Synthesis and evaluation of p-iodophentermine (IP) as a brain perfusion imaging agent
Recently N-isopropyl-rho-(/sup 123/I)-iodoamphetamine (IMP) has been reported as a potential cerebral perfusion imaging agent for single-photon emission tomography (SPECT). Since addition of a methyl group in the alpha position of amphetamine results in increased lipophilicity and prolonged residence time of the compound in the brain, the authors synthesized and evaluated the biological behaviour of rho-Iodo phenteramine (IP). IP was prepared by diazotization of rho-aminophentermine followed by decomposition of the diazonium salt with KI. Radioiodinated analog was prepared either by the solid-phase isotopic exchange reaction of Mangner et al or by decomposition of the piperidinotrazine derivative with a radiochemical yield of 40-60%. Biodistribution in rats showed that the brain concentration of /sup 131/I-IP was 1.69 +- 0.53, 1.70 +- 0.23 and 1.72 +- 0.11% injected dose/g tissue at 5, 30 and 60 min respectively, after IV injection. The lung uptake was 10.82% ID/g at 5 min and decreased to 7.7% ID/g at 60 min. The thyroid activity was low during the first hour of the study indicating minimal deiodination on the aryl ring. Sequential images of the brains of three dogs after intracarotid injection of /sup 123/I-IP showed localization of activity to one hemisphere of the brain, and clearance of <15% at one hour. In addition, SPECT images revealed more intense localization in the region of gray matter then white matter in the brain.
- Research Organization:
- Massachusetts General Hospital, Boston, MA 02114
- OSTI ID:
- 6477894
- Report Number(s):
- CONF-840619-
- Journal Information:
- J. Nucl. Med.; (United States), Journal Name: J. Nucl. Med.; (United States) Vol. 25:5; ISSN JNMEA
- Country of Publication:
- United States
- Language:
- English
Similar Records
Quantifying regional cerebral blood flow by N-isopropyl-P-[I-123]iodoamphetamine (IMP) using a ring type single-photon emission computed tomography system
Biodistribution of I-123-iodo-amphetamine in man
Related Subjects
550501* -- Metabolism-- Tracer Techniques
550601 -- Medicine-- Unsealed Radionuclides in Diagnostics
59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
AMPHETAMINES
ANALEPTICS
ANIMALS
AUTONOMIC NERVOUS SYSTEM AGENTS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BODY
BRAIN
CENTRAL NERVOUS SYSTEM
CENTRAL NERVOUS SYSTEM AGENTS
CHEMICAL PREPARATION
CHEMICAL REACTIONS
COMPUTERIZED TOMOGRAPHY
DAYS LIVING RADIOISOTOPES
DIAGNOSTIC TECHNIQUES
DISTRIBUTION
DOGS
DRUGS
EMISSION COMPUTED TOMOGRAPHY
EVALUATION
INTERMEDIATE MASS NUCLEI
IODINE 131
IODINE ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
LUNGS
MAMMALS
NERVOUS SYSTEM
NUCLEI
ODD-EVEN NUCLEI
ORGANS
RADIOISOTOPES
RADIONUCLIDE KINETICS
RADIOPHARMACEUTICALS
RATS
RESPIRATORY SYSTEM
RODENTS
SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY
STRUCTURE-ACTIVITY RELATIONSHIPS
SYMPATHOMIMETICS
SYNTHESIS
TISSUE DISTRIBUTION
TOMOGRAPHY
UPTAKE
VERTEBRATES