Saturday, May 13, 2017

Mechanism of action of gabapentin and pregabalin

Gabapentin binds to which of the following receptors?
1. GABAA receptors
2. GABAB receptors
3. alpa2delta subunit of voltage-sensitive Ca2+ channels
4. NMDA receptors

The answer is 3.

Gabapentin and pregabalin are structurally similar to gamma-aminobutyric acid (GABA), although they do not bind to GABA receptors. They bind to the α-2-delta subunit of voltage-dependent calcium channels (aka alpha-2-delta calcium channel ligands).

This leads to reduction of the influx of calcium into neurons throughout the central nervous system (CNS). This in turn may decrease the release of glutamate, norepinephrine, and substance P.

In vitro, gabapentin modulates the action of the GABA synthetic enzyme, glutamic acid decarboxylase (GAD) and the glutamate synthesizing enzyme, branched-chain amino acid transaminase.

That's all!
I thought you guys should know this, just in case it is asked in exams!

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