Functional sites involved in modulation of the GABAA receptor channel by the intravenous anesthetics propofol, etomidate and pentobarbital

Neuropharmacology

Volumn 105, Issue , 2016, Pages 207-214

  Maldifassi, Maria C ^a   Baur, Roland ^a   Sigel, Erwin ^a  

^a UNIVERSITY OF BERN   (Switzerland)

Author keywords

Anesthetics; Barbiturates; Chloride channels; Electrophysiology; GABAA receptors; Xenopus oocyte

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID A RECEPTOR ALPHA1; 4 AMINOBUTYRIC ACID A RECEPTOR ALPHA1BETA2GAMMA2; 4 AMINOBUTYRIC ACID A RECEPTOR BETA2; 4 AMINOBUTYRIC ACID A RECEPTOR GAMMA2; ETOMIDATE; PENTOBARBITAL; PROPOFOL; UNCLASSIFIED DRUG; INTRAVENOUS ANESTHETIC AGENT;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; EC50; NEUROMODULATION; NONHUMAN; POINT MUTATION; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN EXPRESSION; PROTEIN FUNCTION; PROTEIN SUBUNIT; ANIMAL; BINDING SITE; DRUG EFFECTS; ELECTROPHYSIOLOGY; GENETICS; MUTATION; OOCYTE; RAT; XENOPUS;

ANESTHETICS, INTRAVENOUS; ANIMALS; BINDING SITES; ELECTROPHYSIOLOGICAL PHENOMENA; ETOMIDATE; MUTATION; OOCYTES; PENTOBARBITAL; PROPOFOL; RATS; RECEPTORS, GABA-A; XENOPUS;

EID: 84955271623     PISSN: 00283908     EISSN: 18737064     Source Type: Journal    
DOI: 10.1016/j.neuropharm.2016.01.003     Document Type: Article

References (52)

