Technetium-99m p-iodophenethyldiaminodithiol (DADT-IPE): potential brain perfusion imaging agent for SPECT

Int J Rad Appl Instrum B. 1992 Apr;19(3):303-10. doi: 10.1016/0883-2897(92)90115-f.

Abstract

A new ligand, an N-p-iodophenethyl diaminodithiol (DADT-IPE), an anlog of N-isopropyl-p-iodoamphetamine (IMP), was synthesized and subsequently complexed with 99mTc, using stannous chloride as a reducing agent. Two complexes (a and b) were separated from 99mTc-DADT-IPE by high performance liquid chromatography (HPLC). Competitive inhibition studies showed that the IC50 value of DADT-IPE (70 microM) was similar to that of IMP (49 microM). Biodistribution studies of one of the complexes [99mTc-DADT-IPE(a)] in rats showed that 0.65% of the injected dose of the tracer remained in the brain at 5 min after intravenous injection, with 0.53% of the dose remaining in the brain at 60 min post-injection, whereas the corresponding values for the other complex [99mTc-DADT-IPE(b)] were 0.34% dose in the brain at 5 min and 0.28% dose in the brain at 60 min post-injection. The half-life for clearance of 99mTc-DADT-IPE(a) from rat brain was found to be more than 5 h. These results suggested that 99mTc-DADT-IPE(a) has characteristics which are suitable for cerebral perfusion imaging.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Autoradiography
  • Binding, Competitive
  • Brain / diagnostic imaging*
  • Brain / metabolism
  • Inosine Monophosphate / chemistry
  • Inosine Monophosphate / metabolism
  • Isotope Labeling / methods
  • Kinetics
  • Male
  • Organotechnetium Compounds / chemical synthesis*
  • Organotechnetium Compounds / pharmacokinetics
  • Perfusion
  • Radionuclide Imaging
  • Rats
  • Rats, Inbred Strains
  • Sulfhydryl Compounds / chemical synthesis*
  • Sulfhydryl Compounds / pharmacokinetics
  • Tissue Distribution

Substances

  • Organotechnetium Compounds
  • Sulfhydryl Compounds
  • Inosine Monophosphate
  • technetium Tc 99m 4-iodophenethyldiaminodithiol