Small molecule
PubChem CID 3446
Gabapentin
Neurontin
- Mechanism of action
- Alpha-2-delta calcium channel subunit modulator
- In plain language
- Calms overactive nerve signals by damping down a calcium-channel doorway that nerve cells use to release pain and seizure signals.
- How it works
- Gabapentin binds with high affinity to the alpha-2-delta auxiliary subunits of voltage-gated calcium channels in the central nervous system. This binding is structurally unrelated to its GABA-like chemical scaffold, as gabapentin has no direct effect on GABA receptor binding, reuptake, or metabolism despite the name similarity. Through this interaction, gabapentin is thought to reduce trafficking of calcium channels to presynaptic nerve terminals, dampening calcium influx and the release of excitatory neurotransmitters implicated in seizure propagation and neuropathic pain signaling. The precise mechanisms underlying its analgesic and antiepileptic effects remain officially unknown, and the causal link between this binding and clinical benefit has not been fully established.
- Therapeutic applications
- Indicated for the management of postherpetic neuralgia in adults, and as adjunctive therapy in the treatment of partial-onset seizures, with and without secondary generalization, in adults and pediatric patients 3 years of age and older with epilepsy.
- Class
- Small molecule
- Therapeutic area
- CNS / Neurology
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