Open main menu
Home
Random
Recent changes
Special pages
Community portal
Preferences
About Wikipedia
Disclaimers
Incubator escapee wiki
Search
User menu
Talk
Dark mode
Contributions
Create account
Log in
Editing
GABAA receptor
(section)
Warning:
You are not logged in. Your IP address will be publicly visible if you make any edits. If you
log in
or
create an account
, your edits will be attributed to your username, along with other benefits.
Anti-spam check. Do
not
fill this in!
=== Examples === * Orthosteric agonists: [[GABA]], [[gaboxadol]], [[isoguvacine]], [[muscimol]], [[progabide]], [[beta-alanine]],<ref name="Mori 191–200">{{cite journal | vauthors = Mori M, Gähwiler BH, Gerber U | title = Beta-alanine and taurine as endogenous agonists at glycine receptors in rat hippocampus in vitro | journal = The Journal of Physiology | volume = 539 | issue = Pt 1 | pages = 191–200 | date = February 2002 | pmid = 11850512 | pmc = 2290126 | doi = 10.1113/jphysiol.2001.013147 }}</ref><ref name="Horikoshi 97–105">{{cite journal | vauthors = Horikoshi T, Asanuma A, Yanagisawa K, Anzai K, Goto S | title = Taurine and beta-alanine act on both GABA and glycine receptors in Xenopus oocyte injected with mouse brain messenger RNA | journal = Brain Research | volume = 464 | issue = 2 | pages = 97–105 | date = September 1988 | pmid = 2464409 | doi = 10.1016/0169-328x(88)90002-2 }}</ref> [[taurine]],<ref name="Horikoshi 97–105"/><ref name="Mori 191–200"/> [[piperidine-4-sulfonic acid]] (partial agonist). * Orthosteric antagonists: [[bicuculline]], [[gabazine]]. * Positive allosteric modulators: [[abecarnil]],<ref>{{Cite journal |last1=Dn |first1=Stephens |last2=Hh |first2=Schneider |last3=W |first3=Kehr |last4=Js |first4=Andrews |last5=Kj |first5=Rettig |last6=L |first6=Turski |last7=R |first7=Schmiechen |last8=Jd |first8=Turner |last9=Lh |first9=Jensen |last10=En |first10=Petersen |date=April 1990 |title=Abecarnil, a metabolically stable, anxioselective beta-carboline acting at benzodiazepine receptors |url=https://pubmed.ncbi.nlm.nih.gov/1970361/ |journal=The Journal of Pharmacology and Experimental Therapeutics |language=en |volume=253 |issue=1 |pages=334–343 |doi=10.1016/S0022-3565(25)12465-8 |issn=0022-3565 |pmid=1970361}}</ref> [[Abecarnil|azocarnil]]<ref>{{Cite journal |last1=Maleeva |first1=Galyna |last2=Nin-Hill |first2=Alba |last3=Wirth |first3=Ulrike |last4=Rustler |first4=Karin |last5=Ranucci |first5=Matteo |last6=Opar |first6=Ekin |last7=Rovira |first7=Carme |last8=Bregestovski |first8=Piotr |last9=Zeilhofer |first9=Hanns Ulrich |last10=König |first10=Burkhard |last11=Alfonso-Prieto |first11=Mercedes |last12=Gorostiza |first12=Pau |date=2024-10-09 |title=Light-Activated Agonist-Potentiator of GABA A Receptors for Reversible Neuroinhibition in Wildtype Mice |journal=Journal of the American Chemical Society |volume=146 |issue=42 |pages=28822–28831 |language=en |doi=10.1021/jacs.4c08446 |pmid=39383450 |issn=0002-7863|pmc=11503767 |bibcode=2024JAChS.14628822M }}</ref> ([[Photoswitch|photoswitchable]]), [[barbiturate]]s, [[benzodiazepine]]s, certain [[carbamates]] (e.g., [[carisoprodol]], [[meprobamate]], [[lorbamate]]), [[honokiol]], [[magnolol]], [[baicalin]], [[baicelin]], [[thienodiazepine]]s, [[alcohol (drug)|alcohol]] ([[ethanol]]), [[etomidate]], [[glutethimide]], [[kavalactone]]s,<ref name="Hunter">{{cite journal |author=Hunter, A | title=Kava (Piper methysticum) back in circulation | journal=Australian Centre for Complementary Medicine |volume=25 | issue=7 | year=2006 | page=529}}</ref> [[meprobamate]], [[quinazolinone]]s (e.g., [[methaqualone]], [[etaqualone]], [[diproqualone]]), [[neuroactive steroid]]s,<ref name="neuroactive_steroid">(a) {{cite journal | vauthors = Herd MB, Belelli D, Lambert JJ | title = Neurosteroid modulation of synaptic and extrasynaptic GABA(A) receptors | journal = Pharmacology & Therapeutics | volume = 116 | issue = 1 | pages = 