Pregabalin may represent a novel class of anxiolytic agents with a broad spectrum of activity

Pregabalin may represent a novel class of anxiolytic agents with a broad spectrum of activity 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 http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png British Journal of Pharmacology Wiley

Pregabalin may represent a novel class of anxiolytic agents with a broad spectrum of activity

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Publisher
Wiley
Copyright
2001 British Pharmacological Society
ISSN
0007-1188
eISSN
1476-5381
DOI
10.1038/sj.bjp.0703794
pmid
11156553
Publisher site
See Article on Publisher Site

Abstract

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

Journal

British Journal of PharmacologyWiley

Published: Jan 1, 2001

References

  • Gabapentin (neurontin) and S‐(+)‐3‐isobutylgaba represent a novel class of selective antihyperalgesic agents
    FIELD, FIELD; OLES, OLES; LEWIS, LEWIS; MCCLEARY, MCCLEARY; HUGHES, HUGHES; SINGH, SINGH
  • The antiepileptic agent gabapentin (Neurontin) possesses anxiolytic‐like and antinociceptive actions that are reversed by D‐Serine
    SINGH, SINGH; FIELD, FIELD; FERRIS, FERRIS; HUNTER, HUNTER; OLES, OLES; WILLIAMS, WILLIAMS; WOODRUFF, WOODRUFF

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