nach oben

Nuclear Medicine and Molecular Imaging

Erschienen in:

16.03.2017 | Review

Recent Progress in the Development of TSPO PET Ligands for Neuroinflammation Imaging in Neurological Diseases

verfasst von: Md. Maqusood Alam, Jihye Lee, Sang-Yoon Lee

Erschienen in: Nuclear Medicine and Molecular Imaging | Ausgabe 4/2017

Einloggen, um Zugang zu erhalten

Abstract

Neuroinflammation is heavily associated with various neurological diseases including Alzheimer’s disease, Parkinson’s disease, multiple sclerosis, and stroke. It is strongly characterized by the activation of microglia which can be visualized using position emission tomography (PET). Traditionally, translocator protein 18 kDa (TSPO) has been the preferred target for imaging the inflammatory progression of the microglial component. TSPO is expressed in the outer mitochondrial membrane and present in very low concentrations in the healthy human brain, but is markedly upregulated in response to brain injury and inflammation. Due to its value as a marker of microglial activation and subsequent utility for evaluating neuroinflammation in CNS disorders, several classes of TSPO radioligands have been developed and evaluated. However, the application of these second-generation TSPO radiotracers has been subject to several limiting factors, including a polymorphism that affects TSPO binding. This review focuses on recent developments in TSPO imaging, as well as current limitations and suggestions for future directions from a medical imaging perspective.

Turkheimer FE, Rizzo G, Bloomfield PS, Howes O, Zanotti-Fregonara P, Bertoldo A, et al. The methodology of TSPO imaging with positron emission tomo-graphy. Biochem Soc Trans. 2015;43:586–92.CrossRefPubMedPubMedCentral

Dolle F, Luus C, Reynolds A, Kassiou M. Radiolabelled molecules for imaging the translocator protein (18KDa) using prsitron emission tomography. Curr Med Chem. 2009;16:2899–923.CrossRefPubMed

Chauveau F, Boutin H, Van Camp N, Dollé F, Tavitian B. Nuclear imaging of neuroinflammation: a comprehensive review of [¹¹C]PK11195 challengers. Eur J Nucl Med Mol Imaging. 2008;35:2304–19.CrossRefPubMed

Ruying F, Qingyu S, Xu P, Luo JJ, Yamei T. Phagocytosis of microglia in the central nervous system diseases. Mol Neurobiol. 2014;49:1422–34.CrossRef

Rupprecht R, Papadopoulos V, Rammes G, et al. Translocator protein (18 kDa) (TSPO) as a therapeutic target for neurological and psychiatric disorders. Nat Rev Drug Discov. 2010;9:971–88.CrossRefPubMed

Chen MK, Guilarte TR. Translocator protein 18kDA (TSPO): molecular sensor of brain injury & repair. Pharmacol Ther. 2008;118:1–17.CrossRefPubMedPubMedCentral

Vezzani A, Aronica E, Mazarati A, Pittman QJ. Epilepsy and brain inflammation. Exp Neurol. 2013;244:11–21.CrossRefPubMed

Scarf AM, Kassiou M. The translocator protein. J Nucl Med. 2011;52:677–80.CrossRefPubMed

Papadopoulos V, Baraldi M, Guilarte TR, Knudsen TB, Lacapere JJ, Lindemann P, et al. Translocator protein (18kDa): new nomenclature for the peripheral-type benzodiazepine receptor based on its structure and molecular function. Trends Pharmacol Sci. 2006;27:402–09.CrossRefPubMed

10.

Casellas P, Galiegue S, Basile AS. Peripheral benzodiazepine receptors and mitochondrial function. Neurochem Int. 2002;40:475–86.CrossRefPubMed

11.

Cherry SR, Gambhir SS. Use of positron emission tomography in animal research. ILAR J. 2001;42:219–32.CrossRefPubMed

12.

