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

Citation
Mj. Field et al., Pregabalin may represent a novel class of anxiolytic agents with a broad spectrum of activity, BR J PHARM, 132(1), 2001, pp. 1-4
Citations number
18
Categorie Soggetti
Pharmacology & Toxicology
Journal title
BRITISH JOURNAL OF PHARMACOLOGY
ISSN journal
00071188 → ACNP
Volume
132
Issue
1
Year of publication
2001
Pages
1 - 4
Database
ISI
SICI code
0007-1188(200101)132:1<1:PMRANC>2.0.ZU;2-H
Abstract
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.