Design of site specific radiopharmaceuticals for tumor imaging. (Parts I and II)

Thesis/Dissertation · Sat Jan 01 00:00:00 EST 1983

OSTI ID:5817010

Van Dort, M E

Part I. Synthetic methods were developed for the preparation of several iodinated benzoic acid hydrazides as labeling moieties for indirect tagging of carbonyl-containing bio-molecules and potential tumor-imaging agents. Biodistribution studies conducted in mice on the derivatives having the I-125 label ortho to a phenolic OH demonstrated a rapid in vivo deiodination. Part II. The reported high melanin binding affinity of quinoline and other heterocyclic antimalarial drugs led to the development of many analogues of such molecules as potential melanoma-imaging agents. Once such analogue iodochloroquine does exhibit high melanin binding, but has found limited clinical use due to appreciable accumulation in non-target tissues such as the adrenal cortex and inner ear. This project developed a new series of candidate melanoma imaging agents which would be easier to radio-label, could yield higher specific activity product, and which might demonstrate more favorable pharmacokinetic and dosimetric characteristics compared to iodochloroquine.

• Research Organization: Lehigh Univ., Bethlehem, PA (USA)
• OSTI ID: 5817010
• Resource Relation: Other Information: Thesis (Ph. D.)
• Country of Publication: United States
• Language: English

Related Subjects

38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
62 RADIOLOGY AND NUCLEAR MEDICINE
IODINE ISOTOPES
TISSUE DISTRIBUTION
RADIOPHARMACEUTICALS
CHEMICAL PREPARATION
BRAIN
MICE
NEOPLASMS
RADIOISOTOPE SCANNING
ANIMALS
BODY
CENTRAL NERVOUS SYSTEM
COUNTING TECHNIQUES
DISEASES
DISTRIBUTION
DRUGS
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
NERVOUS SYSTEM
ORGANS
RODENTS
SYNTHESIS
VERTEBRATES
400702* - Radiochemistry & Nuclear Chemistry- Properties of Radioactive Materials
550601 - Medicine- Unsealed Radionuclides in Diagnostics