Comparison of the metabolism and pharmacokinetics of metbufen and itanoxone and their analogues in rats.

Metbufen, II, itanoxone, I, and two other derivatives of gamma-aryl-gamma-keto-substituted butyric acids labelled with 14C in their carbonyl group were synthesized for a metabolic investigation in rats. Profound changes in pharmacokinetic parameters, most specifically in the distribution, elimination, and metabolic pathways, were induced by substitution in the aromatic nucleus or changes in saturation of the aliphatic chain. The metabolites isolated from plasma and urine were identified by gas chromatography and mass spectrometry, by comparison with chemical controls, revealing the processes of metabolism of these structural analogues.

1-Aryl-2-(aminomethyl)cyclopropanecarboxylic acid derivatives. A new series of potential antidepressants.

A series of 1-aryl-2-(aminomethyl)cyclopropanecarboxylic acid derivatives were synthesized and evaluated as potential antidepressants. Compounds with the Z configuration were synthesized from 1-aryl-2-oxo-3-oxabicyclo[3.1.

Intestinal calcium absorption in the rat after oral Tween 80 administration.

Calcium absorption into rat intestine was investigated in vitro and in vivo after oral administration of Tween 80 (Polyoxyethylene (20) sorbitan monooleate). The in vivo study showed a significant decrease in serum calcium and in the quantity of calcium excreted by the intestine. In vitro, measurement of calcium influx into slices of intestine taken from Tween 80 treated animals showed that passive calcium diffusion was unchanged and that a decrease in the active transport alone is responsible for reduction in total calcium influx.