Context dependent benzodiazepine modulation of GABAA receptor opening frequency

Current Neuropharmacology

Volumn 8, Issue 1, 2010, Pages 10-17

  Bianchi, Matt T ^a  

^a MASSACHUSETTS GENERAL HOSPITAL   (United States)

Author keywords

Affinity; Extra synaptic; Ion channel; Mechanism; Synaptic

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; BENZODIAZEPINE;

GABAERGIC SYSTEM; RECEPTOR AFFINITY; RECEPTOR BINDING; REVIEW; SYNAPTIC TRANSMISSION;

EID: 77950232504     PISSN: 1570159X     EISSN: None     Source Type: Journal    
DOI: 10.2174/157015910790909467     Document Type: Review

References (56)

1. Bianchi, M.T. and Macdonald, R.L. (2001) Agonist Trapping by GABAA Receptor Channels. J. Neurosci., 21(23), 9083-9091
2. Bianchi, M.T. and Macdonald, R.L. (2001) Mutation of the 9' leucine in the GABA(A) receptor gamma2L subunit produces an apparent decrease in desensitization by stabilizing open states without altering desensitized states. Neuropharmacology, 41(6), 737-744
3. Bianchi, M.T., Song, L., Zhang, H., and Macdonald, R.L. (2002) Two different mechanisms of disinhibition produced by GABAA receptor mutations linked to epilepsy in humans. J. Neurosci., 22(13), 5321-5327
4. Bianchi, M.T., Botzolakis, E.J., Haas, K.F., Fisher, J.L. and Macdonald, R.L. (2007) Microscopic kinetic determinants of macroscopic currents: insights from coupling and uncoupling of GABAA receptor desensitization and deactivation. J. Physiol., 584(Pt 3), 769-787
5. Bianchi, M.T., Botzolakis, E.J. Lagrange, A.H. and Macdonald, R.L. (2009) Benzodiazepine modulation of GABA(A) receptor opening frequency depends on activation context: a patch clamp and simulation study. Epilepsy Res., 85(2-3), 212-220
6. Campo-Soria, C., Chang, Y. and Weiss, D.S. (2006.) Mechanism of action of benzodiazepines on GABAA receptors. Br. J. Pharmacol., 148(7), 984-990
7. Choh, D.W., Farb, D.H. and Fischbach, G.D. (1977) Chlordiazepoxide selectively augments GABA action in spinal cord cell cultures. Nature, 269(5626), 342-344
8. Colquhoun, D. (1998) Binding, gating, affinity and efficacy: the interpretation of structure-activity relationships for agonists and of the effects of mutating receptors. Br. J. Pharmacol., 125(5) 924-947
9. Cortelli, P., Avallone, R. Baraldi, M. Zeneroli, M.L. Mandrioli, J. Corsi, L. Riva, R., Tinuper, P., Lugaresi, E. Baruzzi, A. and Montagna, P. (2005) Endozepines in recurrent stupor. Sleep Med. Rev., 9(6), 477-487
10. Crestani, F., Martin, J.R., Mohler, H. and Rudolph, U. (2000) Mechanism of action of the hypnotic zolpidem in vivo. Br. J. Pharmacol., 131(7), 1251-1254
11. Downing, S.S., Lee, Y.T. Farb, D..H and Gibbs, T.T. (2005) Benzodiazepine modulation of partial agonist efficacy and spontaneously active GABA(A) receptors supports an allosteric model of modulation. Br. J. Pharmacol., 145(7), 894-906.
12. Ebert, B., Wafford, K.A. and Deacon, S. (2006) Treating insomnia: Current and investigational pharmacological approaches. Pharmacol. Ther., 112(3), 612-629
13. Farrant, M. and Nusser, Z. (2005) Variations on an inhibitory theme: phasic and tonic activation of GABA(A) receptors. Nat. Rev. Neurosci., 6(3), 215-229
14. Feng, H.J., Botzolakis, E.J.and Macdonald, R.L. (2009) Context-dependent modulation of alphabetagamma and alphabetadelta GABA(A) receptors by penicillin: Implications for phasic and tonic inhibition. Neuropharmacology., 56(1), 161-173
15. Ghansah, E. and Weiss, D.S. (1999) Benzodiazepines do not modulate desensitization of recombinant alpha1beta2gamma2 GABA(A) receptors. Neuroreport, 10(4), 817-821
16. Glykys, J. and Mody, I. (2007) Activation of GABAA receptors: views from outside the synaptic cleft. Neuron, 56(5), 763-770
17. Haas, K.F. and Macdonald, R.L. (1999) GABAA receptor subunit gamma2 and delta subtypes confer unique kinetic properties on recombinant GABAA receptor currents in mouse fibroblasts. J. Physiol., 514(Pt 1), 27-45.
