Abecarnil is a metabolically stable beta-carboline that binds with hig
h affinity and selectivity to central benzodiazepine receptors. The ef
fects on cognitive and psychomotor skills of abecarnil (ZK 112-119), 2
.5 mg and 5.0 mg, were compared with lorazepam 2.0 mg and placebo. Twe
nty-four healthy, young males participated in a double-blind, four-way
Latin square design and performed batteries of behavioral tests at pr
edrug and at 20, 40, 60, 80, 100, 120, 180, 240, 360 and 480 min after
drug administration. Abecarnil 5.0 mg and lorazepam 2.0 mg displayed
similar impairment profiles in tests of cognitive functions including
memory encoding. Abecarnil 2.5 mg was substantially less impairing tha
n lorazepam. Impairment levels of the abecarnil and lorazepam treatmen
ts peaked at 2-3 h after oral administration. The two abecarnil doses
showed dose-dependent effects on the cognitive and psychomotor tasks.
All three drug treatments were well tolerated by the subjects, with no
one terminating early due to adverse events. The incidence of reporte
d adverse events for abecarnil was dose-dependent. The most frequent,
statistically significant adverse effects were drowsiness, lack of con
centration and visual disturbance for abecarnil 5.0 mg; and lack of co
ncentration and dizziness for lorazepam 2.0 mg. There were no signific
ant differences in adverse incidence rates between abecarnil 2.5 mg an
d placebo.