![[Feedback]](/icons/banner/feedbackACT.gif){kind=icon}
![[For Subscribers]](/icons/banner/subscriberACT.gif){kind=icon}
![[Archive]](/icons/banner/archiveACT.gif){kind=icon}
![[Search]](/icons/banner/searchACT.gif){kind=icon}
![[Contents]](/icons/banner/tocACT.gif){kind=icon}
|
|
|
|
|
||
A Slany, J Zezula, V Tretter and W Sieghart
Department of Biochemical Psychiatry, University Clinic for Psychiatry, Vienna, Austria.
Human embryonic kidney 293 cells transiently transfected with beta 3 subunits of gamma-aminobutyric acid type A receptors from the rat exhibited a specific high affinity binding for [35S]t- butylbicyclophosphorothionate (TBPS) that could be inhibited by pentobarbital, etazolate, (+)-etomidate, alphaxalone, propofol, chlormethiazole, and Ro 5-4864. The potency of these compounds for inhibition of [35S]TBPS binding was similar in membranes from beta 3 subunit-transfected human embryonic kidney 293 cells and in cerebellar membranes. In contrast to maximally inhibiting concentrations of unlabeled TBPS or picrotoxin, which caused a monophasic and rather slow dissociation of [35S]TBPS, maximally inhibiting concentrations of pentobarbital, etazolate, alphaxalone, propofol, chlormethiazole, and Ro 5-4864 accelerated the dissociation of [35S]TBPS from beta 3 subunit- containing membranes. Immunoaffinity chromatography and Western blot analysis with subunit-specific antibodies indicated that other endogenous subunits possibly present in these cells were not associated with beta 3 subunits. These results appear to indicate that most of the allosteric binding sites present on gamma-aminobutyric acid type A receptors can be formed by the beta subunit of these receptors. Homo- oligomeric beta 3 receptors therefore are an excellent model system for the structural investigation of gamma-aminobutyric acid type A receptors.
This article has been cited by other articles:
|
|
 |
|
  K. Mizuta, D. Xu, Y. Pan, G. Comas, J. R. Sonett, Y. Zhang, R. A. Panettieri Jr., J. Yang, and C. W. Emala Sr. GABAA receptors are expressed and facilitate relaxation in airway smooth muscle Am J Physiol Lung Cell Mol Physiol, June 1, 2008; 294(6): L1206 - L1216. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 H. L. Payne, W. M. Connelly, J. H. Ives, R. Lehner, B. Furtmuller, W. Sieghart, P. Tiwari, J. M. Lucocq, G. Lees, and C. L. Thompson GABAA {alpha}6-Containing Receptors Are Selectively Compromised in Cerebellar Granule Cells of the Ataxic Mouse, Stargazer J. Biol. Chem., October 5, 2007; 282(40): 29130 - 29143. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 L. Chen, K. A. Durkin, and J. E. Casida Structural model for {gamma}-aminobutyric acid receptor noncompetitive antagonist binding: Widely diverse structures fit the same site PNAS, March 28, 2006; 103(13): 5185 - 5190. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 Z. Nusser, L. M. Kay, G. Laurent, G. E. Homanics, and I. Mody Disruption of GABAA Receptors on GABAergic Interneurons Leads to Increased Oscillatory Power in the Olfactory Bulb Network J Neurophysiol, December 1, 2001; 86(6): 2823 - 2833. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
T. Klausberger, K. Fuchs, B. Mayer, N. Ehya, and W. Sieghart GABAA Receptor Assembly. IDENTIFICATION AND STRUCTURE OF gamma 2 SEQUENCES FORMING THE INTERSUBUNIT CONTACTS WITH alpha 1 AND beta 3 SUBUNITS J. Biol. Chem., March 17, 2000; 275(12): 8921 - 8928. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
K. Kannenberg, M. T. Schaerer, K. Fuchs, W. Sieghart, and E. Sigel A Novel Serine Kinase with Specificity for beta 3-Subunits Is Tightly Associated with GABAA Receptors J. Biol. Chem., July 23, 1999; 274(30): 21257 - 21264. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
E. Bencsits, V. Ebert, V. Tretter, and W. Sieghart A Significant Part of Native gamma -Aminobutyric AcidA Receptors Containing alpha 4 Subunits Do Not Contain gamma or delta Subunits J. Biol. Chem., July 9, 1999; 274(28): 19613 - 19616. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 M. Jechlinger, R. Pelz, V. Tretter, T. Klausberger, and W. Sieghart Subunit Composition and Quantitative Importance of Hetero-oligomeric Receptors: GABAA Receptors Containing alpha 6 Subunits J. Neurosci., April 1, 1998; 18(7): 2449 - 2457. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 A. Buhr, M. T. Schaerer, R. Baur, and E. Sigel Residues at Positions 206 and 209 of the alpha 1 Subunit of gamma -Aminobutyric AcidA Receptors Influence Affinities for Benzodiazepine Binding Site Ligands Mol. Pharmacol., October 1, 1997; 52(4): 676 - 682. [Abstract] [Full Text]
|
|
|
|
|
|
E. Hedblom and E. F. Kirkness A Novel Class of GABAA Receptor Subunit in Tissues of the Reproductive System J. Biol. Chem., June 13, 1997; 272(24): 15346 - 15350. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
V. Tretter, N. Ehya, K. Fuchs, and W. Sieghart Stoichiometry and Assembly of a Recombinant GABAA Receptor Subtype J. Neurosci., April 15, 1997; 17(8): 2728 - 2737. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
T. Klausberger, N. Ehya, K. Fuchs, T. Fuchs, V. Ebert, I. Sarto, and W. Sieghart Detection and Binding Properties of GABAA Receptor Assembly Intermediates J. Biol. Chem., May 4, 2001; 276(19): 16024 - 16032. [Abstract] [Full Text] [PDF]
|
|
 |
 |
 |
|
 |
 |
 |
