Activation of single heteromeric GABAA receptor ion channels by full and partial agonists

Journal of Physiology

Volumn 557, Issue 2, 2004, Pages 389-413

  Mortensen, Martin ^a   Kristiansen, Uffe ^b   Ebert, Bjarke ^c   Frølund, Bente ^b   Krogsgaard Larsen, Povl ^b   Smart, Trevor G ^a  

^a UNIVERSITY COLLEGE LONDON   (United Kingdom)

^b UNIVERSITY OF COPENHAGEN   (Denmark)

^c H LUNDBECK A S   (Denmark)

Author keywords

[No Author keywords available]

Indexed keywords

3 HYDROXY 5 (4 PIPERIDYL)ISOXAZOLE; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID A RECEPTOR BLOCKING AGENT; 4 AMINOBUTYRIC ACID A RECEPTOR STIMULATING AGENT; 4 IMIDAZOLEACETIC ACID; 4 PIPERIDINESULFONIC ACID; 4,5,6,7 TETRAHYDROISOXAZOLO[4,5 C]PYRIDIN 3 OL; ARECAIDINE; COMPLEMENTARY DNA; ION CHANNEL; ISONIPECOTIC ACID; ISOTHIAZOLE DERIVATIVE; 4 AMINOBUTYRIC ACID; 4 AMINOBUTYRIC ACID A RECEPTOR ALPHA1; 4 AMINOBUTYRIC ACID A RECEPTOR BETA2; 4 AMINOBUTYRIC ACID A RECEPTOR GAMMA2; GABOXADOL;

ARTICLE; CELL CULTURE; CONCENTRATION (PARAMETERS); CONCENTRATION RESPONSE; CONTROLLED STUDY; ELECTROPHYSIOLOGY; ELECTROPORATION; EMBRYO; GENE CONSTRUCT; HUMAN; HUMAN CELL; ION CONDUCTANCE; KIDNEY CELL; MEMBRANE CURRENT; PATCH CLAMP; PRIORITY JOURNAL; RECEPTOR BINDING; STATISTICAL ANALYSIS; STATISTICAL SIGNIFICANCE; CHANNEL GATING; CONDUCTANCE; DRUG EFFECT; DRUG EFFICACY; HEK293 CELL LINE; PROTEIN EXPRESSION; RECEPTOR DOWN REGULATION;

CELLS, CULTURED; DNA, COMPLEMENTARY; EMBRYO; GABA AGONISTS; HUMANS; ION CHANNEL GATING; ION CHANNELS; KINETICS; PATCH-CLAMP TECHNIQUES; RECEPTORS, GABA-A; TRANSFECTION;

EID: 2542471956     PISSN: 00223751     EISSN: None     Source Type: Journal    
DOI: 10.1113/jphysiol.2003.054734     Document Type: Article

References (50)

