Gating allosterism at a single class of etomidate sites on α 1β2γ2L GABAA receptors accounts for both direct activation and acronist modulation

Journal of Biological Chemistry

Volumn 279, Issue 20, 2004, Pages 20982-20992

  Rüsch, Dirk ^a,c   Zhong, Huijun ^a   Forman, Stuart A ^a,b  

^a MASSACHUSETTS GENERAL HOSPITAL   (United States)

^b HARVARD MEDICAL SCHOOL   (United States)

^c UNIVERSITY HOSPITAL SCHLESWIG HOLSTEIN   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

CHEMICAL ACTIVATION; CHEMICAL BONDS; ELECTROPHYSIOLOGY; MUTAGENESIS; STEREOCHEMISTRY;

CONSTITUTIVE GATING ACTIVITY; STEREOSELECTIVITY;

BIOCHEMISTRY;

4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID A RECEPTOR BLOCKING AGENT; 4 AMINOBUTYRIC ACID A RECEPTOR STIMULATING AGENT; ETOMIDATE; RECEPTOR SUBTYPE;

ALLOSTERISM; ARTICLE; BINDING SITE; CHANNEL GATING; DRUG MECHANISM; ELECTROPHYSIOLOGY; HUMAN; HUMAN CELL; MODEL; POINT MUTATION; PREDICTION; PRIORITY JOURNAL; QUANTITATIVE ANALYSIS; RECEPTOR BINDING; RECEPTOR UPREGULATION; STEREOCHEMISTRY;

ALLOSTERIC SITE; ANIMALS; CELL LINE; DNA, COMPLEMENTARY; ETOMIDATE; FEMALE; GABA AGONISTS; GAMMA-AMINOBUTYRIC ACID; HUMANS; KINETICS; MEMBRANE POTENTIALS; OOCYTES; RECEPTORS, GABA-A; TRANSFECTION; XENOPUS LAEVIS;

EID: 2442687767     PISSN: 00219258     EISSN: None     Source Type: Journal    
DOI: 10.1074/jbc.M400472200     Document Type: Article

References (69)

