Binding of tritiated and radioiodinated ZM241,385 to brain A2A adenosine receptors

Nucl Med Biol. 2004 Feb;31(2):173-7. doi: 10.1016/j.nucmedbio.2003.10.007.

Abstract

Autoradiography on rat brain using tritiated (1*), mono- (2*) and di-radioiodinated (3*) derivatives of the A(2A) adenosine receptor antagonist ZM241,385 showed high receptor density in striatum. K(D)s of 1*, 2* and 3* were 0.4, 2.2 and 15 nM and nonspecific binding was 5, 40 and 50% of total binding. Striatal uptake of 2* in mice was approximately 0.2% ID/g 60 min post-injection; blocking by 2 was insignificant. Poor penetration of the blood brain barrier and high nonspecific binding make 2* unsuitable for imaging striatal receptors.

Publication types

  • Comparative Study
  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Brain / diagnostic imaging*
  • Brain / metabolism*
  • Iodine Radioisotopes / pharmacokinetics
  • Isotope Labeling / methods
  • Metabolic Clearance Rate
  • Organ Specificity
  • Protein Binding
  • Radionuclide Imaging
  • Radiopharmaceuticals / pharmacokinetics
  • Rats
  • Receptor, Adenosine A2A / metabolism*
  • Tissue Distribution
  • Triazines / pharmacokinetics*
  • Triazoles / pharmacokinetics*
  • Tritium / pharmacokinetics

Substances

  • Iodine Radioisotopes
  • Radiopharmaceuticals
  • Receptor, Adenosine A2A
  • Triazines
  • Triazoles
  • ZM 241385
  • Tritium