Gavish M, Bachman I, Shoukrun R, Katz Y, Veenman L, Weisinger G, et al. Enigma of the peripheral benzodiazepine receptor. Pharmacol Rev. 1999;51:629–50.PubMed

13.

Schweitzer PJ, Fallon BA, Mann JJ, Kumar JS. PET tracers for the peripheral bendiazepine receptor and uses thereof. Drug Discov Today. 2010;15:933–42.CrossRefPubMed

14.

Trapani A, Palazzo C, de Candia M, Lasorsa FM, Trapani G. Targeting of the translocator protein 18 kDa (TSPO): a valuable approach for nuclear and optical imaging of activated microglia. Bioconjug Chem. 2013;24:1415–28.CrossRefPubMed

15.

Luus C, Hanani R, Reynolds A, Kassiou M. The development of PET radioligands for imaging the translocator protein (18 kDa): What have we learned. J Label Compd Radiopharm. 2010;53:501–10.

16.

Junck L, Olson JM, Ciliax BJ, Koeppe RA, Watkins GL, Jewett DM, et al. PET imaging of human gliomas with ligands for the peripheral benzodiazepine binding site. Ann Neurol. 1989;26:752–58.CrossRefPubMed

17.

Farges R, Joseph-Liauzun E, Shire D, Caput D, Le Fur G, Ferrara P. Site-directed mutagenesis of the peripheral benzodiazepine receptor: identification of amino acids implicated in the binding site of Ro5-4864. Mol Pharmacol. 1994;46:1160–67.PubMed

18.

Wang JK, Taniguchi T, Spector S. Properties of [3H]diazepam binding sites on rat blood platelets. Life Sci. 1980;27:1881–88.CrossRefPubMed

19.

Camsonne R, Crouzel C, Comar D, Maziere M, Prenant C, Sastre J, et al. Synthesis of N-(C-11) methyl, N-(methyl-1 propyl), (chloro-2 phenyl)-1 isoquinoleine carboxamide-3 (Pk-11195): a new ligand for peripheral benzodiazepine receptors. J Label Compd Radiopharm. 1984;21:985–91.CrossRef

20.

Cagnin A, Gerhard A, Banati RB. In vivo imaging of neuroinflammation. Eur Neuropsychol Pharmacol. 2002;12:581–86.

21.

Shah F, Hume SP, Pike VW, Ashworth S, McDermott J. Synthesis of the enantiomers of [N methyl-¹¹C]PK11195 and comparison of their behaviours as radioligands for PK binding sites in rats. Nucl Med Biol. 1994;21:573–81.CrossRefPubMed

22.

Rao VL, Butterworth RF. Characterization of binding sites for the Ѡ₃ receptor ligands [³H]PK11195 and [³]H Ro5-4864 in human brain. Eur J Pharmacol. 1997;340:89–99.CrossRefPubMed

23.

Janssen B, Vugts DJ, Funke U, Molenaar GT, Kruijer PS, van Berckel BN, et al. Imaging of neuroinflammation in Alzheimer’s disease, multiple sclerosis and stroke: recent developments in positron emission tomography. Biochim Biophys Acta. 1862;2016:425–41.

24.

Versijpt JJ, Dumont F, Van Laere KJ, Decoo D, Santens P, Audenaert K, et al. Assessment of neuroinflammation and microglial activation in Alzheimer’s disease with radiolabelled PK11195 and single photon emission computed tomography. A pilot study. Eur Neurol. 2003;50:39–47.CrossRefPubMed

25.

Probst KC, Izquierdo D, Bird JL, Brichard L, Franck D, Davies JR, et al. Strategy for improved [¹¹C]DAA1106 radiosynthesis and in vivo peripheral benzodiazepine receptor imaging using microPET, evaluation of [¹¹C]DAA1106. Nucl Med Biol. 2007;34:439–46.CrossRefPubMed

26.

