The diverse therapeutic actions of pregabalin: is a single mechanism responsible for several pharmacological activities?
Trends Pharmacol Sci
; 34(6): 332-9, 2013 Jun.
Article
in En
| MEDLINE
| ID: mdl-23642658
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.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Calcium Channel Blockers
/
Central Nervous System Diseases
/
Gamma-Aminobutyric Acid
Limits:
Animals
/
Humans
Language:
En
Journal:
Trends Pharmacol Sci
Year:
2013
Document type:
Article
Affiliation country:
United States