Mn(II)-Based MRI Contrast Agent Candidate for Vascular Imaging

J Med Chem. 2020 Jun 11;63(11):6057-6065. doi: 10.1021/acs.jmedchem.0c00197. Epub 2020 May 21.

Abstract

Toxicity concerns related to Gd(III)-based magnetic resonance imaging (MRI) agents prompted an intensive research toward their replacement by complexes of essential metal ions, like Mn(II). Here, we report a macrocyclic chelate, [Mn(PC2A-BP)], which possesses high thermodynamic stability (log KMnL = 14.86 and pMn=8.35) and kinetic inertness (t1/2pH=7.4 = 286.2 h) as well as as remarkable relaxivity (r1p = 23.5 mM-1 s-1, 0.49 T, 37 °C) in the presence of human serum albumin, allowing a significant MRI signal intensity increase in the vasculature even at low dose (25 μmol/kg) of the complex.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Contrast Media / chemistry*
  • Coordination Complexes / chemistry
  • Drug Stability
  • Humans
  • Kinetics
  • Ligands
  • Magnetic Resonance Imaging / methods*
  • Manganese / chemistry*
  • Serum Albumin / chemistry
  • Thermodynamics

Substances

  • Contrast Media
  • Coordination Complexes
  • Ligands
  • Serum Albumin
  • Manganese