New Tc-99m brain imaging agents

Conference · Sun Jan 01 04:00:00 EST 1984 · J. Nucl. Med.; (United States)

OSTI ID:6575341

Kung, H F; Yu, C C; Billings, J; Molnar, M; Wicks, R; Blau, M

In developing new Tc-99m brain perfusion imaging agents for SPECT, a series of BAT (bis-aminoethanethiol) derivatives was prepared. These N/sub 2/S/sub 2/ ligands formed stable and neutral complexes with reduced Tc-99m, either by Sn(II)-PPi or sodium borohydride reduction. The purity of the Tc-99m complexes was >95% (HPLC reverse-phase column, acetonitrile: pH 7.0 buffer, 85:15). The biodistribution in rats was evaluated using I-125 iodoantipyrine (IAP), a free diffusible tracer, as the internal reference. Compounds with a free hydroxyl group (I and IV) showed lower brain uptake, inspite of high P.C.; this may be related to in vivo instability of the complexes. High initial brain uptake was observed for three compounds (II, III and V), however, only compound V (P.C.=384) showed significant brain retention. Planar imaging with compound V in a monkey demonstrated that the compound localized in brain and the retention time was T/sub 1/2/=35 min. Compounds of this type may be useful as brain imaging agent in themself or as a basis for further structural modification to improve brain uptake and retention.

• Research Organization: SUNY Buffalo, Buffalo, NY
• OSTI ID: 6575341
• Report Number(s): CONF-840619-
• Conference Information: Journal Name: J. Nucl. Med.; (United States) Journal Volume: 25:5
• Country of Publication: United States
• Language: English

Related Subjects

550501 -- Metabolism-- Tracer Techniques
550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BODY
BRAIN
CENTRAL NERVOUS SYSTEM
CHEMICAL PREPARATION
CHROMATOGRAPHY
COMPUTERIZED TOMOGRAPHY
COUNTING TECHNIQUES
DIAGNOSTIC TECHNIQUES
DISTRIBUTION
DRUGS
EMISSION COMPUTED TOMOGRAPHY
EVALUATION
FUNCTIONS
HOURS LIVING RADIOISOTOPES
INTERMEDIATE MASS NUCLEI
ISOMERIC TRANSITION ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
LIGANDS
LIQUID COLUMN CHROMATOGRAPHY
MAMMALS
METABOLISM
MONKEYS
NERVOUS SYSTEM
NUCLEI
ODD-EVEN NUCLEI
ORGANS
PRIMATES
RADIOISOTOPE SCANNING
RADIOISOTOPES
RADIOPHARMACEUTICALS
RATS
RETENTION FUNCTIONS
RODENTS
SCINTISCANNING
SEPARATION PROCESSES
SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY
STRUCTURE-ACTIVITY RELATIONSHIPS
SYNTHESIS
TECHNETIUM 99
TECHNETIUM ISOTOPES
TISSUE DISTRIBUTION
TOMOGRAPHY
UPTAKE
VERTEBRATES
YEARS LIVING RADIOISOTOPES