Synthesis and in vivo evaluation of 7-chloro-5-[123I]iodo-4-oxo-1,4-dihydroquinoline-2-carboxylic acid.
As a possible radioligand for SPECT visualization of the NMDA receptors in the central nervous system, 7-chloro-5-[123I]iodokynurenic acid was prepared. This paper presents the synthesis of both the radioactive and the non-radioactive product, starting from 5-bromo-7-chlorokynurenic acid and using a non-isotopic nucleophilic halogen exchange reaction in the presence of iodide (Na123I or KI). Under the best labelling conditions, the radiochemical yield was 85%. The specific activity based on UV detection was found to be higher than 1 Ci/mumol (= 37 GBq/mumol) and the chemical and radiochemical (> 95%) purity of the tracer was checked by RP-HPLC.
Dumont
F
F
Department of Radiopharmacy, Faculty of Pharmaceutical Sciences, Ghent, Belgium.
Slegers
G
G
D000818:Animals; D018691:Excitatory Amino Acid Antagonists / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D007457:Iodine Radioisotopes / Q000737:chemistry*; D007553:Isotope Labeling / Q000379:methods; D007736:Kynurenic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000493:pharmacokinetics; D008297:Male; D051379:Mice; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D014018:Tissue Distribution
C109987:7-chloro-5-iodokynurenic acid; D018691:Excitatory Amino Acid Antagonists; D007457:Iodine Radioisotopes; D019275:Radiopharmaceuticals; D007736:Kynurenic Acid