title: Synthesis, characterization and in vivo evaluation of [(62)Zn]-benzo-δ-sultam complex as a possible pet imaging agent.
abstract: OBJECTIVE
  The development of a new tracer based on the cyclic sulfonamides (sultams) was investigated.
  
  
  METHODS
  3-(Methoxy-phenyl-methyl)-1,6-dimethyl-1H benzo[c][1,2] thiazine 2,2-dioxide (benzo-δ-sultam) was synthesized and characterized by elemental analysis, FT-IR spectroscopy and single crystal X-ray structure determination. The prepared cyclic sulfonamide was labeled with non-commercial (62)Zn radioisotope for fast in vivo targeting and Coincidence imaging purposes (radiochemical purity 97 % ITLC, 96 % HPLC, specific activity 20-23 GBq/mmol). In vivo biodistribution of the final complex was investigated in Sprague Dawley(®) rats bearing fibro sarcoma tumor after 2, 4 and 8 h post injection and compared with free Zn(+2) cation.
  
  
  RESULTS
  Using instant paper chromatography method, the physicochemical properties of labeled compounds were found sufficiently stable in organic phases, e.g. a human serum, to be reliably used in bioapplications.
  
  
  CONCLUSIONS
  The complex exhibited a rapid as well as high tumor uptake (tumor to blood ratio 4.38 and tumor to muscle ratio 9.63) resulting in an efficient tumor targeting agent.
authors.affiliation: School of Chemistry, College of Science, University of Tehran, P.O. Box 14155 6455, Tehran, Iran.
authors.forename: Mehdi
authors.initials: M
authors.lastname: Ghandi
authors.forename: Shahzad
authors.initials: S
authors.lastname: Feizi
authors.forename: Farhood
authors.initials: F
authors.lastname: Ziaie
authors.forename: Yousef
authors.initials: Y
authors.lastname: Fazaeli
authors.forename: Behrooz
authors.initials: B
authors.lastname: Notash
mesh_terms: D000818:Animals; D002851:Chromatography, High Pressure Liquid; D002854:Chromatography, Paper; D006801:Humans; D015394:Molecular Structure; D009282:Naphthalenesulfonates / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D009374:Neoplasms, Experimental / Q000000981:diagnostic imaging; D049268:Positron-Emission Tomography / Q000295:instrumentation / Q000379:methods*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D017207:Rats, Sprague-Dawley; D012509:Sarcoma / Q000000981:diagnostic imaging; D044967:Serum / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared; D015037:Zinc Radioisotopes / Q000737:chemistry / Q000493:pharmacokinetics
chemical_list: D009282:Naphthalenesulfonates; D019275:Radiopharmaceuticals; D015037:Zinc Radioisotopes; C016768:naphthosultone