Radio synthesis and in vivo evaluation of two α7 nAChRs radioligands: [125I]CAIPE and [125I]IPPU

详细信息    查看全文

• 作者：Aiqin Wu ; Xiang Li ; Qianqian Xue…
• 关键词：α7 nAChRs ; AD ; I ; 125 radiolabled ; [125I]CAIPE ; [125I]IPPU
• 刊名：Journal of Radioanalytical and Nuclear Chemistry
• 出版年：2016
• 出版时间：February 2016
• 年：2016
• 卷：307
• 期：2
• 页码：1345-1351
• 全文大小：656 KB
• 参考文献：1.Paul A (1992) Nicotinic blockade produces cognitive impairment in normal humans. Psychopharmacol 108:480–484CrossRef
  2.Jones GMM (1992) Effects of acute subcutaneous nicotine on attention, information processing and short-term memory in Alzheimer’s disease. Psychopharmacol 108:485–494CrossRef
  3.Malysz (2009) In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile. J Pharmacol Exp Ther 330:257–267CrossRef
  4.David J (2008) [3H]A-585539 [(1S, 4S)-2, 2-dimethyl-5-(6-phenylpyridazin-3-yl)-5-aza-2-azoniabicyclo [2.2.1] heptane], a novel high-affinity 7 neuronal nicotinic receptor agonist: radioligand binding characterization to rat and human brain. J Pharmacol Exp Ther 324:179–187
  5.Edson X (2009) Mammalian nicotinic acetylcholine receptors: from structure to function. Physiol Rev 89:73–120CrossRef
  6.Parri (2011) Research update: alpha7 nicotinic acetylcholine receptor mechanisms in Alzheimer’s disease. Biochem Pharmacol 82:931–942CrossRef
  7.Philip (2010) Nicotinic acetylcholine receptors and depression: a review of the preclinical and clinical literature. Psychopharmacology 212:1–12CrossRef
  8.Wevers Andrea (2000) Expression of nicotinic acetylcholine receptors in Alzheimer’s disease: postmortem investigations and experimental approaches. Behav Brain Res 113:207–215CrossRef
  9.Gao Y (2013) Derivatives of dibenzothiophene for positron emission tomography imaging of alpha7-nicotinic acetylcholine receptors. J Med Chem 56:7574–7589CrossRef
  10.Rotering (2013) Radiosynthesis and first evaluation in mice of [18F]NS14490 for molecular imaging of alpha7 nicotinic acetylcholine receptors. Bioorg Med Chem 21:2635–2642CrossRef
  11.Ravert (2013) Radiochemical synthesis and in vivo evaluation of [18F]AZ11637326: an agonist probe for the alpha7 nicotinic acetylcholine receptor. Nucl Med Biol 40:731–739CrossRef
  12.Ishikawa Masatomo (2011) Occupancy of α7 nicotinic acetylcholine receptors in the brain by tropisetron: a positron emission tomography study using [11C]CHIBA-1001 in healthy human subjects. Clin Psychopharmacol Neurosci 9:111–116CrossRef
  13.Sakata M (2011) Biodistribution and radiation dosimetry of the alpha7 nicotinic acetylcholine receptor ligand [11C]CHIBA-1001 in humans. Nucl Med Biol 38:443–448CrossRef
  14.Tanibuchi (2010) Characterization of [3H]CHIBA-1001 binding to alpha7 nicotinic acetylcholine receptors in the brain from rat, monkey, and human. Brain Res 1348:200–208CrossRef
  15.Toyohara (2009) Preclinical and the first clinical studies on [11C]CHIBA-1001 for mapping alpha7 nicotinic receptors by positron emission tomography. Ann Nucl Med 23:301–309CrossRef
  16.Kulak J (2004) Differences in alpha7 nicotinic acetylcholine receptor binding in motor symptomatic and asymptomatic MPTP-treated monkeys. Brain Res 999:193–202CrossRef
  17.Kulak (2006) [125I]Iodomethyllycaconitine binds to alpha7 nicotinic acetylcholine receptors in monkey brain. Eur J Neurosci 23:2604–2610CrossRef
  18.Whiteaker Paul (1999) An autoradiographic study of the distribution of binding sites for the novel a7-selective nicotinic radioligand [3H]-methyllycaconitine in the mouse brain. Eur J Neurosci 11:2689–2696CrossRef
  19.Clarke Paul B S (1985) Nicotinic binding in rat brain: autoradiographic comparison of [3H]acetylcholine, [3H]nicotine, and [125I]-α-bungarotoxin. J Neurosci 5:1307–1315
  20.Tichauer (2012) In vivo quantification of tumor receptor binding potential with dual-reporter molecular imaging. Mol Imaging Biol 14:584–592CrossRef
  21.Herna´n A (2000) Synthesis and pharmacological characterization of [125I]iodomethyllycaconitine ([125I]iodo-MLA). A new ligand for the α7 nicotinic acetylcholine receptor. J Med Chem 43:142–145CrossRef
  22.Deuther-Conrad (2011) Assessment of alpha7 nicotinic acetylcholine receptor availability in juvenile pig brain with [18F]NS10743. Eur J Nucl Med Mol Imaging 38:1541–1549CrossRef
  23.Ogawa (2010) Synthesis and evaluation of new imaging agent for central nicotinic acetylcholine receptor alpha7 subtype. Nucl Med Biol 37:347–355CrossRef
  
• 作者单位：Aiqin Wu (1)
  Xiang Li (1)
  Qianqian Xue (1)
  Yongjuan Liu (2)
  Xia Lu (3)
  Xi Yan (1)
  Huabei Zhang (1)
  
  1. Key Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, No. 19, Xinjiekouwai Street, Haidian District, Beijing, 100875, People’s Republic of China
  2. Pfizer Investment Co., Ltd, 11F, Tower B, Minmetals Plaza, No. 3-7 North Chao Yang Men Avenue, Dongcheng District, Beijing, 100010, People’s Republic of China
  3. Beijing An Zhen Hospital of the Capital University of Medical Sciences, No. 2, Anzhen St., Chaoyang District, Beijing, 100029, People’s Republic of China
  
• 刊物类别：Chemistry and Materials Science
• 刊物主题：Chemistry
  Nuclear Chemistry
  Physical Chemistry
  Nuclear Physics, Heavy Ions and Hadrons
  Diagnostic Radiology
  Inorganic Chemistry
  
• 出版者：Akad茅miai Kiad贸, co-published with Springer Science+Business Media B.V., Formerly Kluwer Academic
• ISSN：1588-2780

文摘

The radio synthesis and in vivo evaluation of two α7 nAChRs radioligands [125I]CAIPE and [125I]IPPU were reported. They were obtained from their tributyltin precursors with high radio chemical yields (>90 %) and good radio chemical purities (>95 %). Biodistribution and blockade studies of [125I]CAIPE showed that the accumulation of radioactivity in the mouse brain was specific and selective. Keywords α7 nAChRs AD I-125 radiolabled [125I]CAIPE [125I]IPPU