Radiosynthesis of 7‐chloro‐ N , N ‐dimethyl‐5‐[<sup>11</sup>C]methyl‐4‐oxo‐3‐phenyl‐3,5‐dihydro‐4 H ‐pyridazino[4,5‐ b ]indole‐1‐acetamide, [<sup>11</sup>C]SSR180575, a novel radioligand for imaging the TSPO (peripheral benzodiazepine receptor) with PET
作者: Cyrille ThominiauxAnnelaure DamontBertrand KuhnastStéphane DemphelStéphane Le HelleixSabine BoisnardLuc RivronFabien ChauveauHervé BoutinNadia Van CampRaphaël BoisgardSébastien RoyJohn AllenThomas RooneyJesus BenavidesPhilippe HantrayeBertrand TavitianFrédéric Dollé
作者单位: 1CEA, I2BM, Service Hospitalier Frédéric Joliot, 4 place du Général Leclerc, F‐91401 Orsay, France
2 Sanofi‐Aventis, ICMS, 1 avenue Pierre Brossolette, F‐91385 Chilly‐Mazarin, France
3 INSERM, U1023, 4 place du Général Leclerc, F‐91401 Orsay, France
4 Sanofi‐Aventis, CNS Department, 13 Quai Jules Guesde, F‐94400 Vitry‐sur‐Seine, France
5 CEA, I2BM, MIRCen, 4 place du Général Leclerc, F‐91401 Orsay, France
6 CNRS, UMR 5220; INSERM, U630; INSA de Lyon; Creatis; Bron F‐69677, France; Université de Lyon, Lyon 1, Lyon F‐69003, France.
7 Faculty of Life Sciences, AV Hill Building, University of Manchester, Manchester M13 9PT, UK.
8 CEA, Service hospitalier Frédéric Joliot, Institut d'imagerie biomédicale, 4 place du Général Leclerc, F‐91406 Orsay, France
刊名: Journal of Labelled Compounds and Radiopharmaceuticals, 2010, Vol.53 (13), pp.767-773
来源数据库: Wiley Journal
DOI: 10.1002/jlcr.1794
关键词: carbon‐11methylationSSR180575PBRTSPO 18 kDa
原始语种摘要: Abstract(#br)SSR180575 (7‐chloro‐ N , N, 5‐trimethyl‐4‐oxo‐3‐phenyl‐3,5‐dihydro‐4 H ‐pyridazino[4,5‐ b ]indole‐1‐acetamide) is the lead compound of an original pyridazinoindole series of potent and highly selective TSPO (peripheral benzodiazepine receptor) ligands. Isotopic labeling of SSR180575 with the short‐lived positron‐emitter carbon‐11 (T1/2: 20.38 min) at its 5‐methylpyridazino[4,5‐ b ]indole moiety as well as at its N,N ‐dimethylacetamide function by methylation of the corresponding nor ‐analogues was investigated. Best results in terms of radiochemical yields and purities were obtained for the preparation of [ indole‐N‐methyl‐ 11C]SSR180575, where routine production batches of 4.5–5.0 GBq of radiochemically pure (>99%) i.v. injectable solutions (specific...
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关键词翻译
关键词翻译
  •  二氢的
  • acetamide 乙酰胺
  • dimethyl 二甲基
  • phenyl 苯基
  • chloro 绿
  • indole 吲哚
  • dihydro 二氢的
  • oxo 二氢的
  • radiochemical 放射化学的
  • SSR Secondary Surveillance Radar
  • benzodiazepine 苯二氮