Synthesis and biodistribution of neutral lipid-soluble Tc-99m complexes that cross the blood-brain barrier. [Monkeys]
Three Tc-99m-labeled neutral 1,2-dithia-5,8-diazacyclodecane (BAT) chelates that are capable of crossing the blood-brain barrier (BBB) were prepared and evaluated. Biodistribution (i.v.) in rats showed a significant brain uptake (1-3%/whole brain) at 2 min. At 15 min the uptake dropped to about a tenth of the original level, indicating free passage in both directions across the BBB. Gamma camera images of a monkey confirmed the high initial brain uptake. This group of Tc-99m BAT compounds clearly exhibited in vivo stability and the ability to cross the BBB after an i.v. injection. Derivatives containing tertiary amine groups should have prolonged brain retention and might be suitable for SPECT studies of brain perfusion.
- Research Organization:
- SUNY, Buffalo, NY
- OSTI ID:
- 5031871
- Journal Information:
- J. Nucl. Med.; (United States), Vol. 25:3
- Country of Publication:
- United States
- Language:
- English
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62 RADIOLOGY AND NUCLEAR MEDICINE
BRAIN
RADIONUCLIDE KINETICS
RADIOPHARMACEUTICALS
CHEMICAL PREPARATION
TISSUE DISTRIBUTION
TECHNETIUM 99
AUTORADIOGRAPHY
BLOOD-BRAIN BARRIER
CHELATING AGENTS
CYCLOALKANES
ISOMERIC NUCLEI
MONKEYS
ALKANES
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BODY
CENTRAL NERVOUS SYSTEM
DISTRIBUTION
DRUGS
HOURS LIVING RADIOISOTOPES
HYDROCARBONS
INTERMEDIATE MASS NUCLEI
ISOMERIC TRANSITION ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
NERVOUS SYSTEM
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
PRIMATES
RADIOISOTOPES
SYNTHESIS
TECHNETIUM ISOTOPES
VERTEBRATES
YEARS LIVING RADIOISOTOPES
400702* - Radiochemistry & Nuclear Chemistry- Properties of Radioactive Materials
550601 - Medicine- Unsealed Radionuclides in Diagnostics