The present study examines the effect of pregabalin (previously S‐Isobutylgaba and CI‐1008) in two distinct rat models of anxiety. Pregabalin binds with high affinity and selectivity to the α2δ subunit of voltage dependent calcium channels (VDCC). Its corresponding R‐enantiomer (R‐isobutylgaba) 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 contrast, R‐isobutylgaba only showed activity at the highest dose of 100 mg kg−1 in the conflict test. These data indicate that pregabalin may possess clinical utility as a novel anxiolytic agent and demonstrates the importance of the α2δ subunit of VDCC in the mediation of anxiety related behaviours. British Journal of Pharmacology (2001) 132, 1–4; doi:10.1038/sj.bjp.0703794
British Journal of Pharmacology – Wiley
Published: Jan 1, 2001
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