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Pregabalin is 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) 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.
| Molecular Weight | 159.23 |
| Formula | C8H17NO2 |
| CAS Number | 148553-50-8 |
| Solubility (25°C) | Water 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Sheena Derry, et al. Pregabalin for neuropathic pain in adults
[2] H Karl Greenblatt, et al. Gabapentin and Pregabalin for the Treatment of Anxiety Disorders
[3] E E Morrison, et al. Gabapentin and pregabalin: do the benefits outweigh the harms?
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