The present study examines the effect of pregabalin (previously S-Isobutylg
aba and CI-1008) in two distinct rat models of anxiety. Pregabalin binds wi
th high affinity and selectivity to the alpha (2)delta subunit of voltage d
ependent calcium channels (VDCC). Its corresponding R-enantiomer (R-isobuty
lgaba) is approximately 10 fold weaker. Pregabalin dose-dependently induced
anxiolytic-like effects in both the rat conflict test and elevated X-maze
with respective minimum effective doses (MED) of 3 and 10 mg kg(-1). In con
trast, R-isobutylgaba only showed activity at the highest dose of 100 mg kg
-l in the conflict test. These data indicate that pregabalin may possess cl
inical utility as a novel anxiolytic agent and demonstrates the importance
of the alpha (2)delta subunit of VDCC in the mediation of anxiety related b
ehaviours.