Nuclear medicine: Progress report for quarter ending September 30, 1986

Technical Report · Sun Feb 01 04:00:00 EST 1987

DOI:https://doi.org/10.2172/6941915· OSTI ID:6941915

Knapp, Jr., F. F.; Ambrose, K. R.; Goodman, M. M.; Srivastava, P. C.

The synthesis of two new dimethyl-branched analogues of 15-(p-iodophenyl)-3,3'-dimethylpentadecanoic acid (DMIPP) is described. Methyl-branching was introduced into the 6- and 9-positions to determine the effect of the position of dimethyl-branching on myocardial uptake and clearance kinetics in rats. The goal of these studies is to maximize heart uptake and retention and minimize blood and liver uptake. The 6,6'-dimethyl- (6,6'-DMIPP) and 9.9'-dimethyl- (9,9'-DMIPP) analogues were prepared by multi-step sequences involving successive Friedel-Crafts/Wolf Kishner reactions on thiophene. Regiospecific para-iodination using thallation and treatment with iodide provided the two new analogues. The 9,9'-(I-125)DMIPP was evaluated in rats and showed somewhat lower uptake than 3,3'-DMIPP (3.13 dose/gm at 5 min versus 4.18) and more rapid clearance (approx.30% at 1 h). In addition the heart:blood ratios were lower for the 9,9'-dimethyl isomer. These studies have demonstrated the effects of the position of dimethyl substitution on uptake and retention. 1 ref., 3 figs., 2 tabs.

• Research Organization: Oak Ridge National Lab., TN (USA)
• DOE Contract Number: AC05-84OR21400
• OSTI ID: 6941915
• Report Number(s): ORNL/TM-10294; ON: DE87005288
• Country of Publication: United States
• Language: English

Related Subjects

37 INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY
400201 -- Chemical & Physicochemical Properties
550602* -- Medicine-- External Radiation in Diagnostics-- (1980-)
62 RADIOLOGY AND NUCLEAR MEDICINE
BETA DECAY RADIOISOTOPES
BIOLOGICAL MATERIALS
BLOOD
BODY
BODY FLUIDS
CARBOXYLIC ACIDS
CARDIOVASCULAR SYSTEM
CHEMICAL PREPARATION
CYCLASES
DAYS LIVING RADIOISOTOPES
DIGESTIVE SYSTEM
DISTRIBUTION
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
ELECTROPHORESIS
ENDOCRINE GLANDS
ENZYMES
GLANDS
HEART
IMIDES
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
ISOTOPES
KIDNEYS
LABELLED COMPOUNDS
LIVER
LUNGS
LYASES
MATERIALS
MONOCARBOXYLIC ACIDS
NUCLEI
ODD-EVEN NUCLEI
ORGANIC ACIDS
ORGANIC COMPOUNDS
ORGANIC HALOGEN COMPOUNDS
ORGANIC IODINE COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
RADIOISOTOPES
RADIOPHARMACEUTICALS
RESPIRATORY SYSTEM
STRUCTURE-ACTIVITY RELATIONSHIPS
SYNTHESIS
THYROID
TISSUE DISTRIBUTION