Zhang MR, Kida T, Noguchi J, Furutsuka K, Maeda J, Suhara T, et al. [¹¹C]DAA1106: radio synthesis and in vivo binding to peripheral benzodiazepine receptors in mouse brain. Nucl Med Biol. 2003;30:513–19.CrossRefPubMed

27.

Chaki S, Funakoshi T, Yoshikawa R, Okuyama S, Okubo T, Nakazato A, et al. Binding characteristics of [³H]DAA1106, a novel and selective ligand for peripheral benzodiazepine receptors. Eur J Pharmacol. 1999;371:197–204.CrossRefPubMed

28.

Maeda J, Suhara T, Zhang MR, Okauchi T, Yasuno F, Ikoma Y, et al. Novel peripheral benzodiazepine receptor ligand [¹¹C]DAA1106 for PET: an imaging tool for glial cells in the brain. Synape. 2004;52:283–89.CrossRef

29.

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.CrossRefPubMed

30.

Zhang MR, Maeda J, Furutsuka K, Yoshida Y, Ogawa M, Suhara T, et al. [¹⁸F]FMDAA1106 and [¹⁸F]FEDAA1106: two positron-emitter labeled ligands for peripheral benzodiazepine receptor (PBR). Bioorg Med Chem Lett. 2003;13:201–4.CrossRefPubMed

31.

Zhang MR, Maeda J, Ogawa M, Noguchi J, Ito T, Yoshida Y, et al. Development of a new radioligand, N-(5-fluoro-2-phenoxyphenyl)-N-(2-[18F]fluoroethyl-5-methoxybenzyl)acetamide, for pet imaging of peripheral benzodiazepine receptor in primate brain. J Med Chem. 2004;47:2228–35.CrossRefPubMed

32.

Zhang MR, Maeda J, Ito T, Okauchi T, Ogawa M, Noguchi J, et al. Synthesis and evaluation of N-(5-fluoro-2-phenoxyphenyl)-N-(2-[¹⁸F]fluoromethoxy-d(2)-5-methoxybenzyl)acetamide: a deuterium-substituted radioligand for peripheral benzodiazepine receptor. Bioorg Med Chem. 2005;13:1811–18.CrossRefPubMed

33.

Fujimura Y, Ikoma Y, Yasuno F, Suhara T, Ota M, Matsumoto R, et al. Quantitative analyses of [¹⁸F]FEDAA1106 binding to peripheral benzodiazepine receptors in living human brain. J Nucl Med. 2006;47:43–50.PubMed

34.

Briard E, Zoghbi SS, Imaizumi M, Gourley JP, Shetty HU, Hong J, et al. Synthesis and evaluation in monkey of two sensitive [¹¹C]-labeled aryloxyanilide ligands for imaging brain peripheral benzodiazepine receptors in vivo. J Med Chem. 2008;51:17–30.CrossRefPubMed

35.

Kreisl WC, Fujita M, Fujimura Y, Kimura N, Jenko KJ, Kannan P, et al. Comparison of [¹¹C]-(R)-PK 11195 and [¹¹C]PBR28, two radioligands for translocator protein (18 kDa) in human and monkey: implications for positron emission tomographic imaging of this inflammation biomarker. Neuroimage. 2010;49:2924–32.CrossRefPubMed

36.

Imaizumi M, Briard E, Zoghbi SS, Gourley JP, Hong J, Fujimura Y, et al. Brain and whole-body imaging in nonhuman primates of [¹¹C]PBR28, a promising PET radioligand for peripheral benzodiazepine receptors. Neuroimage. 2008;39:1289–98.CrossRefPubMed

37.

Imaizumi M, Kim HJ, Zoghbi SS, Briard E, Hong J, Musachio JL, et al. PET imaging with [¹¹C]PBR28 can localize and quantify upregulated peripheral benzodiazepine receptors associated with cerebral ischemia in rat. Neurosci Lett. 2007;411:200–5.CrossRefPubMed

38.

