The diverse therapeutic actions of pregabalin: Is a single mechanism responsible for several pharmacological activities?

Stephen M. Stahl, Frank Porreca, Charles P. Taylor, Raymond Cheung, Andrew J. Thorpe, Andrew Clair

Research output: Contribution to journalReview article

67 Scopus citations

Abstract

Pregabalin is a specific ligand of the alpha2-delta (α2-δ) auxiliary subunit of voltage-gated calcium channels. A growing body of evidence from studies of anxiety and pain indicate that the observed responses with pregabalin may result from activity at the α2-δ auxiliary protein expressed presynaptically, in several different circuits of the central nervous system (CNS). The disorders that appear to be effectively treated with pregabalin are thematically linked by neuronal dysregulation or hyperexcitation within the CNS. This review proposes how binding to the α2-δ protein target in different regions of the CNS may contribute to the observed clinical activity of pregabalin, as well as to the adverse event profile of the compound. Whether this compound regulates synaptic function via α2-δ in additional conditions is yet to be discovered. The potential of pregabalin to regulate neuronal hyperactivity involving other CNS circuits will require further exploration.

Original languageEnglish (US)
Pages (from-to)332-339
Number of pages8
JournalTrends in Pharmacological Sciences
Volume34
Issue number6
DOIs
StatePublished - Jun 1 2013

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology

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