Whole-body autoradiography and quantitative organ-level distribution studyof deramciclane in rats

The distribution of H-3-labelled deramciclane (EGIS-3886), a new 5-HT2 anta gonist with anxiolytic activity, has been investigated by whole-body autora diography and quantitative organ-level determination after intravenous and oral administration to male and female rats at a dose of 3 mg kg(-1). Pregn ant dams were also studied, but by autoradiography only. In the autoradiogr aphic study 32 organs were investigated, while in the quantitative organ-le vel study the radioactivity in 15 organs were determined. There are no sex differences in the distribution of deramciclane, absorptio n is rapid, elimination is comparatively fast, no specific organ is targete d, and the accumulation of the compound is very unlikely. Penetration of th e blood-brain barrier was complete and extremely fast, a very important fea ture of a potential anxiolytic drug. There is no penetration of the foetus in pregnant dams. The study demonstrated that deramciclane has advantageous pharmacokinetic p roperties in rats.