Regulation of GABAA receptor structure and function by chronic drug treatments in vivo and with stably transfected cells

Japanese Journal of Pharmacology

Volumn 70, Issue 1, 1996, Pages 1-15

  Klein, Ronald L ^a   Adron Harris, R ^a  

^a UNIVERSITY OF COLORADO   (United States)

Author keywords

Alcohol; Barbiturate; Benzodiazepine; Chloride channel; Dependence; Receptor expression; Transfection; Aminobutyric acid type A (GABAA) receptor

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID RECEPTOR STIMULATING AGENT; ALCOHOL; BARBITURIC ACID DERIVATIVE; BENZODIAZEPINE DERIVATIVE; CHLORIDE CHANNEL; MESSENGER RNA; RECEPTOR SUBUNIT; ANXIOLYTIC AGENT; CENTRAL NERVOUS SYSTEM AGENTS; HYPNOTIC SEDATIVE AGENT; NEUROTRANSMITTER RECEPTOR;

ALLOSTERISM; ANIMAL CELL; ANIMAL TISSUE; BRAIN SLICE; DRUG BINDING SITE; DRUG DEPENDENCE; DRUG RECEPTOR BINDING; DRUG TOLERANCE; GENETIC TRANSFECTION; NERVE CELL CULTURE; NONHUMAN; PROTEIN QUATERNARY STRUCTURE; PROTEIN STRUCTURE; RECEPTOR DENSITY; RECEPTOR DOWN REGULATION; REVIEW; ADDICTION; ANIMAL; CELL CULTURE; DOWN REGULATION; DRUG EFFECT; HUMAN; METABOLISM; PHYSIOLOGY; TIME;

ANIMALS; ANTI-ANXIETY AGENTS; BENZODIAZEPINES; CELLS, CULTURED; CENTRAL NERVOUS SYSTEM AGENTS; CHLORIDE CHANNELS; DOWN-REGULATION; ETHANOL; GABA AGONISTS; HUMANS; HYPNOTICS AND SEDATIVES; RECEPTORS, GABA-A; RECEPTORS, NEUROTRANSMITTER; SUBSTANCE-RELATED DISORDERS; TIME FACTORS; TRANSFECTION;

EID: 0029662170     PISSN: 00215198     EISSN: None     Source Type: Journal    
DOI: 10.1254/jjp.70.1     Document Type: Article

References (124)

