Disposition and metabolism of prinomide in laboratory animals

Thesis/Dissertation · Wed Dec 31 23:00:00 EST 1986

OSTI ID:5989923

Egger, H

The disposition and metabolism of prinomide, the 1:1 triethanolamine salt of 1-methyl-..beta..-oxo-..cap alpha.. (phenylcarbamoyl)-2-pyrrole-propionitrile (CGS 10787B), have been investigated in a number of animal species after single and multiple oral dosing with /sup 14/C-labeled and unlabeled drug. Following single oral doses of 25 to 50 mg/kg of /sup 14/C-prinomide to mice, rats, hamsters, dogs, cynomolgus monkeys and baboons, radioactivity was excreted primarily in urine, in the form of metabolites. However, in the mouse and monkey, fecal excretion was also significant. In the cynomolgus monkey, a radioactive dose of drug administered following multiple doses of unlabeled drug gave rise to peak plasma concentrations of radioactivity within 1 to 6 hr. Intact prinomide accounted for approximately 69% of this radioactivity. The terminal plasma half-life of the drug was 24 to 41 hr. Studies in rats with /sup 14/C-prinomide indicated that radioactivity was distributed rapidly to all tissues, with the highest levels being observed in blood and well perfused organs and tissues. The lowest levels were detected in adipose tissue, eyes, and brain. The metabolism of prinomide was qualitatively similar in all species investigated.

• Research Organization: Saint John's Univ., Jamaica, NY (USA)
• OSTI ID: 5989923
• Country of Publication: United States
• Language: English

Related Subjects

550501* -- Metabolism-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ANIMALS
BABOONS
BIOLOGICAL HALF-LIFE
CARBON 14 COMPOUNDS
DISTRIBUTION
DOGS
HAMSTERS
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
MAMMALS
METABOLISM
MICE
MONKEYS
NITRILES
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
PRIMATES
PROPIOLONITRILE
RATS
RODENTS
SALTS
TISSUE DISTRIBUTION
TRACER TECHNIQUES
VERTEBRATES