Talk:GABAA receptor

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This article is or was the subject of a Wiki Education Foundation-supported course assignment. Further details are available on the course page. Student editor(s): Jbrtn44. Peer reviewers: Wikied007, Biophysics Editor.

Above undated message substituted from Template:Dashboard.wikiedu.org assignment by PrimeBOT (talk) 21:58, 16 January 2022 (UTC)

human body --> brain

I changed this sentence from the introduction because glycine is the major inhibitory neurotransitter in the spine, not GABA. Moez ^talk 23:44, 20 June 2006 (UTC)

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38.100.34.2 16:56, 12 April 2007 (UTC)

???

Is that the text from a thesis or something ? ^talk 19:33, 30 November 2006 (UTC)

Condensation?

This article seems like a very well-researched paper, but I wonder if it too long and detailed for Wikipedia. Would anyone object some major culling? Alki 17:49, 2 December 2006 (UTC)

Thank you, this article as been reported to the WP:Extra-Long Article Committee and may have copyvio issues. We are investigating this. --Sadi Carnot 19:21, 6 December 2006 (UTC)

Move

I've taken the liberty of moving GABA A receptor to GABAA receptor since that way the proper name can show up in the title with the downsize template. I assumed that this would be an uncontroversial move and that there would be no problems with it, but if there are definitely let me know. Thanks, delldot | talk 02:13, 12 February 2007 (UTC)

Benzodiazepine receptor != GABAa receptor

The benzo receptor is not the same as the GABAa receptor! The GABAa receptor has different spots for different ligands, and the receptor site for GABA is different than the site for benzos, although both sites are both on the same receptor protein complex (not necessarily the same protein subunit). This is a very important distinction. If the benzos bound to the same site as GABA, they would presumably have effects similar to, or the same as the endogenous ligand (GABA). In reality, the benzos actually act as allosteric ("other site") GABA modulators by altering the GABA receptor protein's conformation. In fact, the GABAa receptor protein has multiple receptor sites (which are located on multiple subunits) for a variety of ligands, including barbiturates and certain steroids, and also certain anesthetics. As it stands, this article, as well as many, many others that reference the so-called "benzodiazepine receptor" are incredibly misleading. It is the benzo receptor site on the GABA_A receptor complex. See figure 6 on the following page [1] and also [2]. I also have several textbook references that I will add as soon as the article has been changed to reflect this subtle but important difference. Fuzzform 01:16, 28 September 2007 (UTC)

In fact, this article would do better to be named "GABA_A receptor complex". It really is a complex, as it binds multiple ligands in multiple spots around the ion channel, and is made up of multiple subunits (i.e. it is in it's quaternary structure). Fuzzform 01:20, 28 September 2007 (UTC)

• I agree that we should make clear that GABA and benzodiazepine ligands bind to different sites on the GABA_A receptor complex. However the term "receptor" not only refers to the binding site on the protein, but also to the entire protein or protein complex (which would include allosteric binding sites). For example, the gene (and protein encoded by the gene) for GABRA1 is called the "gamma-aminobutyric acid (GABA) A receptor, alpha 1". The reason for this of course is historical. Ligands for many receptors including the GABA_A receptor were discovered before the protein was isolated and characterized. Hence the protein was named after the ligand that bound to it and the name stuck even after the gene/protein was cloned and sequenced. Hence the distinction that you are proposing is in my opinion a semantic one. Cheers. Boghog2 07:15, 4 October 2007 (UTC)

• According to IUPHAR recommendations, the preferred name for benzodiazepine receptors is BZ-sensitive GABAA receptors. I have added this fact with a citation in the lead of the article. Since BZ-sensitive GABA_A receptors are often referred to as benzodiazepine receptors especially in the older literature, I still believe it is worth noting this. I hope this is an improvement. Cheers. Boghog2 (talk) 18:38, 20 June 2008 (UTC)

topiramate

A recent study has shown that use of topiramate has reduced drinking events in alcholics attempting to quit drinking. I looked into the mechanism of action of topiramate and discovered that it also affected the GABAA receptor in a fashion that wasn't blocked by flumazenil. The theory was that this had something to do with its anti-seizure effects. I suspect it also may have something to do with its common side effect of drowsiness and morning hangover feeling.

My question is: topiramate also has some effect in reducing frequency and severity of migraine headaches and decreasing carbohydrate cravings. The latter can actually lead to weight loss. Would this be a possible effect of its actions at the GABAA receptor, or is it more likely due to its effects of antagonizing kainate activation of the kainate/AMPA subtype of the glutamate receptor? —Preceding unsigned comment added by Samuraidoctor (talk • contribs) 13:43, 10 October 2007 (UTC)

Locations in the brain?

