Synthesis and biodistribution studies of (I-125)-iodoergoline derivatives

Conference · Wed May 01 04:00:00 EDT 1985 · J. Nucl. Med.; (United States)

OSTI ID:6857633

Mikhail, E A; Basmadjian, G P; Gilliland, D L; Leonard, J C; Magarian, R A; Rieger, J A

The relatively high uptake in rat and dog brains of (Se-75)-Selenopergolide reported earlier, has prompted the synthesis of four new ergoline analogs that can be labeled with I-123. The radioactive iodoergoline derivatives Ia and II were synthesized in a radiochemical yield of 80% and 30% respectively, by refluxing the corresponding 8..beta..-mesyl derivatives with (I-125)-NaI in absolute ethanol. Their chromatographic purification yielded no-carrier added compounds. Ib and Ic were synthesized in a radiochemical yield of 75% and 40% respectively, by refluxing the 8..beta..-(o-iodobenzoyl)- and the 8..beta..-(p-iodobenzenesulfonyl)-lysergol derivatives with (I-125)-NaI. Chromatographic purification yielded compounds with specific activities of --0.3 mCi/mg. Biodistribution studies performed in mature male rats after injection of 2-7 ..mu..Ci of the compounds, showed high uptake of Ia, Ib and II in the brain and adrenals up to 30 min. This data is in agreement with previously studied Se-75 labeled closely related derivatives. Compound II showed, at maximum uptake time, the highest target/non-target ratios. Complete chemical, radiochemical synthesis, and structure biodistribution relationships are presented to support the hypothesis that radiolabeled ergolines could potentially be used as dopamine receptor site mapping agents.

• Research Organization: Nuclear Pharmacy Programs, College of Pharmacy, Univ. of Oklahoma Health Sciences Center, Oklahoma City, OK
• OSTI ID: 6857633
• Report Number(s): CONF-850611-
• Conference Information: Journal Name: J. Nucl. Med.; (United States) Journal Volume: 26:5
• Country of Publication: United States
• Language: English

Related Subjects

38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
400700 -- Radiochemistry & Nuclear Chemistry
550501* -- Metabolism-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ADRENAL GLANDS
ALCOHOLS
ALKALI METAL COMPOUNDS
AMINES
ANIMALS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
BETA DECAY RADIOISOTOPES
BIOLOGICAL MATERIALS
BLOOD
BODY
BODY FLUIDS
BRAIN
CARDIOTONICS
CARDIOVASCULAR AGENTS
CARRIER-FREE ISOTOPES
CENTRAL NERVOUS SYSTEM
CHEMICAL COMPOSITION
CHEMICAL PREPARATION
CHEMICAL REACTION YIELD
CHEMISTRY
CHROMATOGRAPHY
COUNTING TECHNIQUES
DAYS LIVING RADIOISOTOPES
DISTRIBUTION
DOGS
DOPAMINE
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
ENDOCRINE GLANDS
ETHANOL
GLANDS
HALIDES
HALOGEN COMPOUNDS
HYDROXY COMPOUNDS
IMAGE PROCESSING
INJECTION
INORGANIC PHOSPHORS
INTAKE
INTERMEDIATE MASS NUCLEI
IODIDES
IODINE 125
IODINE COMPOUNDS
IODINE ISOTOPES
ISOTOPES
LABELLING
MAMMALS
MATERIALS
MEMBRANE PROTEINS
NERVOUS SYSTEM
NEUROREGULATORS
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANIC SULFUR COMPOUNDS
ORGANS
PHENOLS
PHOSPHORS
POLYPHENOLS
PROCESSING
PROTEINS
PURIFICATION
RADIOCHEMISTRY
RADIOISOTOPE SCANNING
RADIOISOTOPES
RATS
RECEPTORS
RODENTS
SEPARATION PROCESSES
SODIUM COMPOUNDS
SODIUM IODIDES
STRUCTURAL CHEMICAL ANALYSIS
SYMPATHOMIMETICS
SYNTHESIS
TISSUE DISTRIBUTION
UPTAKE
VERTEBRATES
YIELDS