Preparation and evaluation of radioiodinated 1-(dialkyl-aminoalkyl)-4-phenylpiperazines as potential brain imaging agents
The interest in radioiodinated diamines stems from their similarity to /sup 125/I-HIPDM and to the 1-dialkvlamino-acyl-4-phenylpiperazines that the authors have previously examined as potential brain imaging agents. In this study they converted the 1-(dialkylaminoacyl)-4-phenylpiperazines to their corresponding 1-(dialkylaminoacyl) analogs via reduction with diborane in THF. Radioiodination at the no-carrier-added level with Na/sup 125/I and chloramine-T gave the final compounds, after chromatographic separation, in 30-50% yields. The tissue distributions were determined in rats at 0.25, and 4 hrs after an i.v. injection of the radiochemical. The results indicated that all of the agents were readily extracted by the brain (1.5-2.5% ID) with brain to blood ratios >20. The structure-distribution relationships for this series were, however, decidedly different from the aminoacyl compounds in that morpholino-derivatives had better uptake and retention than the piperidine derivatives. Neither extension of the alkyl chain nor the presence of carrier significantly altered the brain uptake and retention of the radiochemical. Further studies are in progress. In conclusion, they have identified a class of radiotracers that can be readily prepared and show a pattern of brain uptake and retention than the structurally similar 1-dialkylaminoacyl-4-phenylpiperazines.
- Research Organization:
- College of Pharmacy, Northeastern Univ., Boston, MA 02115
- OSTI ID:
- 7030629
- Report Number(s):
- CONF-850611-; TRN: 87-010790
- Journal Information:
- J. Nucl. Med.; (United States), Vol. 26:5; Conference: 32. annual meeting of the Society of Nuclear Medicine, Houston, TX, USA, 2 Jun 1985
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
BRAIN
RADIOISOTOPE SCANNING
IODINE 125
RADIOCHEMISTRY
MORPHOLINES
IODINATION
RETENTION
STRUCTURE-ACTIVITY RELATIONSHIPS
TISSUE DISTRIBUTION
UPTAKE
PIPERAZINES
ACYL RADICALS
ALKYL RADICALS
AMINES
BLOOD
BLOOD-BRAIN BARRIER
CARRIERS
CHEMICAL PREPARATION
CHLORAMINES
CHROMATOGRAPHY
DERIVATIZATION
EVALUATION
PHENYL RADICALS
RATS
SODIUM IODIDES
TRACER TECHNIQUES
ALKALI METAL COMPOUNDS
ANIMALS
ARYL RADICALS
AZINES
BETA DECAY RADIOISOTOPES
BIOLOGICAL MATERIALS
BODY
BODY FLUIDS
CENTRAL NERVOUS SYSTEM
CHEMICAL REACTIONS
CHEMISTRY
COUNTING TECHNIQUES
DAYS LIVING RADIOISOTOPES
DISTRIBUTION
ELECTRON CAPTURE RADIOISOTOPES
ETHERS
HALIDES
HALOGEN COMPOUNDS
HALOGENATION
HETEROCYCLIC COMPOUNDS
INORGANIC PHOSPHORS
INTERMEDIATE MASS NUCLEI
IODIDES
IODINE COMPOUNDS
IODINE ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
MAMMALS
MATERIALS
NERVOUS SYSTEM
NUCLEI
ODD-EVEN NUCLEI
ORGANIC CHLORINE COMPOUNDS
ORGANIC COMPOUNDS
ORGANIC HALOGEN COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANIC OXYGEN COMPOUNDS
ORGANS
PHOSPHORS
PYRAZINES
RADICALS
RADIOISOTOPES
RODENTS
SEPARATION PROCESSES
SODIUM COMPOUNDS
SYNTHESIS
VERTEBRATES
550601* - Medicine- Unsealed Radionuclides in Diagnostics
400700 - Radiochemistry & Nuclear Chemistry