1. Whiting, P. J., McKernan, R. M., and Wafford, K. A. (1995) Int. Rev. Neurobiol. 38, 95-138
2. McKernan, R. M., and Whiting, P. J. (1996) Trends Neurosci. 19, 139-143
3. Turner, D. W., Ransom, R. W., Yang, J., and Olsen, R. W. (1989) J. Pharmacol. Exp. Ther. 248, 960-966
4. Twyman, R. E., and Macdonald, R. L. (1992) J. Physiol. (Lond.) 456, 215-245
5. Lambert, J. J., Belelli, D., Hill-Venning, C., Callachan, H., and Peters, J. A. (1996) Cell. Mol. Neurobiol. 16, 155-174
6. MacDonald, R. L., Rogers, C. J., and Twyman, R. E. (1989) J. Physiol. (Lond.) 417, 483-500
7. Bai, D., Pennefather, P. S., MacDonald, J. F., and Orser, B. A. (1999) J. Neurosci. 19, 10635-10646
8. Krasowski, M. D., Jenkins, A., Flood, P., Kung, A. Y., Hopfinger, A. J., and Harrison, N. L. (2001) J. Pharmacol. Exp. Ther. 297, 338-351
9. Uchida, L, Kamatchi, G., Burt, D., and Yang, J. (1995) Neurosci. Lett. 185, 203-206
10. Belelli, D., Lambert, J. J., Peters, J. A., Wafford, K., and Whiting, P. J. (1997) Proc. Natl. Acad. Sci. U. S. A. 94, 11031-11036
11. Mihic, S. J., Whiting, P. J., and Harris, R. A. (1994) Eur. J. Pharmacol. 268, 209-214
12. Mihic, S. J., Ye, Q., Wick, M. J., Koltchine, V. V., Krasowski, M. D., Finn, S. E., Mascia, M. P., Valenzuela, C. F., Hanson, K. K., Greenblatt, E. P., Harris, R. A., and Harrison, N. L. (1997) Nature 389, 385-389
13. Jones, M. V., Brooks, P. A., and Harrison, N. L. (1992) J. Physiol. (Lond.) 449, 279-293
14. Banks, M. I., and Pearce, R. A. (1999) Anesthesiology 90, 120-134
15. Carlson, B. X., Hales, T. G., and Olsen, R. W. (1997) in Anesthesia: Biologic Foundations (Yaksh, T. L., Lynch, C., III, Zapol, W. M., Maze, M., Biebuyck, J. F., and Saidman, L. J., eds) pp. 259-275, Lippincott-Raven, Philadelphia
16. Colquhoun, D. (1998) Br. J. Pharmacol. 125, 924-947
17. O'Shea, S. M., Wong, L. C., and Harrison, N. L. (2000) Brain Res. 852, 344-348
18. Hall, A. C., Lieb, W. R., and Franks, N. P. (1994) Br. J. Pharmacol. 112, 906-910
19. Husain, S. S., Ziebell, M. R., Ruesch, D., Hong, F., Arevalo, E., Kosterlitz, J. A., Olsen, R. W., Forman, S. A., Cohen, J. B., and Miller, K. W. (2003) J. Med. Chem. 46, 1257-1265
20. Tomlin, S. L., Jenkins, A., Lieb, W. R., and Franks, N. P. (1998) Anesthesiology 88, 708-717
21. Kurata, Y., Marszalec, W., Yeh, J. Z., and Narahashi, T. (1999) Mol. Pharmacol. 55, 1011-1019
22. Cash, D. J., and Subbarao, K. (1988) Biochemistry 27, 4580-4590
23. Arden, J. R., Holley, F. O., and Stanski, D. R. (1986) Anesthesiology 65, 19-27
24. Yang, J., and Uchida, I. (1996) Neuroscience 73, 69-78
25. Hill-Venning, C., Belelli, D., Peters, J. A., and Lambert, J. J. (1997) Br. J. Pharmacol. 120, 749-756
26. Belelli, D., Muntoni, A. L., Merrywest, S. D., Gentet, L. J., Casula, A., Callachan, H., Madau, P., Gemmell, D. K., Hamilton, N. M., Lambert, J. J., Sillar, K. T., and Peters, J. A. (2003) Neuropharmacology 45, 57-71
27. Jurd, R., Arras, M., Lambert, S., Drexler, B., Siegwart, R., Crestani, F., Zaugg, M., Vogt, K. E., Ledermann, B., Antkowiak, B., and Rudolph, U. (2003) FASEB J. 17, 250-252
28. Reynolds, D. S., O'Meara, G. F., Newman, R. J., Bromidge, F. A., Atack, J. R., Whiting, P. J., Rosahl, T. W., and Dawson, G. R. (2003) Neuropharmacology 44, 190-198
29. Scheller, M., and Forman, S. A. (2002) J. Neurosci. 22, 8411-8421
30. Forman, S. A. (1999) Biochemistry 38, 14559-14564
31. Weiss, D. S., and Magleby, K. L. (1989) J. Neurosci. 9, 1314-1324
32. Jones, M. V., and Westbrook, G. L. (1995) Neuron 15, 181-191
33. Steinbach, J. H., and Akk, G. (2001) J. Physiol. (Lond.) 537, 715-733
