Abstract

The advent of preclinical research scanners for in vivo imaging of small animals has added confidence into the multi-step decision-making process of radiotracer discovery and development. Furthermore, it has expanded the utility of imaging techniques available to dissect clinical questions, fostering a cyclic interaction between the clinical and the preclinical worlds. Significant efforts from medicinal chemistry have also made available several high-affinity and selective compounds amenable for radiolabeling, that target different receptors, transporters and enzymes in vivo. This substantially increased the range of applications of molecular imaging using positron emission tomography (PET) or single photon emission computed tomography (SPECT). However, the process of developing novel radiotracers for in vivo imaging of the human brain is a multi-step process that has several inherent pitfalls and technical difficulties, which often hampers the successful translation of novel imaging agents from preclinical research into clinical use. In this paper, the process of radiotracer development and its relevance in brain research is discussed; as well as, its pitfalls, technical challenges and future promises. Examples of successful and unsuccessful translation of brain radiotracers will be presented.

Highlights

  • Single photon emission computed tomography (SPECT) and positron emission tomography (PET) rely on the in vivo detection and quantification of the radiotracer distribution and binding to a specific biological target in the living body (Salvadori, 2008)

  • In the basic research context, which accounts for the majority of these PET and SPECT imaging, the utility of a radiotracer can be difficult to anticipate

  • This is especially true as the physical limits of PET and SPECT detection are approached in the clinical setting as they have been approached in the preclinical setting (Mariani et al, 2008; Seo et al, 2008; Ruth, 2009)

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Summary

Introduction

Single photon emission computed tomography (SPECT) and positron emission tomography (PET) rely on the in vivo detection and quantification of the radiotracer distribution and binding to a specific biological target in the living body (Salvadori, 2008). These techniques are at the leading edge of molecular imaging and allow for exceptional target specificity and high sensitivity (Haberkorn and Eisenhurt, 2005; Salvadori, 2008; Kemp et al, 2010). PET and SPECT imaging can assist in diagnosing multiple neurodegenerative and neuropsychiatric disorders.

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