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PMID: 7643969 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't Review

Heterogeneity of GABAA-receptors: cell-specific expression, pharmacology, and regulation.

Neurochemical research ·Vol. 20 ·No. 5 ·1995-05-00 ·Pages 631-6

Mohler H, Knoflach F, Paysan J, Motejlek K, Benke D, Lüscher B, Fritschy JM

Abstract

Vigilance, anxiety, memory, epileptogenic activity and muscle tension can be regulated by a modulation of GABAA-receptor function. A multitude of different GABAA-receptors exist in the brain due to the combinational assembly of various subunits encoded by at least 15 genes. The clarification of the physiological and pharmacological significance of GABAA-receptor subtypes, in combination with their cellular localization, will make it possible to identify the neuronal circuits regulating the respective CNS states and to provide strategies for the development of subtype-specific drugs for selective therapies.

MeSH Terms
Animals Brain/cytology,metabolism Gene Expression Regulation/physiology Immunohistochemistry Neurons/chemistry Receptors, GABA-A/analysis,chemistry,drug effects
Chemicals
Receptors, GABA-A
Authors & Affiliations
7 authors, click to expand affiliations / ORCID
Mohler H
Institute of Pharmacology, University, Zürich, Switzerland.
Knoflach F
Paysan J
Motejlek K
Benke D
Lüscher B
Fritschy J M
References (36)
36 references, click to expand
  1. Switch in the expression of rat GABAA-receptor subtypes during postnatal development: an immunohistochemical study.
    J Neurosci. 1994 Sep;14(9):5302-24 PMID: 8083738
  2. A single histidine in GABAA receptors is essential for benzodiazepine agonist binding.
    J Biol Chem. 1992 Jan 25;267(3):1426-9 PMID: 1346133
  3. Molecular characterization of type I GABAA receptor complex from rat cerebral cortex and hippocampus.
    Brain Res Mol Brain Res. 1994 Sep;25(3-4):225-33 PMID: 7808221
  4. Identification of distinct GABAA-receptor subtypes in cholinergic and parvalbumin-positive neurons of the rat and marmoset medial septum-diagonal band complex.
    Neuroscience. 1995 Mar;65(1):101-17 PMID: 7753393
  5. Molecular mechanisms of the partial allosteric modulatory effects of bretazenil at gamma-aminobutyric acid type A receptor.
    Proc Natl Acad Sci U S A. 1992 Apr 15;89(8):3620-4 PMID: 1373505
  6. GABAA receptor subunit immunoreactivity in primate visual cortex: distribution in macaques and humans and regulation by visual input in adulthood.
    J Neurosci. 1994 Apr;14(4):2383-401 PMID: 8158275
  7. Novel anxiolytics that act as partial agonists at benzodiazepine receptors.
    Trends Pharmacol Sci. 1990 Nov;11(11):452-6 PMID: 1980040
  8. BSF1, a novel brain-specific DNA-binding protein recognizing a tandemly repeated purine DNA element in the GABAA receptor delta subunit gene.
    J Biol Chem. 1994 May 27;269(21):15265-73 PMID: 8195163
  9. Five subtypes of type A gamma-aminobutyric acid receptors identified in neurons by double and triple immunofluorescence staining with subunit-specific antibodies.
    Proc Natl Acad Sci U S A. 1992 Aug 1;89(15):6726-30 PMID: 1323116
  10. Full and partial agonism displayed by benzodiazepine receptor ligands at recombinant gamma-aminobutyric acidA receptor subtypes.
    J Pharmacol Exp Ther. 1993 Jul;266(1):385-91 PMID: 8392559
  11. Type I and type II GABAA-benzodiazepine receptors produced in transfected cells.
    Science. 1989 Sep 22;245(4924):1389-92 PMID: 2551039
  12. Biphasic differential changes of GABAA receptor subunit mRNA levels in dentate gyrus granule cells following recurrent kindling-induced seizures.
    Brain Res Mol Brain Res. 1994 Jun;23(4):323-32 PMID: 8090072
  13. Altered excitatory and inhibitory amino acid receptor binding in hippocampus of patients with temporal lobe epilepsy.
    Ann Neurol. 1991 May;29(5):529-41 PMID: 1650160
  14. GABAA receptor channels.
    Annu Rev Neurosci. 1994;17:569-602 PMID: 7516126
