NDLI: Optimisation of synthesis, purification and reformulation of $(R)-[N-Methyl-^{11}C]PK11195$ for in vivo PET imaging studies

Content Provider	IEEE Xplore Digital Library
Author	Alves, V.H. Abrunhosa, A.J. Castelo-Branco, M.
Copyright Year	2013
Description	Author affiliation: Inst. de Cienc. Nucl. Aplic. a Saude (ICNAS), Univ. de Coimbra, Coimbra, Portugal (Alves, V.H.; Abrunhosa, A.J.; Castelo-Branco, M.)
Abstract	Neurodegenerative, inflammatory and neoplastic disorders involve neuroinflammatory reactions in the central nervous system that isolate the damaged tissue and promote im-mune responses by the activation of resident cells of the mono-cytes lineage (microglia). This process involves an overexpression of the 18 kDa translocator protein receptor (TSPO). PK11195 is an isoquinoline carboxamide which binds selectively to this re-ceptor. The (R)-enantiomer radiolabelled with carbon-11 is the most widely used radiotracer for in vivo TSPO imaging with Posi-tron Emission Tomography (PET). We report the optimisation of synthesis, purification and reformulation of $(R)-[N-MethyJ-^{11}C]PK11195$ by the captive solvent method suitable for use in human PET imaging studies. $(R)-[NMethyJ-^{11}C]PK11195$ was prepared from [N-Desmethyl]PK11195 by alkylation with [llC]methyl iodide reacting at room temperature in an high-performance liquid chromatography loop, purified and reformulated by solid phase extraction. Synthesis process is carried out in about 35 minutes, and quality control tests were performed to ensure the good quality of product. The specific activity of $(R)-[N-MethyJ-^{11}C]PK11195$ was 25±10 GBq/μmol, and radiochemical purity was better than 95%.
Sponsorship	IEEE Portugal Sect. EMB Chapter
Starting Page	1
Ending Page	5
File Size	573386
Page Count	5
File Format	PDF
ISBN	9781467348591
e-ISBN	9781467348591
DOI	10.1109/ENBENG.2013.6518428
Language	English
Publisher	Institute of Electrical and Electronics Engineers, Inc. (IEEE)
Publisher Date	2013-02-20
Publisher Place	Portugal
Access Restriction	Subscribed
Rights Holder	Institute of Electrical and Electronics Engineers, Inc. (IEEE)
Subject Keyword	Earth Observing System $[^{11}C]CHI$ Europe $[^{11}C]CO$ Neuroinflammation Microglia ‘wet’ method Heating Carbon 11 TSPO PET $[^{11}C]PK11195$ Captive solvent loop
Content Type	Text
Resource Type	Article

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