Zhang J. Mapping neuroinflammation in frontotemporal dementia with molecular PET imaging. J Neuroinflammation. 2015. doi:10.1186/s1297401502365.

39.

Brown AK, Fujita M, Fujimura Y, Liow JS, Stabin M, Ryu YH, et al. Radiation dosimetry and biodistribution in monkey and man of [¹¹C]PBR28: a PET radioligand to image inflammation. J Nucl Med. 2007;48:2072–79.CrossRefPubMed

40.

Hirvonen J, Kreisl WC, Fujita M, Dustin I, Khan O, Appel S, et al. Increased in vivo expression of an inflammatory marker in temporal lobe epilepsy. J Nucl Med. 2012;53:234–40.CrossRefPubMed

41.

Zhang MR, Ogawa M, Maeda J, Ito T, Noguchi J, Kumata K, et al. [2-¹¹C]isopropyl-, [1-¹¹C]ethyl-, and [¹¹C]methyl-labeled phenoxyphenylacetamide derivatives as positron emission tomography ligands for the peripheral benzodiazepine receptor: radiosynthesis, uptake, and in vivo binding in brain. J Med Chem. 2006;49:2735–42.CrossRefPubMed

42.

Imaizumi M, Briard E, Zoghbi SS, Gourley JP, Hong J, Musachio JL, et al. Kinetic evaluation in nonhuman primates of two new PET ligands for peripheral benzodiazepine receptors in brain. Synapse. 2007;61:595–05.CrossRefPubMed

43.

Wilson AA, Garcia A, Parkes J, McCormick P, Stephenson KA, Houle S, et al. Radiosynthesis and initial evaluation of [18F]-FEPPA for PET imaging of peripheral benzodiazepine receptors. Nucl Med Biol. 2008;35:305–14.CrossRefPubMed

44.

Zhang X, Paule MG, Newport GD, Liu F, Callicott, R, et al. MicroPET/CT imaging of [¹⁸F]-FEPPA in the nonhuman primate: a potential biomarker of pathogenic processes associated with anesthetic-induced neurotoxicity. ISRN Anesthesiol. 2012. doi:10.5402/2012/261640.

45.

Vasdev N, Green DE, Vines DC, McLarty K, Mc Cormick PN, Moran MD, et al. Positron-emission tomography imaging of the TSPO with [¹⁸F]FEPPA in a preclinical breast cancer model. Cancer Biother Radiopharm. 2013;28:254–59.CrossRefPubMed

46.

Suridjan I, Rusjan PM, Kenk M, Verhoeff NP, Voineskos AN, Rotenberg D, et al. Quantitative imaging of neuroinflammation in human white matter: a positron emission tomography study with translocator protein 18 kD a radioligand, [¹⁸F]-FEPPA. Synapse. 2014;68:536–47.CrossRefPubMed

47.

Suridjan I, Rusjan PM, Voineskos AN, Selvanathan T, Setiawan E, Strafella AP, et al. Neuroinflammation in healthy aging: a PET study using a novel translocator protein 18kDa (TSPO) radioligand, [¹⁸F]-FEPPA. Neuroimage. 2014;84:868–75.CrossRefPubMed

48.

Ko JH, Koshimori Y, Mizrahi R, Rusjan P, Wilson AA, Lang AE, et al. Voxel-based imaging of translocator protein 18 kDa (TSPO) in high-resolution PET. J Cereb Blood Flow Metab. 2013;33:348–50.CrossRefPubMedPubMedCentral

49.

Mizrahi R, Rusjan PM, Kennedy J, Pollock B, Mulsant B, Suridjan I, et al. Translocator protein (18 kDa) polymorphism (rs6971) explains in-vivo brain binding affinity of the PET radioligand [18F]-FEPPA. J Cereb Blood Flow Metab. 2012;32:968–72.CrossRefPubMedPubMedCentral

50.

