ABSORPTION OF THE NEW ANXIOLYTIC COMPOUND DERAMCICLANE IN RATS, DOGS AND RABBITS

The absorption of deramciclane fumarate )-N,N-dimethyl-2-[(1,7,7-trime thyl-2-phenylbicyclo [2,2,1] hept-2-yl) oxy] ethane amine-2-(E)-butene dioate (1:1), CAS 120444-78-8, EGIS-3886), a new anxiolytic compound, was studied in rats, dogs and rabbits by using H-camphor-or C-14-pheny l-labelled radioisomers of the substance. The compound was readily abs orbed from the intestinal tract after oral administration. The absorpt ion of C-14-deramciclane was also studied from the isolated intestinal loops of rats (duodenal, jejunal, ileal loops) and dogs (duodenal loo p). The absorption was faster in rats and rabbits than in dogs (t(max) = 1 h or 6 h, respectively). The radioactivity was not absorbed from the isolated stomach of any species studied for 2 h. Meanwhile, the su bstance was not decomposed by the gastric juice, as it has been proved by TLC and MS analyses. Deramciclane is preferentially excreted via t he bile. The intensity of its bile excretion is higher in rats than in dogs. Higher plasma levels of labelled deramciclane were found in fem ale than in male rats.