I. Hazai et al., Whole-body autoradiography and quantitative organ-level distribution studyof deramciclane in rats, J PHARM PHA, 51(2), 1999, pp. 165-174
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.