Inactivation of endothelin by polymorphonuclear leukocyte-derived lytic enzymes.

Cultured bovine aortic endothelial cells (BAEC) released endothelin-1 (ET-1) in the culture medium in a time-dependent fashion. Coincubation of fMLP-activated human polymorphonuclear leukocytes (PMN) with BAEC caused a fast (maximal activity was reached within 15 minutes) and cell number-dependent disappearance of ET-1 from the medium. This effect was direct to ET-1, because it was also present when PMN were incubated with the synthetic peptide in the absence of BAEC.

Absorption, disposition, and urinary metabolism of 14C-rifabutin in rats.

14C-rifabutin was given orally (25 mg/kg) and intravenously (i.v.) (10 mg/kg) to female Sprague-Dawley rats.

Disposition of 14C-labelled FCE 22101 in animals.

14C-FCE 22101 was given intravenously to rats (4, 16 and 38 mg/kg), dogs (69 mg/kg), rabbits (99 mg/kg) and monkeys (41 and 99 mg/kg). Radioactivity was eliminated mainly in urine, with faecal excretion being less than 10% in all animal species. Radioactivity as expired 14CO2 was detected in the rat and accounted for less than 0.

Tissue distribution of 14C-indoprofen in the rat.

The tissue distribution of 14C-labelled 2-[p-(1-oxo-2-isoindolinyl)phenyl)propionic acid (indoprofen) after i.v. injection was studied in male and pregnant rats by whole-body autoradiography.

Pharmacokinetics and metabolism of indoprofen in the hamster.

2-[p-(1-Oxo-2-isoindolinyl)phenyl]propionic acid (indoprofen) is rapidly absorbed after oral administration (2 mg/kg) to male and female hamsters. Peak plasma levels of about 12-13 microgram/ml are reached within 1 h of dosing. Plasma concentrations in males and females are similar until 4 h but different at subsequent observation times.