Related Experiment Video
Updated: Jun 6, 2026

Preparation and Evaluation of 99mTc-labeled Tridentate Chelates for Pre-targeting Using Bioorthogonal Chemistry
Published on: February 4, 2017
Minimizing liver uptake of cationic Tc radiotracers with ether and crown ether functional groups
Young-Seung Kim1, Fan Wang, Shuang Liu
1Young-Seung Kim, Shuang Liu, School of Health Sciences, Purdue University, 550 Stadium Mall Drive, West Lafayette, IN 47907, United States.
Insights
New radiotracers are being developed to improve myocardial perfusion imaging for coronary artery disease (CAD). Research focuses on minimizing liver uptake for clearer heart imaging and earlier diagnosis in patients with suspected CAD.
Area of Science:
- Nuclear Medicine
- Radiochemistry
- Cardiology
Background:
- Coronary artery disease (CAD) is a leading cause of death globally.
- Myocardial ischemia requires prompt detection to prevent irreversible damage, especially in the elderly.
- Current myocardial perfusion imaging agents like (99m)Tc-Sestamibi and (99m)Tc-Tetrofosmin have limitations due to high liver uptake.
Purpose of the Study:
- To review recent research on developing novel (99m)Tc radiotracers with reduced liver uptake for myocardial perfusion imaging.
- To enhance the diagnostic accuracy of coronary artery disease assessment.
- To improve imaging protocols for faster and higher quality cardiac scans.
Main Methods:
- Investigating the use of ether and crown ether-containing chelators to modify cationic (99m)Tc radiotracers.
- Evaluating strategies to minimize liver accumulation of radiotracers.
- Assessing the impact of reduced liver uptake on heart-to-liver ratios and image quality.
Main Results:
- Novel chelators show promise in reducing liver uptake of (99m)Tc radiotracers.
- Faster liver clearance facilitates shorter imaging times (< 30 min post-injection).
- Improved heart/liver ratios enhance the detection of coronary artery disease extent.
Conclusions:
- Minimizing liver uptake in (99m)Tc radiotracers is crucial for improving myocardial perfusion imaging.
- Development of new agents with ether/crown ether chelators offers a promising approach for better CAD diagnosis.
- Optimized radiotracers can significantly benefit patients with suspected coronary artery disease.
Abstract:
Ischemia-related diseases, particularly coronary artery disease (CAD), account for the majority of deaths worldwide. Myocardial ischemia is a serious condition and the delay in reperfusion of ischemic tissues can be life-threatening. This is particular true in the aged population. Rapid and accurate early detection of myocardial ischemia is highly desirable so that various therapeutic regiments can be given before irreversible myocardial damage occurs. Myocardial perfusion imaging with radiotracers is an integral component in evaluations of patients with known or suspected CAD. (99m)Tc-Sestamibi and (99m)Tc-Tetrofosmin are commercial radiopharmaceuticals currently available for myocardial perfusion imaging. Despite their widespread clinical applications, both (99m)Tc-Sestamibi and (99m)Tc-Tetrofosmin do not meet the requirements of an ideal perfusion imaging agent, largely due to their high liver uptake. The intense liver uptake makes it difficult to interpret the heart activity in the inferior and left ventricular wall. Photon scattering from the high liver radioactivity accumulation remains a significant challenge for diagnosis of heart diseases. This review will summarize the most recent research efforts to minimize the liver uptake of cationic (99m)Tc radiotracers by using ether and crown ether-containing chelators. Fast liver clearance will shorten the duration of imaging protocols (< 30 min post-injection), and allow for early acquisition of heart images with high quality. Improvement of heart/liver ratio may permit better detection of the presence and extent of coronary artery disease. Identification of such a new radiotracer that allows for the improved noninvasive assessment of myocardial perfusion would be of considerable benefit in treatment of patients with suspected CAD.
Related Concept Videos
Crown Ethers
Tissue-Drug Binding: Localization of Drugs and its Significance
Drugs can bind to different tissue components, enhancing their distribution and localization. The factors influencing drug localization in tissues include the drug's lipophilicity, structural characteristics, tissue perfusion rate, and pH differences. These factors determine the...
Hepatic Drug Excretion: Enterohepatic Cycling
Post-release drugs and metabolites can be reabsorbed into the body from the intestine. For conjugated metabolites like glucuronides, reabsorption requires enzymatic hydrolysis by intestinal microflora. This...
Drug Distribution: Tissue Binding
For...
Masking and Demasking Agents
There are many masking agents, such as cyanide, fluoride, triethanolamine, thiourea, and 2,3-bis(sulfanyl)propan-1-ol (formerly 2,3-dimercapto-1-propanol), with the masking agent chosen based on the metal...

