Feasibility of myocardial PET imaging using a benzylguanidine analog: meta-(3-[18F]fluoropropyl)benzylguanidine ([18F]mFPBG)

Nucl Med Biol. 2018 Jun:61:63-70. doi: 10.1016/j.nucmedbio.2018.04.005. Epub 2018 May 3.

Abstract

Introduction: Global and regional sympathetic activity in the heart can be evaluated using [123I]meta-iodobenzylguanidine ([123I]mIBG) imaging. However, [123I]mIBG is associated with low image spatial resolution and sensitivity in cardiac imaging. We investigated the capability of an F-18-labeled mIBG derivative, meta-(3-[18F]fluoropropyl)benzylguanidine ([18F]mFPBG), for identifying ischemic and viable myocardium in a rat model of myocardial infarction.

Materials and methods: The ex vivo biodistribution and in vivo metabolic stability of [18F]mFPBG were investigated in Sprague-Dawley rats. Selective cardiac adrenergic activation was confirmed via a blocking experiment involving pretreatment with desipramine (2 mg kg-1), followed by the administration of [18F]mFPBG. Imaging properties of [18F]mFPBG were compared with those of traditional cardiac imaging radiotracers ([123I]mIBG and [99mTc]MIBI) in a rat model of myocardial infarction. Non-invasive image-based measurements of infarct sizes were then compared with histological findings by using Bland-Altman analysis.

Results: The differences in infarct sizes determined using histological analysis and [18F]mFPBG PET were -2.55 ± 4.99% (range: -12.33 to 7.22), -2.35 ± 3.32% (range: -8.87 to 4.16), and -3.15 ± 6.16% (range: -15.24 to 8.93) at 5, 20, and 40 min, respectively. Furthermore, [18F]mFPBG PET was superior to traditional imaging methods in assessing the degree of ischemia in areas of myocardial infarction, as well as the actual infarct size.

Conclusion: Compared to [123I]mIBG, [18F]mFPBG showed improved spatial resolution and sensitivity in a rat model of myocardial infarction. This result suggested that [18F]mFPBG is a promising cardiac PET imaging agent for potential diagnostic application in PET cardiology.

Keywords: (18)F; Cardiac sympathetic innervation; Guanidine; Myocardial infarction; PET.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Feasibility Studies
  • Fluorine Radioisotopes / chemistry*
  • Fluorine Radioisotopes / metabolism
  • Fluorine Radioisotopes / pharmacokinetics
  • Guanidines / chemistry*
  • Guanidines / metabolism
  • Guanidines / pharmacokinetics
  • Heart / diagnostic imaging*
  • Heart / innervation
  • Male
  • Positron-Emission Tomography / methods*
  • Rats
  • Rats, Sprague-Dawley
  • Sympathetic Nervous System / diagnostic imaging
  • Sympathetic Nervous System / physiology
  • Tissue Distribution
  • Tomography, Emission-Computed, Single-Photon

Substances

  • Fluorine Radioisotopes
  • Guanidines
  • benzylguanidine