Evaluation of advanced, pathophysiologic new targets for imaging of CNS

Drug Dev Res. 2023 May;84(3):484-513. doi: 10.1002/ddr.22040. Epub 2023 Feb 13.

Abstract

The inadequate information about the in vivo pathological, physiological, and neurological impairments, as well as the absence of in vivo tools for assessing brain penetrance and the efficiency of newly designed drugs, has hampered the development of new techniques for the treatment for variety of new central nervous system (CNS) diseases. The searching sites such as Science Direct and PubMed were used to find out the numerous distinct tracers across 16 CNS targets including tau, synaptic vesicle glycoprotein, the adenosine 2A receptor, the phosphodiesterase enzyme PDE10A, and the purinoceptor, among others. Among the most encouraging are [18 F]FIMX for mGluR imaging, [11 C]Martinostat for Histone deacetylase, [18 F]MNI-444 for adenosine 2A imaging, [11 C]ER176 for translocator protein, and [18 F]MK-6240 for tau imaging. We also reviewed the findings for each tracer's features and potential for application in CNS pathophysiology and therapeutic evaluation investigations, including target specificity, binding efficacy, and pharmacokinetic factors. This review aims to present a current evaluation of modern positron emission tomography tracers for CNS targets, with a focus on recent advances for targets that have newly emerged for imaging in humans.

Keywords: CNS; imaging; neurodegenerative diseases.

Publication types

  • Review
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Brain* / diagnostic imaging
  • Brain* / metabolism
  • Humans
  • Phosphoric Diester Hydrolases / metabolism
  • Positron-Emission Tomography* / methods

Substances

  • Phosphoric Diester Hydrolases
  • PDE10A protein, human