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.
Manning
H Charles
HC
Department of Chemistry and Biochemistry, Texas Tech University, Lubbock, Texas 79409, USA.
Goebel
Timothy
T
Marx
John N
JN
Bornhop
Darryl J
DJ
D001381:Azepines / Q000138:chemical synthesis*; D002614:Chelating Agents / Q000138:chemical synthesis* / Q000737:chemistry; D003287:Contrast Media / Q000138:chemical synthesis*; D005456:Fluorescent Dyes; D028581:Lanthanoid Series Elements / Q000737:chemistry*; D008024:Ligands; D008279:Magnetic Resonance Imaging; D011963:Receptors, GABA-A / Q000378:metabolism*
D001381:Azepines; D002614:Chelating Agents; D003287:Contrast Media; D005456:Fluorescent Dyes; D028581:Lanthanoid Series Elements; D008024:Ligands; C454621:QM-CTMC-PK11195; D011963:Receptors, GABA-A