34. Edelstein, S. J., and Changeux, J. P. (1996) Experientia (Basel) 52, 1083-1090
35. Chang, Y., and Weiss, D. S. (1999) Biophys. J. 77, 2542-2551
36. Boileau, A. J., Li, T., Benkwitz, C., Czajkowski, C., and Pearce, R. A. (2003) Neuropharmacology 44, 1003-1012
37. Scheller, M., and Forman, S. A. (2001) Anesthesiology 95, 123-131
38. Topf, N., Jenkins, A., Baron, N., and Harrison, N. L. (2003) Anesthesiology 98, 306-311
39. McGurk, K. A., Pistis, M., Belelli, D., Hope, A. G., and Lambert, J. J. (1998) Br. J. Pharmacol. 124, 13-20
40. Cestari, I. N., Min, K. T., Kulli, J. C., and Yang, J. (2000) J. Neurochem. 74, 827-838
41. Serafini, R., Bracamontes, J., and Steinbach, J. H. (2000) J. Physiol. (Lond.) 524, 649-676
42. Krasowski, M. D., Nishikawa, K., Nikolaeva, N., Lin, A., and Harrison, N. L. (2001) Neuropharmacology 41, 952-964
43. Amin, J., and Weiss, D. S. (1993) Nature 366, 565-569
44. Monod, J., Wyman, J., and Changeux, J. (1965) J. Mol. Biol. 12, 88-118
45. Chang, Y., Wang, R., Barot, S., and Weiss, D. S. (1996) J. Neurosci. 16, 5415-5424
46. Farrar, S. J., Whiting, P. J., Bonnert, T. P., and McKernan, R. M. (1999) J. Biol. Chem. 274, 10100-10104
47. Petrini, E. M., Zacchi, P., Barberis, A., Mozrzymas, J. W., and Cherubini, E. (2003) J. Biol. Chem. 278, 16271-16279
48. Baumann, A., Baur, R., and Sigel, E. (200) J. Neurosci. 23, 11158-11166
49. Hall, D. (2000) Mol. Pharmacol. 58, 1412-1423
50. Li, X., and Pearce, R. A. (2000) J. Neurosci. 20, 899-907
51. Krasowski, M. D., Koltchine, V. V., Rick, C. E., Ye, Q., Finn, S. E., and Harrison, N. L. (1998) Mol. Pharmacol. 53, 530-538
52. Thompson, S. A., Smith, M. Z., Wingrove, P. B., Whiting, P. J., and Wafford, K. A. (1999) Br. J. Pharmacol. 127, 1349-1358
53. Moody, E. J., Knauer, C., Granja, R., Strakhova, M., and Skolnick, P. (1997) J. Neurochem. 69, 1310-1313
54. Chang, C. S., Olcese, R., and Olsen, R. W. (2003) J. Biol. Chem. 278, 42821-42828
55. Carlson, B. X., Engblom, A. C., Kristiansen, U., Schousboe, A., and Olsen, R. W. (2000) Mol. Pharmacol. 57, 474-484
56. Bianchi, M. T., and Macdonald, R. L. (2003) J. Neurosci. 23, 10934-10943
57. Akk, G., and Steinbach, J. H. (2003) J. Physiol. (Lond.) 546, 641-646
58. Jenkins, A., Greenblatt, E. P., Faulkner, H. J., Bertaccini, E., Light, A., Lin, A., Andreasen, A., Viner, A., Trudell, J. R., and Harrison, N. L. (2001) J. Neurosci. 21, RC136
59. Dalziel, J. E., Cox, G. B., Gage, P. W., and Birnir, B. (1999) Eur. J. Pharmacol. 385, 283-286
60. Ueno, S., Lin, A., Nikolaeva, N., Trudell, J. R., Mihic, S. J., Harris, R. A., and Harrison, N. L. (2000) Br. J. Pharmacol. 131, 296-302
61. Findlay, G. S., Ueno, S., Harrison, N. L., and Harris, R. A. (2001) Neurosci. Lett. 305, 77-80
62. Greenfield, L. J., Jr., Zaman, S. H., Sutherland, M. L., Lummis, S. C., Niemeyer, M. I., Barnard, E. A., and Macdonald, R. L. (2002) Neuropharmacology 42, 502-521
63. Williams, D. B., and Akabas, M. H. (2002) J. Neurosci. 22, 7417-7424
64. Wick, M. J., Mihic, S. J., Ueno, S., Mascia, M. P., Trudell, J. R., Brozowski, S. J., Ye, Q., Harrison, N. L., and Harris, R. A. (1998) Proc. Natl. Acad. Sci. U. S. A. 95, 6504-6509
65. Pistis, M., Belelli, D., Peters, J. A., and Lambert, J. J. (1997) Br. J. Pharmacol. 122, 1707-1719
66. Mascia, M. P., Machu, T. K., and Harris, R. A. (1996) Br. J. Pharmacol. 119, 1331-1336
67. Aistrup, G. L., Marszalec, W., and Narahashi, T. (1999) Mol. Pharmacol. 55, 39-49
68. Forman, S. A., and Zhou, Q. (1999) Mol. Pharmacol. 55, 102-108
69. Zhou, Q., Verdoorn, T. A., and Lovinger, D. M. (1998) J. Physiol. (Lond.) 507, 335-352