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pregabalin
A 3-isobutyl derivative of gamma-amino butyric acid (GABA) with anti-convulsant, anti-epileptic, anxiolytic, and analgesic activities. Although the exact mechanism of action is unknown, pregabalin selectively binds to alpha2delta (A2D) subunits of presynaptic voltage-dependent calcium channels (VDCCs) located in the central nervous system (CNS). Binding of pregabalin to VDCC A2D subunits prevents calcium influx and the subsequent calcium-dependent release of various neurotransmitters, including glutamate, norepinephrine, serotonin, dopamine, and substance P, from the presynaptic nerve terminals of hyperexcited neurons; synaptic transmission is inhibited and neuronal excitability is diminished. Pregabalin does not bind directly to GABA-A or GABA-B receptors and does not alter GABA uptake or degradation. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)
| Synonym: | | 3-Isobutyl GABA | | | | US brand name: | | Lyrica | | | | Code names: | | CI-1008
PD-144723 | | | | Chemical structure name: | | 3-(aminomethyl)-5-methyl-hexanoic acid | | |
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