PT  - JOURNAL ARTICLE
AU  - Damont, Annelaure
AU  - Van Camp, Nadja
AU  - Kuhnast, Bertrand
AU  - Boisgard, Raphael
AU  - Chauveau, Fabien
AU  - Probst, Katrin
AU  - Katsifis, Andrew
AU  - Kassiou, Mickael
AU  - Tavitian, Bertrand
AU  - Dolle, Frederic
TI  - Radiolabeling and comparative studies of [18F]DPA-714, [18F]PBR111 AND [18F]FEDAA1106, potent TSPO 18kDa PET-imaging candidates
DP  - 2009 May 01
TA  - Journal of Nuclear Medicine
PG  - 1962--1962
VI  - 50
IP  - supplement 2
4099  - http://jnm.snmjournals.org/content/50/supplement_2/1962.short
4100  - http://jnm.snmjournals.org/content/50/supplement_2/1962.full
SO  - J Nucl Med2009 May 01; 50
AB  - 1962 Objectives DPA-714, PBR111, FEDAA1106, three challengers of PK11195 for TSPO 18 kDa imaging, were labeled with fluorine-18. Comparative pharmacological evaluation was performed by autoradiography in an acute rodent model of neuroinflammation. Methods Fluorine-18-labeling has been automated on our Zymate-XP robotic system and involves: (A) reaction of K[18F]F-Kryptofix®222 with the appropriate precursor at 165°C for 5 min in DMSO, (B) C-18 PrepSep cartridge pre-purification, (C) semi-preparative HPLC purification and (4) Sep-pak®Plus-based formulation. In vitro binding properties of these labeled ligands were studied in a rat model of focal acute neuroinflammation, and were compared with the reference compound [11C]PK11195, using autoradiography. Immunohistochemistry study was performed to validate the in vitro data. Results 5-7 GBq of [18F]DPA-714, [18F]PBR111 and [18F]FEDAA1106 (> 95% chemically and radiochemically pure) could be obtained with SRA ranging from 37 to 111 GBq/micromol within 90 minutes starting from a 37 GBq [18F]fluoride batch. Radiotracer localisation as detected by autoradiography correlated well with that activated microglial cells demonstrated by immunohistochemistry and TSPO 18kDa expression. Conclusions [18F]DPA-714, [18F]PBR111, [18F]FEDAA1106 were synthesized in 8%-20% ndc radiochemical yield. Autoradiography studies confirm their potential for TSPO 18kDa expression imaging Research Support Supported by the EC DiMI (LSHB-CT-2005-512146) and EMIL (LSH-2004-503569). Thanks’ to J. Clark (Univ. Edinburgh).