  15. GABAA-receptors: drug binding profile and distribution of receptors containing the alpha 2-subunit in situ.
    J Recept Res. 1993;13(1-4):467-77 PMID: 8383760
  16. Distribution, prevalence, and drug binding profile of gamma-aminobutyric acid type A receptor subtypes differing in the beta-subunit variant.
    J Biol Chem. 1994 Oct 28;269(43):27100-7 PMID: 7929453
  17. In-vivo demonstration of reduced benzodiazepine receptor binding in human epileptic foci.
    Lancet. 1988 Oct 15;2(8616):863-6 PMID: 2902315
  18. Biochemical evidence for the existence of gamma-aminobutyrateA receptor iso-oligomers.
    J Biol Chem. 1990 Mar 5;265(7):3831-5 PMID: 2154490
  19. GABAA receptor populations with novel subunit combinations and drug binding profiles identified in brain by alpha 5- and delta-subunit-specific immunopurification.
    J Biol Chem. 1993 Mar 15;268(8):5965-73 PMID: 8383681
  20. GABAA receptor alpha 1 subunit, an early marker for area specification in developing rat cerebral cortex.
    J Comp Neurol. 1994 Dec 1;350(1):133-49 PMID: 7860797
  21. Gamma-aminobutyric acidA receptor alpha 5-subunit creates novel type II benzodiazepine receptor pharmacology.
    J Neurochem. 1990 May;54(5):1802-4 PMID: 2157817
  22. Cloning, pharmacological characteristics and expression pattern of the rat GABAA receptor alpha 4 subunit.
    FEBS Lett. 1991 Sep 9;289(2):227-30 PMID: 1655526
  23. The distribution of GABAA-benzodiazepine receptors in the basal ganglia in Huntington's disease and in the quinolinic acid-lesioned rat.
    Prog Brain Res. 1993;99:105-23 PMID: 8108544
  24. Neuron-specific expression of GABAA-receptor subtypes: differential association of the alpha 1- and alpha 3-subunits with serotonergic and GABAergic neurons.
    Neuroscience. 1993 Jun;54(4):881-92 PMID: 8393540
  25. Lamina-specific expression and activity-dependent regulation of seven GABAA receptor subunit mRNAs in monkey visual cortex.
    J Neurosci. 1994 Apr;14(4):2236-59 PMID: 8158267
  26. Quaternary structure of the native GABAA receptor determined by electron microscopic image analysis.
    J Neurochem. 1994 Feb;62(2):815-8 PMID: 7507518
  27. Cerebellar GABAA receptor selective for a behavioural alcohol antagonist.
    Nature. 1990 Aug 16;346(6285):648-51 PMID: 2166916
  28. Importance of a novel GABAA receptor subunit for benzodiazepine pharmacology.
    Nature. 1989 Apr 13;338(6216):582-5 PMID: 2538761
  29. GABAA-receptor expressed from rat brain alpha- and beta-subunit cDNAs displays potentiation by benzodiazepine receptor ligands.
    Brain Res Mol Brain Res. 1990 Aug;8(3):199-208 PMID: 1977069
  30. Differences in affinity and efficacy of benzodiazepine receptor ligands at recombinant gamma-aminobutyric acidA receptor subtypes.
    Mol Pharmacol. 1993 Feb;43(2):240-4 PMID: 8381510
  31. GABAA receptors display association of gamma 2-subunit with alpha 1- and beta 2/3-subunits.
    J Biol Chem. 1991 Mar 5;266(7):4478-83 PMID: 1847922
  32. GABAA receptor subtypes immunopurified from rat brain with alpha subunit-specific antibodies have unique pharmacological properties.
    Neuron. 1991 Oct;7(4):667-76 PMID: 1657058
  33. Abecarnil is a full agonist at some, and a partial agonist at other recombinant GABAA receptor subtypes.
    Psychopharmacol Ser. 1993;11:50-61 PMID: 7908433
  34. Assembly of GABAA receptor subunits: alpha 1 beta 1 and alpha 1 beta 1 gamma 2S subunits produce unique ion channels with dissimilar single-channel properties.
    J Neurosci. 1993 Apr;13(4):1429-40 PMID: 7681870
  35. The effect of subunit composition of rat brain GABAA receptors on channel function.
    Neuron. 1990 Nov;5(5):703-11 PMID: 1699569
  36. Sequence and functional expression of the GABA A receptor shows a ligand-gated receptor super-family.
    Nature. 1987 Jul 16-22;328(6127):221-7 PMID: 3037384
Article Info
Journal
Neurochemical research
Abbr.
Neurochem Res
ISSN
0364-3190
Published
1995-05-00
Pages
631-6
Language
English
Region
United States
NLM ID
7613461
Subset
IM
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