Human pharmacodynamics of the psychodysleptic 4-bromo-2,5-dimethoxy-phenylisopropylamine labelled with /sup 82/Br
A centrally active psychodysleptic, 4-Bromo-2,5-dimethoxy-phenylisopropylamine (4-Br-DPIA) (1) was synthesized with /sup 82/Br (T/sub 1/2 = 35 hr) at a specific activity of 1 mCi/mg and administered orally or intravenously to 4 human subjects in 6 experiments. The gamma radiation was measured externally in vivo with the Anger Mark II Whole-Body Scanner combined with a Hewlett Packard 5047 A scintigraphic data computer, yielding both whole-body scan photos and digital data for specific organ areas. A whole-body counter was used to measure the biological half life and the solvent extracted urinary metabolites of 4-/sup 82/Br-DPIA. Urinary metabolites were also studied by thin layer chromatography. Organ areas were outlined by light pen on the computer. Digital data analysis showed a striking first-pass accumulation of the intravenously injected compound in the lung. After release from lung, radioactivity accumulated in the liver, with a peak at one hour. Plasma radioactivity reached a broad peak at about two hours, and concentration in the brain reached a maximum at 3 hours, subsequently declining at the same rate as the total body activity.
- Research Organization:
- Univ. of California, Berkeley
- OSTI ID:
- 6312452
- Journal Information:
- IRCS Res. Clin. Pharmacol. Therapeut.; (United States), Journal Name: IRCS Res. Clin. Pharmacol. Therapeut.; (United States) Vol. 2; ISSN IRCTD
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BIOLOGICAL ACCUMULATION
BIOLOGICAL MATERIALS
BIOLOGICAL WASTES
BIOMEDICAL RADIOGRAPHY
BODY
BODY FLUIDS
BRAIN
BROMINE 82
BROMINE ISOTOPES
CENTRAL NERVOUS SYSTEM
CHROMATOGRAPHY
COMPUTERS
COUNTING TECHNIQUES
DAYS LIVING RADIOISOTOPES
DIAGNOSTIC TECHNIQUES
DIGESTIVE SYSTEM
DRUGS
ELECTROMAGNETIC RADIATION
GAMMA RADIATION
GLANDS
IN VIVO
INTERMEDIATE MASS NUCLEI
IONIZING RADIATIONS
ISOTOPES
LABELLED COMPOUNDS
LIVER
LUNGS
MAMMALS
MAN
MEASURING INSTRUMENTS
MEDICINE
METABOLISM
NERVOUS SYSTEM
NUCLEAR MEDICINE
NUCLEI
ODD-ODD NUCLEI
ORGANS
PATIENTS
PRIMATES
RADIATIONS
RADIOACTIVE MATERIALS
RADIOISOTOPE SCANNING
RADIOISOTOPES
RADIOLOGY
RADIONUCLIDE KINETICS
RADIOPHARMACEUTICALS
RESPIRATORY SYSTEM
SEPARATION PROCESSES
THIN-LAYER CHROMATOGRAPHY
URINE
VERTEBRATES
WASTES
WHOLE-BODY COUNTING