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GABA: Difference between revisions
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GABA is metabolized by the enzyme GABA transaminase and certain drugs (such as the antiepileptic [[vigabatrin]]) have inhibition of this enzyme as their mechanism of action. Eventually, GABA can be recovered by its metabolite succinic semialdehyde which is transformed by succinic semialdehyde dehydrogenase into succinic acid and enters the Krebs cycle, a complicated pathway that begins with glucose. On the other end of the cycle, glutamine emerges and can be transported back to the neuron where it is converted by the enzyme glutaminase into glutamate which can then be remade into GABA via GAD, completing the loop. This loop is called the GABA shunt.<ref>GABA Synthesis, Uptake and Release (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/books/NBK27979/</ref> | GABA is metabolized by the enzyme GABA transaminase and certain drugs (such as the antiepileptic [[vigabatrin]]) have inhibition of this enzyme as their mechanism of action. Eventually, GABA can be recovered by its metabolite succinic semialdehyde which is transformed by succinic semialdehyde dehydrogenase into succinic acid and enters the Krebs cycle, a complicated pathway that begins with glucose. On the other end of the cycle, glutamine emerges and can be transported back to the neuron where it is converted by the enzyme glutaminase into glutamate which can then be remade into GABA via GAD, completing the loop. This loop is called the GABA shunt.<ref>GABA Synthesis, Uptake and Release (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/books/NBK27979/</ref> | ||
== | == Pharmacology == | ||
Drugs that act as allosteric modulators of GABA receptors (known as GABA analogues or ''GABAergic'' drugs), or increase the available amount of GABA, typically have relaxing, anti-anxiety, and anti-convulsive effects.<ref>Foster AC, Kemp JA (February 2006). "Glutamate- and GABA-based CNS therapeutics". ''Curr Opin Pharmacol''. '''6''' (1): 7–17. doi:10.1016/j.coph.2005.11.005. <nowiki>PMID 16377242</nowiki>.</ref> | |||
In general, GABA does not cross the blood–brain barrier,<ref>Kuriyama K, Sze PY (January 1971). "Blood–brain barrier to H3-γ-aminobutyric acid in normal and amino oxyacetic acid-treated animals". ''Neuropharmacology''. '''10''' (1): 103–108. doi:10.1016/0028-3908(71)90013-X. <nowiki>PMID 5569303</nowiki>.</ref> although certain areas of the brain that have no effective blood–brain barrier, such as the periventricular nucleus, can be reached by drugs such as systemically injected GABA.<ref>Müller EE, Locatelli V, Cocchi D (April 1999). "Neuroendocrine control of growth hormone secretion". ''Physiol. Rev''. '''79''' (2): 511–607. doi:10.1152/physrev.1999.79.2.511. <nowiki>PMID 10221989</nowiki>.</ref> | |||
==Inhibitory response== | ==Inhibitory response== | ||
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===Drugs targeting [[GABA-A|GABA<sub>A</sub>]]=== | ===Drugs targeting [[GABA-A|GABA<sub>A</sub>]]=== | ||
====[[Benzodiazepine|Benzodiazepines]]==== | ====[[Benzodiazepine|Benzodiazepines]]==== | ||
* [[Alprazolam]] | |||
* [[Clonazepam]] | *[[Alprazolam]] | ||
* [[Clonazolam]] | *[[Clonazepam]] | ||
* [[Diazepam]] | *[[Clonazolam]] | ||
* [[Diclazepam]] | *[[Diazepam]] | ||
* [[Flubromazolam]] | *[[Diclazepam]] | ||
* [[Flubromazepam]] | *[[Flubromazolam]] | ||
* [[Nifoxipam]] | *[[Flubromazepam]] | ||
* [[Lorazepam]] | *[[Nifoxipam]] | ||
* [[Phenazepam]] | *[[Lorazepam]] | ||
* [[Pyrazolam]] | *[[Phenazepam]] | ||
* [[Temazepam]] | *[[Pyrazolam]] | ||
* [[Triazolam]] | *[[Temazepam]] | ||
*[[Triazolam]] | |||
====[[Thienodiazepine|Thienodiazepines]]==== | ====[[Thienodiazepine|Thienodiazepines]]==== | ||
* [[Etizolam]] | |||
* [[Deschloroetizolam]] | *[[Etizolam]] | ||
* [[Metizolam]] | *[[Deschloroetizolam]] | ||
*[[Metizolam]] | |||
====Others==== | ====Others==== | ||
* [[Alcohol]] | |||
* [[2-Methyl-2-butanol]] | *[[Alcohol]] | ||
* [[Barbiturates]] | *[[2-Methyl-2-butanol]] | ||
* [[Carisoprodol]] | *[[Barbiturates]] | ||
* [[Methaqualone]] | *[[Carisoprodol]] | ||
* [[Amanita muscaria|Muscimol]] | *[[Methaqualone]] | ||
* [[Zaleplon]] | *[[Amanita muscaria|Muscimol]] | ||
* [[Zopiclone]] | *[[Zaleplon]] | ||
* [[Zolpidem]] | *[[Zopiclone]] | ||
*[[Zolpidem]] | |||
===Drugs targeting [[GABA-B|GABA<sub>B</sub>]]=== | ===Drugs targeting [[GABA-B|GABA<sub>B</sub>]]=== | ||
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==See also== | ==See also== | ||
*[[Responsible use]] | *[[Responsible use]] | ||
*[[Acetylcholine]] | *[[Acetylcholine]] | ||
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==External links== | ==External links== | ||
*[[wikipedia:gamma-Aminobutyric acid|''gamma''-Aminobutyric acid (Wikipedia)]] | *[[wikipedia:gamma-Aminobutyric acid|''gamma''-Aminobutyric acid (Wikipedia)]] | ||
==References== | ==References== | ||
<references/> | <references /> | ||
[[Category:Neurotransmitter]] | [[Category:Neurotransmitter]] | ||
[[Category:Amino acid]] | [[Category:Amino acid]] | ||