The Sound of Evolution
Pregabalin
Mechanism of action:
Pregabalin is a gamma-aminobutyric acid (GABA) analog. Pregabalin binds with high affinity to the alpha2delta-1 and alpha2delta-2 subunits of voltage-gated Ca2+ channels in the central nervous system. When neurons undergo depolarization, pregabalin reduces calcium entry into presynaptic nerve terminals and thereby inhibits the release of neurotransmitters.
Reference(s):
1. Authors unspecified et al. (2005). Schedules of controlled substances: placement of pregabalin into schedule V. Fed Regist.
2. Su TZ et al. (2005). Mediation of highly concentrative uptake of pregabalin by L-type amino acid transport in Chinese hamster ovary and Caco-2 cells. J Pharmacol Exp Ther.
3. Li Z et al. (2011). Pregabalin is a potent and selective ligand for alpha(2)delta-1 and alpha(2)delta-2 calcium channel subunits. Eur J Pharmacol.