Damont A et al. Synthesis of 6-[¹⁸F]fluro-PBR28, a novel radiotracer for imaging the TSPO 18KDa with PET. Bioorg Med Chem Lett. 2011;21:4819–22.CrossRefPubMed

51.

Wang M, Gao M, Zhenq QH. Fully automated synthesis of PET TSPO radioligands [¹¹C]DAA1106 and [¹⁸F]FEDAA1106. Appl Radiat Isot. 2012;70:965–73.CrossRefPubMed

52.

Moon BS, Kim BS, Park C, Jung JH, Lee YW, Lee HY, et al. [¹⁸F]Fluoromethyl-PBR28 as a potential radiotracer for TSPO: preclinical comparison with [¹¹C]PBR28 in a rat model of neuroinflammation. Bioconjug Chem. 2014;25:442–50.CrossRefPubMed

53.

Bereczki D, Fekete I. Vinpocetine for acute ischaemic stroke. Cochrane Database Syst Rev. 2008. doi:10.1002/14651858.

54.

Gulayas B, Halldin C, Vas A, Banati RB, Shchukin E, Finnema S, et al. [¹¹C]vinpocetine: a prospective peripheral benzodiazepine receptor ligand for primate PET studies. J Neurol Sci. 2005;229–230:219–23.CrossRef

55.

Gulayas B, Halldin C, Sandell J, Karlsson P, Sóvágó J, Kárpáti E, et al. PET studies on the brain uptake and regional distribution of [¹¹C]vinpocetine in human subjects. Acta Neurol Scand. 2002;106:325–32.CrossRef

56.

Vas A, Shchukin Y, Karrenbauer VD, Cselényi Z, Kostulas K, Hillert J, et al. Functional neuroimaging in multiple sclerosis with radiolabelled glia markers: preliminary comparative PET studies with [¹¹C]vinpocetine and [11C]PK11195 in patients. J Neurol Sci. 2008;264:9–17.CrossRefPubMed

57.

Gulyas B, Vas A, Tóth M, Takano A, Varrone A, Cselényi Z, et al. Age and disease related changes in the translocator protein (TSPO) system in the human brain: positron emission tomography measurements with [¹¹C]vinpocetine. Neuroimage. 2011;56:1111–21.CrossRefPubMed

58.

Gulyás B, Tóth M, Schain M, Airaksinen A, Vas A, Kostulas K, et al. Evolution of microglial activation in ischaemic core and peri-infarct regions after stroke: a PET study with the TSPO molecular imaging biomarker [¹¹C]vinpocetine. J Neurol Sci. 2012;320:110–7.CrossRefPubMed

59.

Zhang MR, Kumata K, Maeda J, Yanamoto K, Hatori A, Okada M, et al. [11C]AC-5216: a novel PET ligand for peripheral benzodiazepine receptors in the primate brain. J Nucl Med. 2007;48:1853–61.

60.

Kita A, Kohayakawa H, Kinoshita T, Ochi Y, Nakamichi K, Kurumiya S, et al. Antianxiety and antidepressant-like effects of AC-5216, a novel mitochondrial benzodiazepine receptor ligand. Br J Pharmacol. 2004;142:1059–72.

61.

Okuyama S, Chaki S, Yoshikawa R, Ogawa S, Suzuki Y, Okubo T, et al. Neuropharmacological profile of peripheral benzodiazepine receptor agonists, DAA1097 and DAA1106. Life Sci. 1999;64:1455–64.

62.

Yanamoto K, Zhang MR, Kumata K, Hatori A, Okada M, Suzuki K. In vitro and ex vivo autoradiography studies on peripheral-type benzodiazepine receptor binding using [11C]AC-5216 in normal and kainic acid-lesioned rats. Neuro Sci Lett. 2007;428:59–63.

63.

Amitani M, Zhang MR, Noguchi J, Kumata K, Ito T, Takai N, et al. Blood flow dependence of the intratumoral distribution of peripheral benzodiazepine receptor binding in intact mouse fibrosarcoma. Nucl Med Biol. 2006;33:971–75.