Are GABA-A receptors used pervasively throughout the entire brain? Or are they located in specific regions? I think this is an important fact to include, either way. --1000Faces (talk) 15:46, 20 September 2008 (UTC)

I'm sure you know what and where a synapse is. the chemical connections between nerve cells at the end of an axon? these are one type of receptor at the opposite end of the synapse. any synapse. — Preceding unsigned comment added by 173.49.233.207 (talk) 17:00, 4 October 2019 (UTC)

Perhaps too technical

I've tried reading this article twice, and I still can't figure out what this receptor actually *does* on anything other than a chemical level. Can we get a big picture view, explaining what these receptors do and how they affect human behavior? --72.207.70.17 (talk) 16:46, 29 April 2009 (UTC)

I tend to agree. As a note, GABAA activation is (in my understanding) sedating (older term: tranquilizing) in humans.67.167.106.3 (talk) 16:29, 11 June 2012 (UTC)

== Totally agree. I'm a student in an EMT basic class and I hear talk about GABA receptors -- how alcohol affects them, etc. Can we have one paragraph at the beginning that says in very simple terms how this thing affects the body? Obviously I'm not the person to write it but ... THANKS! Reilly Capps

the problem is that the functions are only known at this technical level. the information you seek is where research is currently being done. I'm not trying to be mean when I say this, but suggesting a possible career: go find out the answer to your questions about this. the world will want to know.

any way, beyond that; when receptor sites are occupied and busy, you are conscious and aware. the more that are occupied by medications that inhibit activity (like gabapentin for GABA sites and a muscle relaxer for BZ sites) the closer one gets to being asleep. Take gabapentin with a muscle relaxer in high enough quantities, and you *will sleep. this is why taking both classes of drugs is not medically advised, and shows up as a drug interaction at the pharmacy. -maxnort 173.49.233.207 (talk) 16:39, 4 October 2019 (UTC)

Dementia, memory impairment

I'm now reading on neurosteroids and regularly meet statements about GABA-A overstimulation leading in the chronic cases to dementia and memory impairment. Would be great if someone with deeper knowledge adds the relevant information into the article. Best regards, --CopperKettle 19:10, 10 December 2009 (UTC)

Zolpidem?

in the article, zolpidem is listed as GABA-A-agonist. is that true? can one give sources? as far as I know, zolpidem is in fact a modulator of GABA-A-receptors, just as benzodiazepines. --188.22.162.47 (talk) 23:30, 17 December 2010 (UTC)

Questionable language, encyclopedic?

To me this sounds vague and a bit sensationalist: "... in many cases the patient can sleep for days, weeks, months, years, or even die." 67.167.106.3 (talk) 17:04, 31 May 2012 (UTC)

it's the actual, literal truth. -maxnort — Preceding unsigned comment added by 173.49.233.207 (talk) 16:51, 4 October 2019 (UTC)

Negative Allosteric Modulator - Harmala Alkaloids

I'm not sure if this applies to GABAA receptor benzo sites, or others in the body. The article on Harmala Alkaloids comments that "As a benzodiazepine site inverse agonist, harmala alkaloids are..." which implies that it might be GABAAergic as an inverse benzo modulating (reducing) GABAA's overall activity.67.167.106.3 (talk) 16:26, 11 June 2012 (UTC)

Concomitant anxiolytic-like and cognitive-enhancing effects produced by Isovitexin and 6-C-glycoside-Diosmetin

I just found this article, it's a great finding! I'm just thinking were exactly this could be put on Wikipedia.

Article Conclusion: Altogether, our findings demonstrate a concomitant anxiolytic-like and cognitive-enhancement effect produced by Isovitexin and 6-C-glycoside-Diosmetin. These flavones modulate GABA A receptors via their benzodiazepine-binding site, such as Diazepam, which may result in anxiolytic-like behaviour. We suggest that cognitive-enhancements as observed in the group treated with Isovitexin and 6-C-glycoside-Diosmetin, may be the result of a lack of interaction in α1His101 in the BZ-binding site on GABA A receptors. Additional approaches are required to understand the mechanisms involved in these processes. These findings suggest that Isovitexin and 6-C-glycoside-Diosmetin provide novel therapeutic approaches that may be employed for anxiety disorders.

— Oliveira, Daniela Rodrigues de; Todo, Andréia Hatsue; Rêgo, Gizelda Maia; Cerutti, Janete Maria; Cavalheiro, Alberto José; Rando, Daniela Gonçales Galasse; Cerutti, Suzete Maria (July 2018). "Flavones-bound in benzodiazepine site on GABA A receptor: Concomitant anxiolytic-like and cognitive-enhancing effects produced by Isovitexin and 6-C-glycoside-Diosmetin". European Journal of Pharmacology. pp. 77–86. doi:10.1016/j.ejphar.2018.05.004. Retrieved 2019-06-19.

—Arthurfragoso (talk) 19:47, 19 June 2019 (UTC)

Hi Wikipedia!

I'm a student at Uskudar University in Istanbul, Turkiye. Right now, I'm taking a summer course in 2023 focused on Special Topics in Neuroscience. As part of the course, I'm working on improving a Wikipedia article about "GABAA receptor." If you have any feedback or suggestions, I'd really appreciate hearing them. Feel free to share your thoughts! Yumna alakash (talk) 11:09, 23 August 2023 (UTC)

Two cleanup items

I made two changes to this article; if either of them are unwarranted please feel free to revert them. The first one was removing the "which" tag from the first paragraph of the Ligands section. I felt it was unnecessary as there is a sub-section listing a large number of examples, which should satisfy the "which" criteria. The second change was that I moved the first entry in Ligands/Examples to the Structure and function section, as I felt the information fit better there (it was not an example of a ligand, it was just a sentence stating that research was done in a specific area). Lumberjane Lilly (talk) 17:44, 15 December 2023 (UTC)