1. A receptor needs two homologous domains of the β-subunit for activation by GABA but not by pentobarbital. Nature 366; 565-569.
2. 2S subunits produce unique ion channels with dissimilar single- channel properties. J Neurosci 13, 1429-1440.
3. Barker JL & Mathers DA (1981). GABA analogues activate channels of different duration on cultured mouse spinal neurons. Science 212, 358-361.
4. Baumann SW, Baur R & Sigel E (2001). Subunit arrangement of gamma-aminobutyric acid type A receptors. J Biol Chem 276, 36275-36280.
5. A receptor: evidence for a b-strand. J Neurosci 19, 4847-4854.
6. A receptor beta 2 Tyr97 and Leu99 line the GABA-binding site. Insights into mechanisms of agonist and antagonist actions. J Biol Chem 277, 2931-2937.
7. Burkat PM, Yang J & Gingrich KJ (2001). Dominant gating governing transient GABA (A) receptor activity: a first latency and Po/o analysis. J Neurosci 21, 7026-7036.
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, 924-947.
9. Colquhoun D & Hawkes AG (1990). Stochastic properties of ion channel openings and bursts in a membrane patch that contains two channels: evidence concerning the number of channels present when a record containing only single openings is observed. Proc R Soc Lond B Biol Sci 240, 453-477.
10. Colquhoun D, Hatton CJ & Hawkes AG (2003). The quality of maximum likelihood estimates of ion channel rate constants. J Physiol 547, 699-728.
11. Colquhoun D & Sakmann B (1985). Fast events in single-channel currents activated by acetylcholine and its analogues at the frog muscle end-plate. J Physiol 369, 501-557.
12. Del Castillo & Katz B (1957). Interaction at end-plate receptors between different choline derivatives. Proc R Soc Lond B Biol Sci 146, 369-381.
13. A receptors. Bioorg Med Chem Lett 11, 1573-1577.
14. Ebert B, Wafford KA, Whiting PJ, Krogsgaard-Larsen P & Kemp JA (1994). Molecular pharmacology of γ-aminobutyric acid type A receptor agonists and partial agonists in oocytes injected with different α, β, and γ receptor subunit combinations. Mol Pharmacol 46, 957-963.
15. A channel conductance increased by diazepam. Nature 388, 71-75.
16. Eghbali M, Gage PW & Birnir B (2000). Pentobarbital modulates γ-aminobutyric acid-activated single-channel conductance in rat cultured hippocampal neurons. Mol Pharmacol 58, 463-469.
17. A antagonists: synthesis, pharmacology, and molecular modeling. J Med Chem 45, 2454-2468.
18. Hadingham KL, Wingrove P, Le Bourdelles B, Palmer KJ, Ragan CI & Whiting PJ (1993a). Cloning of cDNA sequences encoding human alpha 2 and alpha 3 gamma-aminobutyric acidA receptor subunits and characterization of the benzodiazepine pharmacology of recombinant alpha 1-, alpha 2-, alpha 3-, and alpha 5-containing human gamma-aminobutyric acidA receptors. Mol Pharmacol 43, 970-975.
19. Hadingham KL, Wingrove PB, Wafford KA, Bain C, Kemp JA, Palmer KJ, Wilson AW, Wilcox AS, Sikela JM, Ragan CI & Whiting PJ (1993b). Role of the b subunit in determining the pharmacology of human y-aminobutyric acid type A receptors. Mol Pharmacol 44, 1211-1218.
20. Hamill OP, Bormann J & Sakmann B (1983). Activation of multiple-conductance state chloride channels in spinal neurones by glycine and GABA. Nature 305, 805-808.
21. 5 subunit are crucial for receptor function. J Neurochem 75, 1746-1753.
22. Hatton CJ, Shelley C, Brydson M, Beeson D & Colquhoun D (2003). Properties of the human muscle nicotinic receptor, and of the slow-channel myasthenic syndrome mutant eL221F, inferred from maximum likelihood fits. J Physiol 547, 729-760.
23. A receptor pore-lining M2 segment. Nat Neurosci 4, 477-485.
24. Jackson MB, Lecar H, Mathers DA & Barker JL (1982). Single channel currents activated by γ-aminobutyric acid, muscimol, and (-)-pentobarbital in cultured mouse spinal neurons. J Neurosci 2, 889-894.
25. A channel responses to brief agonist pulses. Neuron 15, 181-191.
26. A receptor. Nature 421, 272-275.
27. Kier LB & Truitt EB Jr (1970). Molecular orbital studies on the conformation of γ-aminobutyric acid and muscimol. Experientia 26, 988-989.
28. A receptors. Prog Neurobiol 67, 113-159.
29. - channels in embryonic rat olfactory bulb neurons. Mol Pharmacol 48, 268-279.
30. A receptor ligand, 4-PIOL, on cultured hippocampal neurones. Br J Pharmacol 104, 85-90.
31. Krogsgaard-Larsen P (1988). GABA synaptic mechanisms: stereochemical and conformational requirements. Med Res Rev 8, 27-56.
32. A receptor main conductance state of mouse spinal cord neurones in culture. J Physiol 410, 479-499.
33. Mathers DA (1985). Spontaneous and GABA-induced single channel currents in cultured murine spinal cord neurons. Can J Physiol Pharmacol 63, 1228-1233.
34. Mistry DK & Hablitz JJ (1990). Activation of subconductance states by γ-aminobutyric acid and its analogs in chick cerebral neurons. Pflugers Arch 416, 454-461.
35. Miyazawa A, Fujiyoshi Y & Unwin N (2003). Structure and gating mechanism of the acetylcholine receptor pore. Nature 424, 949-955.
36. Moss SJ & Smart TG (2001). Constructing inhibitory synapses. Nat Rev Neurosci 2, 240-250.
37. A system. Biochem Pharmacol 37, 943-945.
38. A receptor research. Synapse 21, 189-274.
39. A receptors. J Neurosci 22, 8411-8421.
40. A receptor subtypes. Pharmacol Rev 47, 181-234.
41. A receptor subtypes. Curr Top Med Chem 2, 795-816.
42. A receptor channels. EMBO J 11, 2017-2023.
43. A receptor complex in cultured rat neurones. J Physiol 447, 587-625.
44. A receptor a subunit. J Biol Chem 269, 20380-20387.
45. A receptor subtype. J Neuroscience 17, 2728-2737.
46. A receptor main conductance state of mouse spinal cord neurones in culture. J Physiol 423, 193-22O.
47. Wagner DA & Czajkowski C (2001). Structure and dynamics of the GABA binding pocket: a narrowing cleft that constricts during activation. J Neurosci 21, 67-74.
48. Weiss DS, Barnes EM Jr & Hablitz JJ (1988). Whole-cell and single-channel recordings of GABA-gated currents in cultured chick cerebral neurons. J Neurophysiol 59, 495-513.
49. 1, subunit is essential for GABA binding and chloride ion current gating. Neuroreport 10, 2417-2421.
50. A receptors. Eur J Neurosci 9, 2225-2235.