Disposition and metabolism of codorphone in the rat, dog, and man.

The disposition and metabolism of codorphone, 17-cyclopropyl-methyl-4,5 alpha-8 beta-ethyl-3-methoxymorphinan-6-one (I), a new narcotic antagonist, analgesic agent, have been studied in the rat, dog, and man. Rats and dogs were given single 100- and 50-mg/kg po doses, respectively, of I-3H; human volunteers received single 10- to 30-mg doses of unlabeled I po. The compound appeared to be well absorbed in the three species.

Methodology for the identification of the urinary metabolites of the analgesic-narcotic antagonist, codorphone, by gas chromatography mass spectrometry.

Methodology is presented for the identification of codorphone and its metabolites in urine samples using gas chromatography mass spectrometry. The procedure focuses on the clean-up of biological samples and a derivatization technique suitable for these samples. Sep-Pak C-18 cartridges were employed in the clean-up procedure permitting the biological sample to be derivatized in a relatively small volume of reagents.

Influence of broperamole, a new antiinflammatory agent, on gastrointestinal microbleeding in the dog.

59Ferrous sulfate was administered i.v. to 12 male beagles.

Pharmacological study of broperamole, a chemical novel antiinflammatory compound.

N-3[5'-(3"-Bromophenyl)-2'H-tetrazole]propionyl piperidine (broperamole) was shown to elicit potent antiinflammatory activity following systemic administration to rats in acute and subchronic studies. The compound demonstrated systemic antiinflammatory activity 5-6 times that of phenylbutazone. Toical antiinflammatory activity was also demonstrated which was less than that of hydrocortisone but still should have clinical utility.