The diverse therapeutic actions of pregabalin: is a single mechanism responsible for several pharmacological activities?
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 presyna...
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| Veröffentlicht in: | Trends in pharmacological sciences (Regular ed.) 2013-06, Vol.34 (6), p.332-339 |
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| container_title | Trends in pharmacological sciences (Regular ed.) |
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| creator | Stahl, Stephen M Porreca, Frank Taylor, Charles P Cheung, Raymond Thorpe, Andrew J Clair, Andrew |
| description | 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. |
| doi_str_mv | 10.1016/j.tips.2013.04.001 |
| format | Article |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Advanced Basic Science Animals Calcium Channel Blockers - pharmacology Calcium Channel Blockers - therapeutic use Central Nervous System Diseases - drug therapy gamma-Aminobutyric Acid - analogs & derivatives gamma-Aminobutyric Acid - pharmacology gamma-Aminobutyric Acid - therapeutic use Humans Pregabalin Synaptic Transmission - drug effects |
| title | The diverse therapeutic actions of pregabalin: is a single mechanism responsible for several pharmacological activities? |
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