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Mechanisms of action of Neurontin: Advanced

Topics List
New comprehensive downloadable medication sheet
  • Additional information on this drug and how to use it.
  • A starting point for discussion with your doctor.
  • Answers to frequently asked questions.

Neurontin was formed by the addition of a cyclohexyl group to gamma-aminobutyric acid (GABA), which allowed this form of GABA to cross the blood-brain barrier.

Despite its structural similarity to GABA, Neurontin does not bind to GABA receptors in the CNS. Its mechanism of action is unknown, but may involve enhanced neuronal GABA synthesis.


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