[A 3-isobutyl derivative of gamma-amino butyric acid (GABA) with anti-convulsant, anti-epileptic, anxiolytic and analgesic activities. Pregabalin selectively binds to alpha2delta (A2D) subunit of the presynaptic voltage-gated calcium channels located in the central nervous system (CNS). Binding of A2D subunits prevent calcium influxes and the subsequent calcium-dependent releases of various neurotransmitters from presynaptic nerve terminals in hyperexcited neurons, including glutamate, norepinephrine, serotonin, dopamine, and substance P. This leads to an inhibition of synaptic transmission and reduces neuronal excitability. Pregabalin does not bind directly to GABA-A, GABA-B receptors and does not alter GABA uptake or degradation. ( NCI )]
UMLS (NCI) C0657912 - Amino Acid, Peptide, or Protein
- Pharmacologic Substance