64.

Miyoshi M, Ito H, Arakawa R, Takano H, Hiquchi M, Qkumura M, et al. Quantitative analysis of peripheral benzodiazepine receptor in the human brain using PET with [11C]AC-5216. J Nucl Med. 2009;50:1095–101.

65.

Yanamoto K, Yamasaki T, Kumata K, Yui J, Odawara C, Kawamura K, et al. Evaluation of N-benzyl-N-[11C]methyl-2-(7-methyl-8-oxo-2-phenyl-7,8-dihydro-9H-purin-9yl)acetamide ([11C]-DAC as a novel translocator protein (18 kDa) radioligand in kainic acid-lesioned rat. Synapse. 2009;63:961–71.

66.

James ML, Fulton RR, Henderson DJ, Eberl S, Meikle SR, Thomson S, et al. Synthesis and in vivo evaluation of a novel peripheral benzodiazepine receptor PET radioligand. Bioorg Med Chem. 2005;13:6188–94.

67.

Boutin H, Chauveau F, Thominiaux C, Grégoire MC, James ML, Trebossen R, et al. [11C]DPA-713: a novel peripheral benzodiazepine receptor PET ligand for in vivo imaging of neuroinflammation. J Nucl Med. 2007;48:573–81.

68.

Endres CJ, Pomper MG, James M, Uzuner O, Hammoud DA, Watkins CC, et al. Initial evaluation of [11C]DPA-713, a novel TSPO PET ligand, in humans. J Nucl Med. 2009;50:1276–82.

69.

Endres CJ, Coughlin JM, Gage KL, Watkins CC, Kassiou M, Pomper MG. Radiation dosimetry and biodistribution of the TSPO ligand [11C]DPA-713 in humans. J Nucl Med. 2012;53:330–35.

70.

Arlicot N, Vercouillie J, Ribeiro MJ, Tauber C, Venel Y, Baulieu JL, et al. Initial evaluation in healthy humans of [18F]DPA-714, a potential PET biomarker for neuroinflammation. Nucl Med Biol. 2012;39:570–8.

71.

James ML, Fulton RR, Vercoullie J, Henderson DJ, Garreau L, Chalon S, et al. DPA-714, a new translocator protein-specific ligand: synthesis, radiofluorination, and pharmacologic characterization. J Nucl Med. 2008;49:814–22.

72.

Chauveau F, Van Camp N, Dollé F, Kuhnast B, Hinnen F, Damont A, et al. Comparative evaluation of the translocator protein radioligands [11C]DPA-713, [18F]DPA-714, and [11C]PK11195 in a rat model of acute neuroinflammation. J Nucl Med. 2009;50:468–47.

73.

Corcia P, Tauber C, Vercoullie J, Arlicot N, Prunier C, Praline J, et al. Molecular imaging of microglial activation in amyotrophic lateral sclerosis. PLoS One. 2012;7:e52941.

74.

Golla SS, Boellaard R, Oikonen V, HolfMann A, van Berckel BN, Windhorst AD, et al. Quantification of [18F]DPA-714 binding in the human brain: initial studies in healthy controls and Alzheimer’s disease patients. J Cereb Blood Flow Metab. 2015;35:766–72.

75.

Ribeiro MJ, Vercouillie J, Debiais S, Cottier JP, Bonnaud I, Camus V, et al. Could [18F]DPA-714 PET imaging be interesting to use in the early post-stroke period. EJNMMI Res. 2014. doi:10.1186/s1355001400284.

76.

Boutin H, Prenant C, Maroy R, Galea J, Greenhalgh AD, Smigova A, et al. [18F]DPA-714: direct comparison with [11C]PK11195 in a model of cerebral ischemia in rats. PLoS One. 2013;8:e56441.

77.