20–34 | date = October 2007 | pmid = 17531325 | doi = 10.1016/j.pharmthera.2007.03.007 | url = http://www.journals.elsevier.com/pharmacology-and-therapeutics | arxiv = 1607.02870 }}<br/>(b) {{cite journal | vauthors = Hosie AM, Wilkins ME, da Silva HM, Smart TG | title = Endogenous neurosteroids regulate GABAA receptors through two discrete transmembrane sites | journal = Nature | volume = 444 | issue = 7118 | pages = 486–9 | date = November 2006 | pmid = 17108970 | doi = 10.1038/nature05324 | bibcode = 2006Natur.444..486H | s2cid = 4382394 }}<br/>(c) {{cite journal | vauthors = Agís-Balboa RC, Pinna G, Zhubi A, Maloku E, Veldic M, Costa E, Guidotti A | title = Characterization of brain neurons that express enzymes mediating neurosteroid biosynthesis | journal = Proceedings of the National Academy of Sciences of the United States of America | volume = 103 | issue = 39 | pages = 14602–7 | date = September 2006 | pmid = 16984997 | pmc = 1600006 | doi = 10.1073/pnas.0606544103 | bibcode = 2006PNAS..10314602A | doi-access = free }}<br/>(d) {{cite journal | vauthors = Akk G, Shu HJ, Wang C, Steinbach JH, Zorumski CF, Covey DF, Mennerick S | title = Neurosteroid access to the GABAA receptor | journal = The Journal of Neuroscience | volume = 25 | issue = 50 | pages = 11605–13 | date = December 2005 | pmid = 16354918 | pmc = 6726021 | doi = 10.1523/JNEUROSCI.4173-05.2005 }}<br/>(e) {{cite journal | vauthors = Belelli D, Lambert JJ | title = Neurosteroids: endogenous regulators of the GABA(A) receptor | journal = Nature Reviews. Neuroscience | volume = 6 | issue = 7 | pages = 565–575 | date = July 2005 | pmid = 15959466 | doi = 10.1038/nrn1703 | s2cid = 12596378 }}<br/>(f) {{cite journal | vauthors = Pinna G, Costa E, Guidotti A | title = Fluoxetine and norfluoxetine stereospecifically and selectively increase brain neurosteroid content at doses that are inactive on 5-HT reuptake | journal = Psychopharmacology | volume = 186 | issue = 3 | pages = 362–372 | date = June 2006 | pmid = 16432684 | doi = 10.1007/s00213-005-0213-2 | s2cid = 7799814 }}<br/>(g) {{cite journal | vauthors = Dubrovsky BO | title = Steroids, neuroactive steroids and neurosteroids in psychopathology | journal = Progress in Neuro-Psychopharmacology & Biological Psychiatry | volume = 29 | issue = 2 | pages = 169–192 | date = February 2005 | pmid = 15694225 | doi = 10.1016/j.pnpbp.2004.11.001 | s2cid = 36197603 }}<br/>(h) {{cite journal | vauthors = Mellon SH, Griffin LD | title = Neurosteroids: biochemistry and clinical significance | journal = Trends in Endocrinology and Metabolism | volume = 13 | issue = 1 | pages = 35–43 | year = 2002 | pmid = 11750861 | doi = 10.1016/S1043-2760(01)00503-3 | s2cid = 11605131 }}<br/>(i) {{cite journal | vauthors = Puia G, Santi MR, Vicini S, Pritchett DB, Purdy RH, Paul SM, Seeburg PH, Costa E | title = Neurosteroids act on recombinant human GABAA receptors | journal = Neuron | volume = 4 | issue = 5 | pages = 759–765 | date = May 1990 | pmid = 2160838 | doi = 10.1016/0896-6273(90)90202-Q | s2cid = 12626366 }}<br/>(j) {{cite journal | vauthors = Majewska MD, Harrison NL, Schwartz RD, Barker JL, Paul SM | title = Steroid hormone metabolites are barbiturate-like modulators of the GABA receptor | journal = Science | volume = 232 | issue = 4753 | pages = 1004–7 | date = May 1986 | pmid = 2422758 | doi = 10.1126/science.2422758 | url = https://zenodo.org/record/1230988 | bibcode = 1986Sci...232.1004D }}<br/>(k) {{cite book |vauthors=Reddy DS, Rogawski MA | chapter = Neurosteroids — Endogenous Regulators of Seizure Susceptibility and Role in the Treatment of Epilepsy |veditors=Noebels JL, Avoli M, Rogawski MA |title = Jasper's Basic Mechanisms of the Epilepsies [Internet] |edition=4th |publisher=National Center for Biotechnology Information (US) | date = 2012 | chapter-url = https://www.ncbi.nlm.nih.gov/books/NBK98218/ |id=NBK98218 |display-editors=etal | pmid = 