Radioiodinated benzodiazepines: agents for mapping glial tumors

Journal Article · Tue Nov 01 04:00:00 EST 1988 · J. Med. Chem.; (United States)

DOI:https://doi.org/10.1021/jm00119a005· OSTI ID:6601690

Van Dort, M E; Ciliax, B J; Gildersleeve, D L; Sherman, P S; Rosenspire, K C; Young, A B; Junck, L; Wieland, D M

Two isomeric iodinated analogues of the peripheral benzodiazepine binding site (PBS) ligand Ro5-4864 have been synthesized and labeled in high specific activity with iodine-125. Competitive binding assays conducted with the unlabeled analogues indicate high affinity for PBS. Tissue biodistribution studies in rats with these /sup 125/I-labeled ligands indicate high uptake of radioactivity in the adrenals, heart, and kidney--tissues known to have high concentrations of PBS. Preadministration of the potent PBS antagonist PK 11195 blocked in vivo uptake in adrenal tissue by over 75%, but to a lesser degree in other normal tissues. In vivo binding autoradiography in brain conducted in C6 glioma bearing rats showed dense, PBS-mediated accumulation of radioactivity in the tumor. Ligand 6 labeled with /sup 123/I may have potential for scintigraphic localization of intracranial glioma.

• Research Organization: Univ. of Michigan Medical Center, Ann Arbor (USA)
• OSTI ID: 6601690
• Journal Information: J. Med. Chem.; (United States), Journal Name: J. Med. Chem.; (United States) Vol. 31:11; ISSN JMCMA
• Country of Publication: United States
• Language: English

Related Subjects

550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
AUTORADIOGRAPHY
BETA DECAY RADIOISOTOPES
BODY
BRAIN
CENTRAL NERVOUS SYSTEM
CENTRAL NERVOUS SYSTEM AGENTS
CHEMICAL PREPARATION
COUNTING TECHNIQUES
DAYS LIVING RADIOISOTOPES
DIAGNOSIS
DIAGNOSTIC TECHNIQUES
DISEASES
DISTRIBUTION
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
GLIOMAS
HOURS LIVING RADIOISOTOPES
INTERMEDIATE MASS NUCLEI
IODINE 123
IODINE 125
IODINE ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
LIGANDS
MAMMALS
MEMBRANE PROTEINS
NEOPLASMS
NERVOUS SYSTEM
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
PROTEINS
PSYCHOTROPIC DRUGS
RADIOISOTOPE SCANNING
RADIOISOTOPES
RADIOPHARMACEUTICALS
RATS
RECEPTORS
RODENTS
SCINTISCANNING
SYNTHESIS
TISSUE DISTRIBUTION
TRANQUILIZERS
VERTEBRATES