Sulfonyl-Containing Boronate Caps for Optimization of Biological Properties of 99m Tc(III) Radiotracers [ 99m TcCl(CDO)(CDOH) 2 B-R] (CDOH 2 = Cyclohexanedione Dioxime)

J Med Chem. 2018 Jan 11;61(1):319-328. doi: 10.1021/acs.jmedchem.7b01412. Epub 2017 Dec 27.

Abstract

In this study, different boronate caps were used to optimize biodistribution properties of radiotracers [99mTcCl(CDO)(CDOH)2B-R] (1, R = 3S; 2, R = 3SP; 3, R = 3MS; 4, R = 3DMS; 5, R = 3MSB; 6, R = 3MMS; 7, R = 3MSA; 8, R = 3DMSA; 9, R = 4S; 10, R = 4MS; 11, R = 4MSB). Among the 11 new 99mTc radiotracers, 2 shows the most promising characteristics of an optimal heart imaging agent. Its initial heart uptake is close to that of 99mTc-Teboroxime, but its heart retention time is significantly longer. Its heart/liver, heart/lung, and heart/muscle ratios are also better than those of 99mTc-Teboroxime. The SPECT image quality with 2 in SD rats is better than that with 99mTc-Teboroxime. The high initial heart uptake, long heart retention, and high heart/background ratios make 2 an excellent SPECT radiotracer for MPI.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Biological Transport
  • Boronic Acids / chemistry*
  • Kinetics
  • Models, Molecular
  • Molecular Conformation
  • Myocardium / metabolism
  • Organotechnetium Compounds / chemistry*
  • Organotechnetium Compounds / metabolism*
  • Organotechnetium Compounds / pharmacokinetics
  • Oximes / chemistry*
  • Radioactive Tracers
  • Rats
  • Single Photon Emission Computed Tomography Computed Tomography
  • Swine
  • Tissue Distribution

Substances

  • Boronic Acids
  • Organotechnetium Compounds
  • Oximes
  • Radioactive Tracers