1. A receptor Mol. Pharmacol. 65 2004 68 76
2. E.A. Barnard, P. Skolnick, R.W. Olsen, H. Möhler, W. Sieghart, G. Biggio, C. Braestrup, A.N. Bateson, and S.Z. Langer International Union of Pharmacology. XV. Subtypes of gamma-aminobutyric acidA receptors: classification on the basis of subunit structure and receptor function Pharmacol. Rev. 50 1998 291 313
3. S.W. Baumann, R. Baur, and E. Sigel Subunit arrangement of gamma aminobutyric acid type A receptors J. Biol. Chem. 276 2001 36275 36280
4. A receptors. Insight into the absolute arrangement J. Biol. Chem. 277 2002 46020 46025
5. A receptors J. Neurosci. 23 2003 11158 11166
6. A receptor of defined subunit composition and positioning: concatenation of five subunits FEBS Lett. 580 2006 1616 1620
7. D. Belelli, J.J. Lambert, J.A. Peters, K. Wafford, and P.J. Whiting The interaction of the general anesthetic etomidate with the gamma-aminobutyric acid type A receptor is influenced by a single amino acid Proc. Natl. Acad. Sci. U. S. A. 94 1997 11031 11036
8. A receptor Nat. Rev. Neurosci. 6 2005 565 575
9. H. Betz Ligand-gated ion channels in the brain: the amino acid receptor superfamily Neuron 5 1990 383 392
10. A receptors expressed in Xenopus oocytes Neuropharmacol 43 2002 695 700
11. A receptor J. Neurochem. 95 2005 1724 1731
12. A receptor J. Neurosci. 16 1996 5415 5424
13. 3 γ-aminobutyric acid type A receptors with [H]TDBzl-etomidate, a photoreactive etomidate analogue Biochemistry 51 2012 836 847
14. 2 γ-aminobutyric acid type A (GABAA) receptor J. Biol. Chem. 288 2013 19343 19357
15. A receptors Nat. Rev. Neurosci. 6 2005 215 229
16. S.J. Farrar, P.J. Whiting, T.P. Bonnert, and R.M. McKernan Stoichiometry of a ligand-gated ion channel determined by fluorescence energy transfer J. Biol. Chem. 274 1999 10100 10104
17. S.P. Fernandez, N. Karim, K.N. Mewett, M. Chebib, G.A. Johnston, and J.R. Hanrahan Flavan-3-ol esters: new agents for exploring modulatory sites on GABA(A) receptors Br. J. Pharmacol. 165 2012 965 977
18. 2 γ-aminobutyric acid type A receptors contribute equally and noncooperatively to modulation of channel gating Anesthesiology 116 2012 1235 1244
19. R.E. Hibbs, and E. Gouaux Principles of activation and permeation in an anion-selective Cys-loop receptor Nature 474 2011 54 60
20. AR) identified using a photoreactive propofol analog J. Biol. Chem. 289 2014 27456 27468
21. - interface J. Biol. Chem. 2015 10.1074
22. A receptor beta3 subunit FASEB J. 17 2003 250 262
23. A receptor anesthetic binding site at subunit interfaces by photolabeling with an etomidate analog J. Neurosci. 26 2006 11599 11605
24. G.D. Li, D.C. Chiara, J.B. Cohen, and R.W. Olsen Neurosteroids allosterically modulate binding of the anesthetic etomidate to gamma-aminobutyric acid type A receptors J. Biol. Chem. 284 2009 11771 11775
25. A) receptors J. Biol. Chem. 285 2010 8615 8620
26. A receptor channels Annu. Rev. Neurosci. 17 1994 569 602
27. A receptor β2 subunit critical for the actions of alcohols and anesthetics J. Pharmacol. Exp. Ther. 335 2010 600 606
28. A receptors by an antagonist of the high affinity benzodiazepine binding site Neuropharmacology 95 2015 459 467
29. S.J. Middendorp, R. Puthenkalam, R. Baur, M. Ernst, and E. Sigel Accelerated discovery of novel benzodiazepine ligands by experiment-guided virtual screening ACS Chem. Biol. 9 2014 1854 1859
30. P.S. Miller, and T.G. Smart Binding, activation, and modulation of Cys loop receptors Trends Pharmacol. Sci. 31 2010 161 174
31. F. Minier, and E. Sigel Positioning of the α-subunit isoforms confers a functional signature to γ-aminobutyric acid type A receptors Proc. Natl. Acad. Sci. U. S. A. 101 2004 7769 7774
32. A receptors: contrasting effects of alpha 1(S270) and beta 2(N265) point mutations Neuropharmacology 42 2002 337 345
33. R.W. Olsen, and W. Sieghart International Union of Pharmacology. LXX. Subtypes of gamma-aminobutyric acid (A) receptors: classification on the basis of subunit composition, pharmacology, and function Update. Pharmacol. Rev. 60 2008 243 260
34. A receptor research Synapse 21 1995 189 274
35. 2 subunit M4 segment is a determinant of gamma-aminobutyric acid type A receptor sensitivity to propofol Anesthesiology 107 2007 412 418
36. A receptors Anesthesiology 95 2001 123 131
37. W. Sieghart Structure and pharmacology of gamma-aminobutyric acidA receptor subtypes Pharmacol. Rev. 47 1995 181 233
38. A receptors: revived interest in the development of subtype-selective drugs Curr. Med. Chem. 5 2005 217 242
39. 2 gamma-aminobutyric acid(A) receptors J. Neurochem. 80 2002 140 148
40. 2 BMC Pharmacol. 3 2003 13
41. E. Sigel Properties of single sodium channels translated by Xenopus oocytes after injection with messenger ribonucleic acid J. Physiol. Lond 386 1987 73 90
42. A receptors on channel function Neuron 5 1990 703 711
43. A receptors Trends Pharmacol. Sci. 18 1997 425 429
44. E. Sigel, and F. Minier The Xenopus oocyte: system for the study of functional expression and modulation of proteins Mol. Nutr. Food Res. 49 2005 228 234
45. A receptors Curr. Top. Med. Chem. 11 2011 241 246
46. A receptors J. Biol. Chem. 287 2012 40224 40231
47. D.S. Stewart, D.W. Pierce, M. Hotta, A.T. Stern, and S.A. Forman Mutations at beta N265 in γ-aminobutyric acid type A receptors alter both binding affinity and efficacy of potent anesthetics PLoS One 9 2014 e111470
48. A receptor subtype J. Neurosci. 17 1997 2728 2737
49. A receptors via two distinct and separable mechanisms Nat. Neurosci. 12 2000 1274 1281
50. P.B. Wingrove, K.A. Wafford, C. Bain, and P.J. Whiting The modulatory action of loreclezole at the gamma-aminobutyric acid type A receptor is determined by a single amino acid in the beta2 and beta3 subunit Proc. Natl. Acad. Sci. U. S. A. 91 1994 4569 4573
51. A receptors identified by photolabeling Nat. Chem. Biol. 9 2013 715 720
52. A. Zeller, M. Arras, R. Jurd, and U. Rudolph Identification of a molecular target mediating the general anesthetic actions of pentobarbital Mol. Pharmacol. 71 2007 852 859