18. Hajos, N., Nusser, Z., Rancz, E.A. Freund, T.F.and Mody, I. (2000) Cell type- and synapse-specific variability in synaptic GABAA receptor occupancy. Eur. J. Neurosci., 12, 810-818
19. Jones-Davis, D.M., Song, L., Gallagher, M.J. and Macdonald, R.L. (2005) Structural determinants of benzodiazepine allosteric regulation of GABA(A) receptor currents. J. Neurosci., 25(35), 8056-8065
20. Jones, M.V. and Westbrook, G.L. (1995) Desensitized states prolong GABAA channel responses to brief agonist pulses. Neuron, 15(1), 181-191
21. Jones, M.V. and Westbrook, G.L. (1996) The impact of receptor desensitization on fast synaptic transmission. Trends Neurosci., 19(3), 96-101.
22. Jones, M.V., Sahara, Y. Dzubay, J.A. and Westbrook, G.L. (1998) Defining affinity with the GABAA receptor. J. Neurosci., 18(21) 8590-8604
23. Kloda, J.H. and Czajkowski, C. (2007) Agonist-, antagonist-, and benzodiazepine-induced structural changes in the alpha1 Met113-Leu132 region of the GABAA receptor. Mol. Pharmacol., 71(2), 483-493
24. Kopp, C., Rudolph, U., Keist, R and Tobler, I. (2003) Diazepaminduced changes on sleep and the EEG spectrum in mice: role of the alpha3-GABA(A) receptor subtype. Eur. J. Neurosci., 17(10), 2226-2230
25. Kopp, C., Rudolph, U., Low, K. and Tobler, I. (2004) Modulation of rhythmic brain activity by diazepam: GABA(A) receptor subtype and state specificity. Proc. Natl. Acad. Sci. U S A, 101(10), 3674-3679
26. Kullmann, D.M., Ruiz, A. Rusakov, D.M., Scott, R., Semyanov, A., and Walker, M.C. (2005) Presynaptic, extrasynaptic and axonal GABAA receptors in the CNS: where and why? Prog. Biophys. Mol. Biol., 87(1). 33-46.
27. Lagrange, A.H., Botzolakis, E.J., and. Macdonald, R.L. (2007) Enhanced macroscopic desensitization shapes the response of alpha4 subtype-containing GABAA receptors to synaptic and extrasynaptic GABA. J. Physiol., 578(Pt 3), 655-676
28. Lavoie, A.M. and Twyman, R.E. (1996) Direct evidence for diazepam modulation of GABAA receptor microscopic affinity. Neuropharmacology, 35(9-10), 1383-1392
29. Low, K., Crestani, F., Keist, R., Benke, D. Brunig, I., Benson, J.A., Fritschy, J.M., Rulicke, T., Bluethmann, H., Mohler, H. and Rudolph, U. (2000) Molecular and neuronal substrate for the selective attenuation of anxiety. Science, 290(5489), 131-134
30. Macdonald, R. and Barker, J.L. (1978) Benzodiazepines specifically modulate GABA-mediated postsynaptic inhibition in cultured mammalian neurones. Nature, 271(5645), 563-564
31. MacDonald, R.L., Rogers, C.J. and Twyman, R.E. (1989) Barbiturate regulation of kinetic properties of the GABAA receptor channel of mouse spinal neurones in culture. J. Physiol., 417, 483-500.
32. Maksay, G., Thompson, S.A. and Wafford, K.A. (2000) Allosteric modulators affect the efficacy of partial agonists for recombinant GABA(A) receptors. Br. J. Pharmacol., 129(8), 1794-1800
33. McKernan, R.M. and. Whiting, P.J. (1996) Which GABAA-receptor subtypes really occur in the brain? Trends Neurosci., 19(4), 139-143
34. Mehta, A.K. and Ticku, M.K. (1999) An update on GABAA receptors. Brain Res Brain Res. Rev., 29(2-3), 196-217.
35. Mercik, K., Piast, M. and Mozrzymas, J.W. (2007) Benzodiazepine receptor agonists affect both binding and gating of recombinant alpha1beta2gamma2 gamma-aminobutyric acid-A receptors. Neuroreport, 18(8), 781-785
36. Mody, I. and Pearce, R.A. (2004) Diversity of inhibitory neurotransmission through GABA(A) receptors. Trends Neurosci., 27(9), 569-575
37. Morris, H.V., Dawson, G.R., Reynolds, D.S., Atack, J.R. and Stephens, D.N. (2006) Both alpha2 and alpha3 GABAA receptor subtypes mediate the anxiolytic properties of benzodiazepine site ligands in the conditioned emotional response paradigm. Eur. J. Neurosci., 23(9), 2495-2504
