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

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• 作者：Stephen M. Stahl¹ ; Frank Porreca² ; Charles P. Taylor³ ; Raymond Cheung⁴ ; Andrew J. Thorpe⁴ ; Andrew Clair⁴ ; ^{andrew.clair@pfizer.com} ; ^{brenda.meyer@ubc-envisiongroup.com}
• 刊名：Trends in Pharmacological Sciences
• 出版年：2013
• 出版时间：June, 2013
• 年：2013
• 卷：34
• 期：6
• 页码：332-339
• 全文大小：1336 K

文摘

Pregabalin is a specific ligand of the alpha₂-delta (¦Á₂-¦Ä) 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 ¦Á₂-¦Ä 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 ¦Á₂-¦Ä 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 ¦Á₂-¦Ä in additional conditions is yet to be discovered. The potential of pregabalin to regulate neuronal hyperactivity involving other CNS circuits will require further exploration.