A structural determinant of desensitization and allosteric regulation by pentobarbitone of the GABA(A) receptor

Journal of Membrane Biology

Volumn 155, Issue 2, 1997, Pages 157-166

  Birnir, B ^a   Tierney, M L ^b   Dalziel, J E ^a   Cox, G B ^a   Gage, P W ^a  

^a Biology and Environment   (Australia)

^b MRC LABORATORY OF MOLECULAR BIOLOGY   (United Kingdom)

Author keywords

Baculovirus; Expression; GABA(A) subunit; Ligand gated; M2; Patch clamp

Indexed keywords

4 AMINOBUTYRIC ACID; 4 AMINOBUTYRIC ACID A RECEPTOR; PENTOBARBITAL; PROTEIN SUBUNIT;

ALLOSTERISM; ANIMAL CELL; ARTICLE; BACULOVIRUS; CONFORMATIONAL TRANSITION; CONTROLLED STUDY; ELECTROPHYSIOLOGY; GENE EXPRESSION; GENE TRANSFER; HUMAN; INSECT; MUTATION; NONHUMAN; PATCH CLAMP; RECEPTOR DOWN REGULATION; SITE DIRECTED MUTAGENESIS;

ALLOSTERIC REGULATION; AMINO ACID SEQUENCE; BACULOVIRIDAE; DOSE-RESPONSE RELATIONSHIP, DRUG; GAMMA-AMINOBUTYRIC ACID; HUMANS; MOLECULAR SEQUENCE DATA; MUTAGENESIS, SITE-DIRECTED; PATCH-CLAMP TECHNIQUES; PENTOBARBITAL; RECEPTORS, GABA;

EID: 0031039647     PISSN: 00222631     EISSN: None     Source Type: Journal    
DOI: 10.1007/s002329900167     Document Type: Article

References (43)

