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Synthesis and radioiodination of ergoline derivatives: potential in-vivo dopamine receptor site mapping radiopharmaceuticals

Thesis/Dissertation ·
OSTI ID:5886855
The need of a dopamine-receptor based radiopharmaceutical for brain imaging is apparent. If such an agent is made available to physicians, it could provide means for detecting brain tumors, and diagnose such mental disorders as parkinsonism, schizophrenia and psychosis. Currently, such agents are yet to be discovered. Procedures were developed to synthesize and label four ergoline derivatives which could potentially exhibit affinity to dopamine receptors. Labelling with /sup 125/I was accomplished in some cases by displacing a suitably positioned leaving group with /sup 125/I-anion, while in other cases iodine exchange procedures were utilized. Formulations of the labeled derivatives were achieved via the formation of their water soluble tartarate salts. Biodistribution studies in mature Sprague-Dawley rats showed that of the four radioactive compounds injected, the highest uptake in the brain and adrenals was achieved with 8 ..beta..-(I-125)-iodomethyl-6-propylergoline. In addition, high target/nontarget ratios were obtained with the above mentioned compound. On the other hand, the least brain and adrenal uptake as well as the lowest target/nontarget ratios were exhibited by 8 ..beta..-(I-125)-(p-iodobenzenesulfonyl)-lysergol presumably due to its in-vivo instability. A comparative biodistribution study for ergoline derivatives and N-isopropyl-(I-123)-p-iodoamphetamine was conducted. The biodistribution studies showed that the brain to blood ratio for the ergoline derivative 8 ..beta..-(I-125)-iodomethyl-6-propylergoline to be very close to that for /sup 125/I-IMP at 1 minute after dose administration. However after 15 minutes the brain/blood ratio of compound XLVI was half the value of /sup 123/I-IMP. Different mechanisms of brain influx and efflux are known to occur with the amphetamine and ergoline derivatives.
Research Organization:
Oklahoma Univ., Oklahoma City (USA). Medical Center
OSTI ID:
5886855
Country of Publication:
United States
Language:
English

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Related Subjects

550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
62 RADIOLOGY AND NUCLEAR MEDICINE
ADRENAL GLANDS
ANIMALS
BETA DECAY RADIOISOTOPES
BODY
BRAIN
CENTRAL NERVOUS SYSTEM
COUNTING TECHNIQUES
DAYS LIVING RADIOISOTOPES
DIAGNOSTIC TECHNIQUES
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
ENDOCRINE GLANDS
GLANDS
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
NERVOUS SYSTEM
NUCLEI
ODD-EVEN NUCLEI
ORGANS
RADIOISOTOPE SCANNING
RADIOISOTOPES
RADIOPHARMACEUTICALS
RATS
RODENTS
SCINTISCANNING
UPTAKE
VERTEBRATES