Tang D, Nickels ML, Tantawy MN, Buck JR, Manning HC. Preclinical imaging evaluation of novel TSPO-PET ligand 2-(5,7-Diethyl-2-(4-(2-[18F]fluoroethoxy) phenyl) pyrazolo[1,5-a]pyrimidin-3-yl)-N, N-diethylacetamide ([18F]VUIIS1008) in glioma. Mol Imaging Biol. 2014;16:813–20.

78.

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;16:2899–923.

79.

Boutin H, Chauveau F, Thominiaux C, Kuhnast B, Grégoire MC, Jan S, et al. In vivo imaging of brain lesions with [11C]CLINME, a new PET radioligand of peripheral benzodiazepine receptors. GLIA. 2007;55:1459–68.

80.

Sekimata K, Hatano K, Ogawa M, Abe J, Magata Y, Biggio G, et al. Radiosynthesis and in vivo evaluation of N-[11C]methylated imidazopyridineacetamides as PET tracers for peripheral benzodiazepine receptors. Nucl Med Biol. 2008;35:327–34.

81.

Perrone M, Perrone M, Moon BS, Park HS, Laquintana V, Jung JH, et al. A novel PET imaging probe for the detection and monitoring of translocator protein 18 kDa expression in pathological disorders. Sci Rep. 2016;6:204–22.

82.

Van Camp N, Boisgard R, Kuhnast B, Thézé B, Viel T, Grégoire MC, et al. In vivo imaging of neuroinflammation: a comparative study between [¹⁸F]PBR111, [¹¹C]CLINME and [¹¹C]PK11195 in an acute rodent model. Eur J Nucl Med Mol Imaging. 2010;37:962–72.CrossRefPubMed

83.

Fookes CJ, Pham TQ, Mattner F, Greguric I, Loc’h C, Liu X, et al. Synthesis and biological evaluation of substituted [¹⁸F]imidazo[1,2-a] pyridines and [¹⁸F]pyrazolo[1,5-a]pyrimidines for the study of the peripheral benzodiazepine receptor using positronemission tomography. J Med Chem. 2008;51:3700–12.CrossRefPubMed

84.

Thominiaux C, Damont A, Kuhnast B, Demphel S, Helleix S, Boisnard S, et al. Radiosynthesis of 7- chloro-N, N-dimethyl-5-[11C]methyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide, [11C]SSR180575, a novel radioligand for imaging the TSPO (peripheral benzodiazepine receptor) with PET. J Label Compd Radiopharm. 2010;53:767–73.

85.

Chauveau F, Boutin H, Van Camp N, Thominiaux C, Hantraye P, Rivron L, et al. In vivo imaging of neuroinflammation in the rodent brain with [¹¹C] SSR180575, a novel indoleacetamide radioligand of the translocator protein (18 kDa). Eur J Nucl Med Mol Imaging. 2011;38:509–14.CrossRefPubMed

86.

Chau WF, Black AM, Clarke A, Durrant C, Gausemel I, Khan I, et al. Exploration of the impact of stereochemistry on the identification of the novel translocator protein PET imaging agent [¹⁸F]GE-180. Nucl Med Biol. 2015;42:711–19.

87.

Wadsworth H, Jones PA, Chau WF, Durrant C, Fouladi N, Passmore J, et al. 18F-GE- 180: a novel fluorine-18 labelle PET tracer for imaging translocator protein 18kDa (TSPO). Bioorg Med Chem Lett. 2012;22:1308–13.

88.

Dickens AM, Vainio S, Marjamäki P, Johansson J, Lehtiniemi P, Rokka J, et al. Detection of microglial activation in an acute model of neuroinflammation using PET and radiotracers [¹¹C](R)-PK11195 and [¹⁸F]-GE-180. J Nucl Med. 2014;55:466–72.

89.

Boutin H, Murray K, Pradillo J, Maroy R, Smigova A, Gerhard A, et al. [¹⁸F]GE-180: a novel TSPO radiotracer compared to 11C-R-PK11195 in a preclinical model of stroke. Eur J Nucl Med Mol Imaging. 2015;42:503–11.CrossRefPubMed

90.