1. A receptor needs two homologous domains of the β-subunit for activation by GABA but not by pentobarbital. Nature 366:565-569
2. A channels in rat dentate gyms. J. Membrane Biol. 142:93-102
3. A receptor expresed in Sf9 cells under optimized conditions. J. Membrane Biol. 148:193-202
4. Cash, D.J., Subbarao, K. 1988. Different effects of pentobarbital on two γ-aminobutyrate receptors from rat brain: channel opening, desensitization, and an additional conformational change. Biochemistry 27:4580-4590
5. Connors, B.W. 1981. A comparison of the effects of pentobarbital and diphenylhydantoin on the GABA sensitivity and excitability of adult sensory ganglion cells. Brain Res. 207:357-369
6. 1 cDNA: a GABA receptor subunit highly expressed in the retina. Proc. Natl. Acad. Sci USA 88:2673-2677
7. Dahlquist, F.W. 1978. The meaning of Scatchard and Hill plots. Methods Enzymol. 48:270-299
8. Devillers Thiery, A., Galzi, J.L., Eisele, J.L., Bertrand, S., Bertrand, D., Changeux, J.P. 1993. Functional architecture of the nicotinic acetylcholine receptor: a prototype of ligand-gated ion channels. J. Membrane Biol. 136:97-112
9. ffrench Constant, R.H., Rocheleau, T.A., Steichen, J.C., Chalmers, A.E. 1993. A point mutation in a Drosophila GABA receptor confers insecticide resistance. Nature 363:449-451
10. Filatov, G.N., White, M.M. (1995. The role of conserved leucines in the M2 domain of the acetylcholine receptor in channel gating. Mol. Pharmacol 48:379-384
11. Forman, S.A., Miller, k.W., Yellen, G. 1995. A discrete site for general anesthetics on a postsynaptic receptor. Mol. Pharmacol 48:574-581
12. Franks, N.P., Lieb, W.R. 1994. Molecular and cellular mechanisms of general anaesthesia. Nature 367:607-614
13. Gage, P.W., Robertson, B. 1985. Prolongation of inhibitory postsynaptic currents by pentobarbitone, halothane and ketamine in CA1 pyramidal cells in rat hippocampus. Br. J. Pharmacol 85:675-681
14. A channel that abolish block by picrotoxin. Receptors and Channels 3:13-20
15. Hamill, O.P., Marty, A., Neher, E., Sakmann, B., Sigworth, F.J. 1981. Improved patch-clamp techniques for high resolution current recording from cells and cell-free membrane patches. Pfluegers Arch. 391:85-100
16. Imoto, K., Melhfessel, L.C., Sakmann, B., Mishina, M., Mori, Y., Konno, T., Fukuda, K., Kurasaki, M., Bujo, H., Fujita, Y., Numa, S. 1986. Location of a δ-subunit region determining ion transport through the acetylcholine receptor channel. Nature 324:670-674
17. A channel responses to brief agonist pulses. Neuron 15:181-191
18. Karlin, A., Akabas, M.H. 1995. Toward a structural basis for the function of nicotinic acetylcholine receptors and their cousins. Neuron 15:1231-1244
19. Kawamoto, S., Onishi, H., Hattori, S., Miyagi, Y., Amaya, Y., Mishina, M., Okuda, K. 1991. Functional expression of the α1 subunit of the AMPA-selective glutamate receptor channel, using a baculovirus system. Biochem. Biophys. Res. Commun. 181:756-763 IS
20. Labarca, C., Nowak, M.W., Zhang, H., Tang, L., Deshpande, P., Lester, H.A. 1995. Channel gating governed symmetrically by conserved leucine residues in the M2 domain of nicotinic receptors. Nature 376:514-516
21. Leonard, R.J., Labarca, C.G., Charnet, P., Davidson, N., Lester, H.A. 1988. Evidence that the M2 membrane-spanning region lines the ion channel pore of the nicotinic receptor. Science 242:1578-1581
22. A receptor channel of mouse spinal neurones in culture. J. Physiol. Lond 417:483-500
23. Miller, C. 1989. Genetic manipulation of ion channels: a new approach to structure and mechanism. Neuron 2:1195-1205
24. Nicoll, R.A., Eccles, J.C., Oshima, T., Rubia, F. 1975. Prolongation of hippocampal inhibitory postsynaptic potentials by barbiturates. Nature 258:625-627
25. Oh, D.J., Dichter, M.A. 1992. Desensitization of GABA-induced currents in cultured rat hippocampal neurons. Neuroscience 49:571-76
26. Parker, I., Gundersen, C.B., Miledi, R. 1986. Actions of pentobarbital on rat brain receptors expressed in Xenopus oocytes. J. Neurosci. 6:2290-2297
27. Polenzani, L., Woodward, R.M., Miledi, R. 1991. Expression of mammalian γ-aminobutyric acid receptors with distinct pharmacology in Xenopus oocytes. Proc. Natl. Acad. Sci. USA 88:4318-432
28. A receptor research. Synapse 21:189-274
29. Revah, F., Bertrand, D., Galzi, J.L., Devillers Thiery, A., Mulle, C., Hussy, N., Bertrand, S., Ballivet, M., Changeux, J.P. 1991. Mutations in the channel domain after desensitization of a neuronal nicotinic receptor. Nature 353:846-849
30. 1 subunits. FEBS Lett 244:361-364
31. A receptors. Trends. Pharmacol Sci. 16:162-168
32. A receptor: a chemically gated ion channel. Biochem. J. 249:21-32
33. Study, R.E., Barker, j.L. 1981. Diazepam and (-)-pentobarbital: fluctuation analysis reveals different mechanisms for potentiation of γ-aminobutyric acid responses in cultured central neurons. Proc. Natl. Acad. Sci. USA 78:7180-7184
34. A receptor/chloride channel complex in anesthesia. Anesthesiology 78:757-776
35. Taylor, J.W., Ott, J., Eckstein, F. 1985. The rapid generation of oligonucleotide-directed mutations at high frequency using phosphorothioate-modified DNA. Nucleic Acids Res. 13:8765-8785
36. Ticku, M.K., Rastogi, S.K., Thyagarajan, R. 1985. Separate site(s) of action of optical isomers of 1-methyl-5-phenyl-5-propylbarbituric acid with opposite pharmacological activities at the GABA receptor complex. Eur. J. Pharmacol. 112:1-9
37. 1 receptors. J. Membrane Biol. 154:11-21
38. Tossman, U., Jonsson, G., Ungerstedt, U. 1986. Regional distribution and extracellular levels of amino acids in rat central nervous system. Acta Physiol. Scand. 127:533-545
39. A receptor channels from mouse spinal cord meurones in culture. J. Physiol. 445:97-106
40. Unwin, N. 1995. Acetylcholine receptor channel imaged in the open state. Nature 373:37-43
41. Villarroel, A., Herlitze, S., Witzemann, V., Koenen, M., Sakmann, B. 1992. Asymmetry of the rat acetylcholine receptor subunits in the narrow region of the pore. Proc. R. Soc. Lond B. 249:317-324
42. Willow, M., Johnston, G.A. 1980. Enhancement of GABA binding by pentobarbitone. Neurosci. Lett. 18:323-327
43. 3 subunit. Proc. Natl. Acad. Sci. USA 91:4569-4573