyloid Imaging Agents. J Med Chem 2003;46:2740-54   DOI   ScienceOn
15 Jeong JM, Kim YJ, Lee YS, Ko JI, Son M, Lee DS, et al. Lipiodol solution of a lipophilic agent, $^{188]Re$-TDD, for the treatment of liver cancer. Nucl Med Biol 2001;28:197-204   DOI   ScienceOn
16 Zhen W, Han H, Anguiano M, Lemere CA, Cho C-G, Lansbury PT Jr. Synthesis and amyloid binding properties of rhenium complexes: preliminary progress toward a reagent for SPECT imaging of Alzheimer's disease brain. J Med Chem 1999;42:2805-15   DOI   ScienceOn
17 Selkoe DJ. Amyloid $\beta$-protein and the genetics of Alzheimer's disease. J Biol Chem 1996;271:18295-8   DOI
18 Ashburn TT, Han H, McGuinness BF, Lansbury PT. Amyloid probes based on Congo Red distinguish between fibrils comprising different peptides. Chem Biol 1996;3:351-8   DOI   ScienceOn
19 Zhuang Z-P, Kung M-P, Wilson A, Lee C-W, Plössl K, Hou C, et al. Structure-activity relationship of imidazo[1,2-a]pyridines as ligands for detecting $\beta$-amyloid plaques in the brain. J Med Chem 2003;46:237-43   DOI   ScienceOn
20 Saito Y, Buciak J, Yang J, Pardridge WM. Vector-mediated delivery of $^{125}I$-labeled $\beta$-amyloid peptide $A{\beta}_{1-40}$ through the blood-brain barrier and binding to Alzheimer disease amyloid of the $A{\beta}_{1-40}$/vector complex. Proc Natl Acad Sci USA 1995;92:10227-31
21 Zhuang Z-P, Kung M-P, Hou C, Skovronsky D, Gur TL, Trojanowski JQ, et al. Radioiodinated styrylbenzenes and thioflavins as probes for amyloid aggregates. J Med Chem 2001;44:1905-14   DOI   ScienceOn
22 Dezutter NA, Dom RJ, de Groot TJ, Bromans GM, Verbruggen AM. $^{99m}Tc$-MAMA-chrysamine G, a probe for beta-amyloid protein of Alzheimer's disease. Eur J Nucl Med 1999;26:1392-9   DOI
23 Chang YS, Jeong JM, Lee Y-S, Kim HW, Rai BG, Kim YJ, et al. Synthesis and evaluation of benzothiophene derivatives as ligands for imaging $\beta$-amyloid plaques in Alzheimer's disease. Nucl Med Biol 2006;33:811-820   DOI   ScienceOn
24 Mathis CA, Bacskai BJ, Kajdasz ST, McLellan ME, Frosch MP, Hyman BT, et al. A lipophilic thioflavin-T derivative for positron emission tomography (PET) imaging of amyloid in brain. Bioorg Med Chem Lett 2002;12:295-8   DOI   ScienceOn
25 Zhuang Z-P, Kung M-P, Hou C, Plössl K, Skovronsky D, Gur TL, et al. IBOX (2-(4'-dimethylaminophenyl)-6-iodobenzoxazole): a ligand for imaging amyloid plaques in the brain. Nucl Med Biol 2001;28:887-94   DOI   ScienceOn
26 Klunk WE, Mathis CA, Wang Y. Thioflavin derivatives for use in antemortem diagnosis of Alzheimer's disease and vivo imaging and prevention of amyloid deposition. US Patent 2002/0133019 A1
27 Yankner BA. Mechanism of neuronaldegeneration in Alzheimer's disease. Neuron 1996;16:921-32   DOI   ScienceOn
28 Klunk WE, Debnath ML, Pettegrew JW. Development of small molecule probes for the beta-amyloid protein of Alzheimer's disease. Neurobiol Aging 1994;15:691-8   DOI   ScienceOn