A structure-distribution-relationship approach leading to the development of Tc-99m mebrofenin: an improved cholescintigraphic agent
Journal Article
·
· J. Nucl. Med.; (United States)
OSTI ID:5899021
Thirty-three HIDA (hepatobiliary IDA) derivatives were tested and correlations drawn between physicochemical parameters, structural effects, and in vivo characteristics. Capacity factors of the ligands on reverse-phase HPLC were used as a measure of lipophilicity, and to predict protein binding and in vivo distribution of the complexes. Fragmentary pi values were used to derive theoretical lipophilicities, which showed that ortho substituents have reduced lipophilic activity, probably because of self-shielding. Ortho substitution was found to affect hepatocellular transit times. Various combinations of substituents with the desired overall lipophilicity were tested. The best compound, Tc-3-bromo-2,4,6-trimethyl HIDA, possessed high hepatic specificity, and rapid hepatocellular transit; it was also resistant to competition for hepatobiliary excretion from bilirubin.
- Research Organization:
- Squibb Institute for Medical Research, New Brunswick, New Jersey
- OSTI ID:
- 5899021
- Journal Information:
- J. Nucl. Med.; (United States), Journal Name: J. Nucl. Med.; (United States) Vol. 24:5; ISSN JNMEA
- Country of Publication:
- United States
- Language:
- English
Similar Records
Biological distribution and biokinetics of Tc-99m diethyl HIDA and HIDA analogs in humans
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Tc-99m-diethyl-IDA imaging: clinical evaluation in jaundiced patients
Conference
·
Mon Jun 01 00:00:00 EDT 1981
· HHS Publ. (FDA) (U.S.); (United States)
·
OSTI ID:5870165
Clinical comparison of /sup 99m/Tc-diethyl-IDA and /sup 99m/Tc-PIPIDA for evaluation of the hepatobiliary system
Journal Article
·
Mon Dec 31 23:00:00 EST 1979
· Radiology; (United States)
·
OSTI ID:5253614
Tc-99m-diethyl-IDA imaging: clinical evaluation in jaundiced patients
Conference
·
Fri Oct 31 23:00:00 EST 1980
· J. Nucl. Med.; (United States)
·
OSTI ID:6819572
Related Subjects
550201 -- Biochemistry-- Tracer Techniques
550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
ADIPOSE TISSUE
ANIMAL TISSUES
AZOLES
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BILIARY TRACT
BILIRUBIN
BIOCHEMISTRY
BODY
CARBOXYLIC ACIDS
CHEMICAL BONDS
CHEMISTRY
CHROMATOGRAPHY
CONNECTIVE TISSUE
COUNTING TECHNIQUES
DIAGNOSTIC TECHNIQUES
DIGESTIVE SYSTEM
HETEROCYCLIC ACIDS
HETEROCYCLIC COMPOUNDS
HOURS LIVING RADIOISOTOPES
INTERMEDIATE MASS NUCLEI
ISOMERIC NUCLEI
ISOMERIC TRANSITION ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
LIPIDS
LIQUID COLUMN CHROMATOGRAPHY
NUCLEI
ODD-EVEN NUCLEI
ORGANIC ACIDS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
PIGMENTS
PROTEINS
PYRROLES
RADIOISOTOPE SCANNING
RADIOISOTOPES
SCINTISCANNING
SEPARATION PROCESSES
TECHNETIUM 99
TECHNETIUM ISOTOPES
TISSUES
YEARS LIVING RADIOISOTOPES
550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
ADIPOSE TISSUE
ANIMAL TISSUES
AZOLES
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BILIARY TRACT
BILIRUBIN
BIOCHEMISTRY
BODY
CARBOXYLIC ACIDS
CHEMICAL BONDS
CHEMISTRY
CHROMATOGRAPHY
CONNECTIVE TISSUE
COUNTING TECHNIQUES
DIAGNOSTIC TECHNIQUES
DIGESTIVE SYSTEM
HETEROCYCLIC ACIDS
HETEROCYCLIC COMPOUNDS
HOURS LIVING RADIOISOTOPES
INTERMEDIATE MASS NUCLEI
ISOMERIC NUCLEI
ISOMERIC TRANSITION ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
LIPIDS
LIQUID COLUMN CHROMATOGRAPHY
NUCLEI
ODD-EVEN NUCLEI
ORGANIC ACIDS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
PIGMENTS
PROTEINS
PYRROLES
RADIOISOTOPE SCANNING
RADIOISOTOPES
SCINTISCANNING
SEPARATION PROCESSES
TECHNETIUM 99
TECHNETIUM ISOTOPES
TISSUES
YEARS LIVING RADIOISOTOPES