38. Mozrzymas, J.W., Barberis, A., Mercik, K. and Zarnowska, E.D. (2003) Binding sites, singly bound states, and conformation coupling shape GABA-evoked currents. J. Neurophysiol., 89(2), 871-883
39. Mozrzymas, J.W., Wojtowicz, T. Piast, M., Lebida, K., Wyrembek, P. and Mercik, K. (2007) GABA transient sets the susceptibility of mIPSCs to modulation by benzodiazepine receptor agonists in rat hippocampal neurons. J. Physiol., 585(Pt 1), 29-46.
40. Neelands, T.R., Fisher, J.L. Bianchi, M. and Macdonald, R.L. (1999) Spontaneous and gamma-aminobutyric acid (GABA)-activated GABA(A) receptor channels formed by epsilon subunitcontaining isoforms. Mol. Pharmacol., 55(1).168-178
41. Nusser, Z., Naylor, D and Mody, I. (2001) Synapse-specific contribution of the variation of transmitter concentration to the decay of inhibitory postsynaptic currents. Biophys. J., 80(3), 1251-1261
42. Nusser, Z. and Mody, I. (2002) Selective modulation of tonic and phasic inhibitions in dentate gyrus granule cells. J. Neurophysiol., 87(5), 2624-2628
43. Overstreet, L.S., Jones, M.V. and Westbrook, G.L. (2000) Slow desensitization regulates the availability of synaptic GABA(A) receptors. J. Neurosci., 20(21), 7914-7921
44. Perrais, D. and Ropert, N. (1999) Effect of zolpidem on miniature IPSCs and occupancy of postsynaptic GABAA receptors in central synapses. J. Neurosci., 19(2), 578-588
45. Poncer, J.C., Durr, R Gahwiler, B.H., and Thompson, S.M. (1996) Modulation of synaptic GABAA receptor function by benzodiazepines in area CA3 of rat hippocampal slice cultures. Neuropharmacology, 35(9-10), 1169-1179
46. Rogers, C.J., Twyman, R.E. and Macdonald, R.L. (1994) Benzodiazepine and beta-carboline regulation of single GABAA receptor channels of mouse spinal neurones in culture. J. Physiol., 475(1), 69-82.
47. Rudolph, U. F. Crestani, D., Benke, I., Brunig, J.A., Benson, J.M. Fritschy, J.R. Martin, H. Bluethmann, and Mohler, H. (1999) Benzodiazepine actions mediated by specific gamma-aminobutyric acid(A) receptor subtypes. Nature, 401(6755), 796-800.
48. Rusch, D. and Forman, S.A. (2005) Classic benzodiazepines modulate the open-close equilibrium in alpha1beta2gamma2L gamma-aminobutyric acid type A receptors. Anesthesiology, 102(4), 783-792
49. Semyanov, A., Walker, M.C., Kullmann, D.M. and Silver, R.A. (2004) Tonically active GABA A receptors: modulating gain and maintaining the tone. Trends Neurosci., 27(5), 262-269
50. Steinbach, J.H. and Akk, G. (2001) Modulation of GABA(A) receptor channel gating by pentobarbital. J. Physiol., 537(Pt 3), 715-733
51. Thompson, S.A., Smith, M.Z., Wingrove, P.B., Whiting, P.J. and Wafford, K.A. (1999) Mutation at the putative GABA(A) ion-channel gate reveals changes in allosteric modulation. Br. J. Pharmacol., 127(6), 1349-1358
52. Tobler, I., Kopp., C. Deboer, T. and Rudolph, U. (2001) Diazepaminduced changes in sleep: role of the alpha 1 GABA(A) receptor subtype. Proc, Natl. Acad .Sci. U S A, 98(11), 6464-6469
53. Twyman, R.E., Rogers, C.J. and Macdonald, R.L. (1989) Differential regulation of gamma-aminobutyric acid receptor channels by diazepam and phenobarbital. Ann. Neurol., 25(3), 213-220
54. van Rijnsoever, Tauber C., M., Choulli, M.K. Keist, R. Rudolph, U.. Mohler, H Fritschy, J.M. and Crestani, F. (2004) Requirement of alpha5-GABAA receptors for the development of tolerance to the sedative action of diazepam in mice. J. Neurosci., 24(30), 6785-6790
55. Walker, M.C. and Semyanov, A. (2008) Regulation of excitability by extrasynaptic GABA(A) receptors. Results Probl. Cell Differ., 44, 29-48.
56. Williams, D.B. and Akabas, M.H. (2000) Benzodiazepines induce a conformational change in the region of the gamma-aminobutyric acid type A receptor alpha(1)-subunit M3 membrane-spanning segment. Mol. Pharmacol., 58(5), 1129-1136