99mTc-glucarate for detection of isoproterenol-induced myocardial infarction in rats

Int J Pharm. 2002 Feb 21;233(1-2):29-34. doi: 10.1016/s0378-5173(01)00922-x.

Abstract

Infarct-avid radiopharmaceuticals are necessary for rapid and timely diagnosis of acute myocardial infarction. The animal model used to produce infarction implies artery ligation but chemical induction can be easily obtained with isoproterenol. A new infarct-avid radiopharmaceutical based on glucaric acid was prepared in the hospital radiopharmacy of the INCMNSZ. 99mTc-glucarate was easy to prepare, stable for 96 h and was used to study its biodistribution in rats with isoproterenol-induced acute myocardial infarction. Histological studies demonstrated that the rats developed an infarct 18 h after isoproterenol administration. The rat biodistribution studies showed a rapid blood clearance via the kidneys. Thirty minutes after 99mTc-glucarate administration the standardised heart uptake value S(h)UV was 4.7 in infarcted rat heart which is six times more than in normal rats. ROIs drawn over the gamma camera images showed a ratio of 4.4. The high image quality suggests that high contrast images can be obtained in humans and the 96 h stability makes it an ideal agent to detect, in patients, early cardiac infarction.

MeSH terms

  • Animals
  • Cardiotonic Agents / adverse effects
  • Glucaric Acid / analogs & derivatives*
  • Glucaric Acid / chemical synthesis
  • Glucaric Acid / pharmacokinetics
  • Isoproterenol / adverse effects*
  • Male
  • Myocardial Infarction / chemically induced*
  • Myocardial Infarction / diagnostic imaging*
  • Organotechnetium Compounds* / pharmacokinetics
  • Radionuclide Imaging
  • Radiopharmaceuticals* / chemical synthesis
  • Radiopharmaceuticals* / pharmacokinetics
  • Rats
  • Rats, Wistar

Substances

  • Cardiotonic Agents
  • Organotechnetium Compounds
  • Radiopharmaceuticals
  • technetium Tc 99m glucarate
  • Isoproterenol
  • Glucaric Acid