Gabapentin: Difference between revisions

>Gabapentinoid
m Altered and clarified description of pharmacological effects on GABA biosynthesis and Voltage-Gated Calcium Channels.
>Gabapentinoid
m Linked the word "anxiolytic" to https://psychonautwiki.org/wiki/Anxiety_suppression
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==Pharmacology==
==Pharmacology==
Gabapentin modulates the action of [[glutamate]] decarboxylase (GAD) and branched chain aminotransferase (BCAT), two enzymes involved in [[GABA]] biosynthesis. In human and rat studies, gabapentin was found to increase GABA biosynthesis, and to increase non-synaptic GABA neurotransmission in vitro.<ref>Mechanisms of action of gabapentin (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/9686247</ref> As the GABA system is the most prolific inhibitory receptor set within the brain, its increase in biosynthesis results in the [[sedating]] and anxiolytic (or [[Anxiety suppression|calming effects]]) of gabapentin on the nervous system.
Gabapentin modulates the action of [[glutamate]] decarboxylase (GAD) and branched chain aminotransferase (BCAT), two enzymes involved in [[GABA]] biosynthesis. In human and rat studies, gabapentin was found to increase GABA biosynthesis, and to increase non-synaptic GABA neurotransmission in vitro.<ref>Mechanisms of action of gabapentin (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/9686247</ref> As the GABA system is the most prolific inhibitory receptor set within the brain, its increase in biosynthesis results in the [[sedating]] and [[Anxiety_suppression|anxiolytic]] (or [[Anxiety suppression|calming effects]]) of gabapentin on the nervous system.


Gabapentin, as a gabapentinoid, has also been shown to bind to the α2δ-1 subunits of Voltage-Gated Calcium Channels to act as a VGCC blocker, which contributes to its inhibitory, analgesic, and anxiolytic effects. It is uncertain exactly how this method of action contributes to gabapentin's psychoactive effects.
Gabapentin, as a gabapentinoid, has also been shown to bind to the α2δ-1 subunits of Voltage-Gated Calcium Channels to act as a VGCC blocker, which contributes to its inhibitory, analgesic, and anxiolytic effects. It is uncertain exactly how this method of action contributes to gabapentin's psychoactive effects.