22787590 }}</ref> [[Niacin (nutrient)|niacin]]/[[niacinamide]],<ref>{{cite journal| vauthors = Toraskar M, Singh PR, Neve S |title=STUDY OF GABAERGIC AGONISTS|journal=Deccan Journal of Pharmacology|year=2010|volume=1|issue=2|pages=56–69|url=http://www.ijdpls.com/uploaded/journal_files/120402040442.pdf|access-date=2013-02-12|archive-url=https://web.archive.org/web/20131016082147/http://www.ijdpls.com/uploaded/journal_files/120402040442.pdf|archive-date=2013-10-16|url-status=dead}}</ref> [[nonbenzodiazepine]]s (e.g., [[zolpidem]], [[eszopiclone]]), [[propofol]], [[stiripentol]],<ref>{{cite journal | vauthors = Fisher JL | title = The anti-convulsant stiripentol acts directly on the GABA(A) receptor as a positive allosteric modulator | journal = Neuropharmacology | volume = 56 | issue = 1 | pages = 190–7 | date = January 2009 | pmid = 18585399 | pmc = 2665930 | doi = 10.1016/j.neuropharm.2008.06.004 }}</ref> [[theanine]],{{citation needed|date=November 2017}} [[valerenic acid]], [[Volatile anaesthetic|volatile/inhaled]] [[anesthetic]]s, [[lanthanum]],<ref>{{cite journal | vauthors = Boldyreva AA | title = Lanthanum potentiates GABA-activated currents in rat pyramidal neurons of CA1 hippocampal field | journal = Bulletin of Experimental Biology and Medicine | volume = 140 | issue = 4 | pages = 403–5 | date = October 2005 | pmid = 16671565 | doi = 10.1007/s10517-005-0503-z | s2cid = 13179025 }}</ref> [[riluzole]],<ref name="pmid11804616">{{cite journal | vauthors = He Y, Benz A, Fu T, Wang M, Covey DF, Zorumski CF, Mennerick S | title = Neuroprotective agent riluzole potentiates postsynaptic GABA(A) receptor function | journal = Neuropharmacology | volume = 42 | issue = 2 | pages = 199–209 | date = February 2002 | pmid = 11804616 | doi = 10.1016/s0028-3908(01)00175-7 | s2cid = 24194421 }}</ref> and [[menthol]].<ref>{{cite journal | pmc=4243856 | date=2014 | last1=Lau | first1=B. K. | last2=Karim | first2=S. | last3=Goodchild | first3=A. K. | last4=Vaughan | first4=C. W. | last5=Drew | first5=G. M. | title=Menthol enhances phasic and tonic GABAA receptor-mediated currents in midbrain periaqueductal grey neurons | journal=British Journal of Pharmacology | volume=171 | issue=11 | pages=2803–13 | doi=10.1111/bph.12602 | pmid=24460753 }}</ref> * Negative allosteric modulators: [[flumazenil]], [[Ro15-4513]], [[sarmazenil]], [[pregnenolone sulfate]], [[amentoflavone]], and [[zinc]].<ref name="pmid12640458">{{cite journal | vauthors = Hosie AM, Dunne EL, Harvey RJ, Smart TG | title = Zinc-mediated inhibition of GABA(A) receptors: discrete binding sites underlie subtype specificity | journal = Nature Neuroscience | volume = 6 | issue = 4 | pages = 362–9 | date = April 2003 | pmid = 12640458 | doi = 10.1038/nn1030 | s2cid = 24096465 }}</ref> * Inverse allosteric agonists: [[beta-carbolines]] (e.g., [[harmine]], [[harmaline]], [[tetrahydroharmine]]). * Second-order modulators: [[Epigallocatechin gallate|(−)‐epigallocatechin‐3‐gallate]].<ref>{{cite journal | vauthors = Campbell EL, Chebib M, Johnston GA | title = The dietary flavonoids apigenin and (-)-epigallocatechin gallate enhance the positive modulation by diazepam of the activation by GABA of recombinant GABA(A) receptors | journal = Biochemical Pharmacology | volume = 68 | issue = 8 | pages = 1631–8 | date = October 2004 | pmid = 15451406 | doi = 10.1016/j.bcp.2004.07.022 | series = Six Decades of GABA }}</ref> * Non-competitive channel blockers: [[cicutoxin]], [[oenanthotoxin]], [[pentylenetetrazol]], [[picrotoxin]]{{citation needed|date=April 2019}}, [[thujone]], and [[lindane]].
Edit summary
(Briefly describe your changes)
By publishing changes, you agree to the
Terms of Use
, and you irrevocably agree to release your contribution under the
CC BY-SA 4.0 License
and the
GFDL
. You agree that a hyperlink or URL is sufficient attribution under the Creative Commons license.
Cancel
Editing help
(opens in new window)