Tiwari AK, Yui J, Fujinaga M, Kumata K, Shimoda Y, Yamasaki T, et al. Characterization of a novel acetamido-benzoxazolone-based PET ligand for translocator protein (18 kDa) imaging of neuroinflammation in the brain. J Neurochem. 2014;129:712–20.CrossRefPubMed

91.

Tiwari AK, Fujinaga M, Yui J, Yamasaki T, Xie L, Kumata K, et al. Synthesis and evaluation of new [¹⁸F]-labelled acetamidobenzoxazolone-based radioligands for imaging of the translocator protein (18 kDa, TSPO) in the brain. Org Biomol Chem. 2014;12:9621–31.CrossRefPubMed

92.

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.

93.

Dickstein LP, Zoghbi SS, Fujimura Y, Imaizumi M, Zhang Y, Pike VW, et al. Comparison of [¹⁸F]- and [¹¹C]-labeled aryloxyanilide analogs to measure translocator protein in human brain using positron emission tomography. Eur J Nucl Med Mol Imaging. 2011;38:352–7.CrossRefPubMed

94.

Guo Q, Colasanti A, Owen DR, Onega M, Kamalakaran A, Bennacef I, et al. Quantification of the specific translocator protein signal of 18F-PBR111 in healthy humans: a genetic polymorphism effect on in vivo binding. J Nucl Med. 2013;54:1915–23.

95.

Lavisse S, Guillermier M, Hérard AS, Petit F, Delahaye M, Van Camp N, et al. Reactive astrocytes overexpress TSPO and are detected by TSPO positron emission tomography imaging. J Neurosci. 2012;32:10809–18.

96.

Varley J, Brooks DJ, Edison P. Imaging neuroinflammation in Alzheimer’s disease and other dementias: recent advances and future directions. Alzheimers Dement. 2015;11:1110–20.CrossRefPubMed

Titel: Recent Progress in the Development of TSPO PET Ligands for Neuroinflammation Imaging in Neurological Diseases
verfasst von: Md. Maqusood Alam
Jihye Lee
Sang-Yoon Lee
Publikationsdatum: 16.03.2017
Verlag: Springer Berlin Heidelberg
Erschienen in: Nuclear Medicine and Molecular Imaging / Ausgabe 4/2017
Print ISSN: 1869-3474
Elektronische ISSN: 1869-3482
DOI: https://doi.org/10.1007/s13139-017-0475-8

Live-Webinar: Aktuelle Leitlinien bei Herz-Kreislauf-Erkrankungen

Springer Medizin

Recent Progress in the Development of TSPO PET Ligands for Neuroinflammation Imaging in Neurological Diseases

Abstract

Live-Webinar: Aktuelle Leitlinien bei Herz-Kreislauf-Erkrankungen

Springer Medizin

Abstract

Bitte loggen Sie sich ein, um Zugang zu diesem Inhalt zu erhalten

Weitere Artikel der Ausgabe 4/2017

Evaluation of Cadmium-Zinc-Telluride Detector-based Single-Photon Emission Computed Tomography for Nuclear Cardiology: a Comparison with Conventional Anger Single-Photon Emission Computed Tomography

Recurrent Follicular Dendritic Cell Sarcoma of the Parotid Gland Imaged with 18F-FDG PET/CT

Longitudinal Decline of Striatal Subregional [18F]FP-CIT Uptake in Parkinson’s Disease

68Ga-PSMA PET-CT Imaging of Metastatic Adenoid Cystic Carcinoma

Microcalcified Hepatic Metastases Incidentally Detected on F-18 NaF PET/CT in a Patient with Prostate Cancer

Usefulness of Tc-99m Pertechnetate SPECT/CT in the Diagnosis of Testicular Infarction After Inguinal Herniorrhaphy