Pharmaceutical properties, biodistribution, and imaging characteristics of manganese-mesoporphyrin. A potential hepatobiliary contrast agent for magnetic resonance imaging

Invest Radiol. 1993 Oct;28(10):925-32. doi: 10.1097/00004424-199310000-00013.

Abstract

Objectives: Manganese (III) mesoporphyrin (Mn-mesoporphyrin) was investigated for its pharmaceutical properties and magnetic resonance imaging characteristics as a potential hepatobiliary contrast agent.

Methods: Solubility, partition coefficient, plasma binding, proton relaxation enhancement, biodistribution, biliary excretion, liver extraction ratio, and liver enhancement were measured in various in-vitro and in-vivo systems.

Results: Mn-mesoporphyrin was soluble and stable at moderate alkaline pH in phosphate buffer. The octanol/water coefficient was 25.98, and the compound was highly protein bound. R1 for water and plasma were 1.94 and 2.35 L/mmol sec, respectively. R1 in liver was calculated to be 15.72 L/mmol sec. Biodistribution studies in rats and mice confirmed hepatotrophic properties and biliary excretion was 65% over 24 hours. First pass liver uptake was 15%. Magnetic resonance imaging studies showed persistent liver enhancement at 0.05 mmol/kg.

Conclusion: Mn-mesoporphyrin is a lipophilic compound that shows potential as a hepatobiliary magnetic resonance contrast agent.

Publication types

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

MeSH terms

  • Animals
  • Bile / metabolism
  • Biliary Tract / anatomy & histology
  • Colonic Neoplasms / metabolism
  • Contrast Media
  • Female
  • Liver / anatomy & histology
  • Liver / metabolism
  • Magnetic Resonance Imaging*
  • Mesoporphyrins* / pharmacokinetics
  • Mesoporphyrins* / pharmacology
  • Mice
  • Mice, Nude
  • Neoplasm Transplantation
  • Rats
  • Rats, Sprague-Dawley
  • Rats, Wistar
  • Tissue Distribution

Substances

  • Contrast Media
  • Mesoporphyrins
  • manganese mesoporphyrin