Facile, efficient conjugation of a trifunctional lanthanide chelate to a peripheral benzodiazepine receptor ligand.

[reaction: see text] Receptor-mediated imaging and therapy of diseased tissue is rapidly gaining favor in the medical community. The synthesis and facile aqueous/organic coupling of a peripheral-type benzodiazepine receptor ligand to a cyclen-based fluorophore is described herein. The contrast agent QM-CTMC-PK11195, when chelated with lanthanides, produces bright luminescence and good MRI contrast and can potentially serve as an imaging and demarcation agent for certain types of cancers.
AuthorsH Charles Manning, Timothy Goebel, John N Marx, Darryl J Bornhop
JournalOrganic letters (Org Lett) Vol. 4 Issue 7 Pg. 1075-8 (Apr 04 2002) ISSN: 1523-7060 [Print] United States
PMID11922786 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Azepines
  • Chelating Agents
  • Contrast Media
  • Fluorescent Dyes
  • Lanthanoid Series Elements
  • Ligands
  • QM-CTMC-PK11195
  • Receptors, GABA-A
  • Azepines (chemical synthesis)
  • Chelating Agents (chemical synthesis, chemistry)
  • Contrast Media (chemical synthesis)
  • Fluorescent Dyes
  • Lanthanoid Series Elements (chemistry)
  • Ligands
  • Magnetic Resonance Imaging
  • Receptors, GABA-A (metabolism)

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