New Tc-99m brain imaging agents
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-; TRN: 87-018892
- Journal Information:
- J. Nucl. Med.; (United States), Vol. 25:5; Conference: 31. annual meeting of the Society of Nuclear Medicine, Los Angeles, CA, USA, 5 Jun 1984
- Country of Publication:
- United States
- Language:
- English
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59 BASIC BIOLOGICAL SCIENCES
BRAIN
METABOLISM
SCINTISCANNING
SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY
RADIOPHARMACEUTICALS
EVALUATION
RETENTION FUNCTIONS
TISSUE DISTRIBUTION
UPTAKE
CHEMICAL PREPARATION
LIGANDS
LIQUID COLUMN CHROMATOGRAPHY
MONKEYS
RATS
STRUCTURE-ACTIVITY RELATIONSHIPS
TECHNETIUM 99
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BODY
CENTRAL NERVOUS SYSTEM
CHROMATOGRAPHY
COMPUTERIZED TOMOGRAPHY
COUNTING TECHNIQUES
DIAGNOSTIC TECHNIQUES
DISTRIBUTION
DRUGS
EMISSION COMPUTED TOMOGRAPHY
FUNCTIONS
HOURS LIVING RADIOISOTOPES
INTERMEDIATE MASS NUCLEI
ISOMERIC TRANSITION ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
NERVOUS SYSTEM
NUCLEI
ODD-EVEN NUCLEI
ORGANS
PRIMATES
RADIOISOTOPE SCANNING
RADIOISOTOPES
RODENTS
SEPARATION PROCESSES
SYNTHESIS
TECHNETIUM ISOTOPES
TOMOGRAPHY
VERTEBRATES
YEARS LIVING RADIOISOTOPES
550601* - Medicine- Unsealed Radionuclides in Diagnostics
550501 - Metabolism- Tracer Techniques