1. Nestler EJ, Hope BT and Widnell KL: Drug addiction: A model for the molecular basis of plasticity. Neuron 11, 995-1006 (1993)
2. A receptor mRNAs in bovine cerebellum: Localization of α2 mRNA in Bergmann glia layer. Neurosci Lett 106, 7-12 (1989)
3. Cherubini E, Gaiarsa JL and Ben-Ari Y: GABA: An excitatory transmitter in early postnatal life. Trends Neurosci 14, 515-519 (1991)
4. Kravitz EA, Kuffler SW and Potter DD: α-Aminobutyric acid and other blocking compounds in Crustacea. Their relative concentrations in separated motor and inhibitory axons. J Neurophysiol 26, 739-751 (1963)
5. A receptor subtypes. Pharmacol Rev 47, 181-234 (1995)
6. A receptor channels. Annu Rev Neurosci 17, 569-602 (1994)
7. A receptor function and gene expression in the central nervous system. Int Rev Neurobiol 38, 1-91 (1995)
8. A receptor structure and function. J Biol Chem 267, 16747-16750 (1992)
9. A receptor shows a ligand-gated receptor super-family. Nature 328, 221-227 (1987)
10. A receptor subunit for benzodiazepine pharmacology. Nature 338, 582-585 (1989)
11. A-benzodiazepine receptors produced in transfected cells. Science 245, 1389-1394 (1989)
12. Pritchett DB and Seeburg PH: γ-Aminobutyric acid type A receptor point mutation increases the affinity of compounds for the benzodiazepine site. Proc Natl Acad Sci USA 88, 1421-1425 (1991)
13. Whiting PJ, McKernan RM and Iversen LL: Another mechanism for creating diversity in γ-aminobutyrate type A receptors: RNA splicing directs expression of two forms of γ2 subunit, one of which contains a protein kinase C phosphorylation site. Proc Natl Acad Sci USA 87, 9966-9970 (1990)
14. A receptor heterogeneity is increased by alternative splicing of a novel γ-subunit gene transcript. J Neurochem 56, 1432-1437 (1991)
15. A receptors. FASEB J 4, 1469-1480 (1990)
16. A receptor determined by electron microscopic image analysis. J Neurochem 62, 815-818 (1994)
17. A receptor subunit mRNAs in the rat brain I. Telencephalon, diencephalon, mesencephalon. J Neurosci 12, 1040-1062 (1992)
18. A receptor but the a I polypeptide is the principal site of the agonists benzodiazepine photoaffinity labelling reaction. J Biol Chem 265, 21160-21165 (1990)
19. A receptor currents by chronic elevation of cAMP-dependent protein kinase is mediated by phosphorylation of the 1 subunit. Mol Pharmacol 44, 1202-1210 (1994)
20. 2+. Neuron 5, 781-788 (1990)
21. A-receptor channels of mouse spinal neurones in culture. J Physiol (Lond) 475, 69-82 (1994)
22. Majewska MD, Harrison ML, Schwartz RD, Barker JL and Paul SM: Steroid hormone metabolites are barbiturate-like modulators of the GABA receptor. Science 232, 1004-1007 (1986)
23. Deitrich RA, Dunwiddie TV, Harris RA and Erwin VG: Mechanism of action of ethanol: initial central nervous system actions. Pharmacol Rev 41, 489-537 (1989)
24. Harris RA and Allan AM: Alcohol intoxication: Ion channels and genetics. FASEB J 3, 1689-1695 (1989)
25. Suzdak DP, Glowa JR, Crawley JN, Schwartz RD, Skolnick P and Paul SM: A selective imidazobenzodiazepine antagonist of ethanol in the rat. Science 234, 1243-1247 (1986)
26. Mehta AK and Ticku MK: Chronic GABA exposure down-regulates GABA-benzodiazepine receptor-ionophore complex in cultured cerebral cortical neurons. Mol Brain Res 16, 29-36 (1992)
27. Aguayo LG, Pancetti FC, Klein RL and Harris RA: Differential effects of GABAergic ligands in mouse and rat hippocampal neurons. Brain Res 647, 97-105 (1994)
28. A receptors: Generalization to other ligand-gated ion channels. J Pharmacol Exp Ther 267, 522-537 (1993)
29. A receptors requires phosphorylation of the alternatively spliced variant of the γ2 subunit. FEBS Lett 313, 113-117 (1992)
30. A receptor subunits expressed in human embryonic kidney cells. J Pharmacol Exp Ther 269, 157-163 (1994)
31. A receptor function and ethanol. FEBS Lett 324, 140-142 (1993)
32. Cash DJ and Subbarao K: Desensitization of gamma-aminobutyric acid receptor from rat brain: two distinguishable receptors on the same membrane. Biochemistry 26, 7556-7562 (1987)
33. A receptor in outside-out patches. Biophys J 66, 1039-1050 (1994)
34. Maloteaux JM, Octave JN, Gossuin A, Laterre C and Trouet A: GABA induces down-regulation of the benzodiazepine-GABA receptor complex in the rat cultured neurons. Eur J Pharmacol 144, 173-183 (1987)
35. A/benzodiazepine receptors in chick cortical neurons. J Neurochem 57, 1307-1312 (1991)
36. Roca DJ, Rozenberg I, Farrant M and Farb DH: Chronic agonist exposure induces down-regulation and allosteric uncoupling of the γ-aminobutyric acid/benzodiazepine receptor complex. Mol Pharmacol 37, 37-43 (1990)
37. A-gated chloride channels. J Pharmacol Exp Ther 246, 558-564 (1988)
38. Hablitz JJ, Tehrani MHJ and Barnes EM Jr: Chronic exposure of developing cortical neurons to GABA down-regulates GABA/benzodiazepine receptors and GABA-gated chloride currents. Brain Res 501, 332-338 (1989)
39. A receptor α subunit messenger RNAs in embryonic chick neurons in culture. J Biol Chem 266, 6011-6014 (1991)
40. A receptor α1-subunit mRNA in primary cultured cerebral cortical neurons. Mol Brain Res 15, 327-331 (1992)
41. A/benzodiazepine receptor polypeptides from the surface of chick cortical neurons. J Biol Chem 269, 1548-1553 (1994)
42. A receptor α2 and α3 subunit mRNAs as well as polypeptide expression in primary cultured cerebral cortical neurons. Mol Brain Res 24, 159-165 (1994)
43. A /benzodiazepine receptors on clatharin-coated vesicles from rat brain. J Neurochem 60, 1755-1761 (1993)
44. Gallager DW, Lakoski JM, Gonsalves SF and Rauch SL: Chronic benzodiazepine treatment decreases postsynaptic GABA sensitivity. Nature 308, 74-77 (1984)
45. A receptor regulation in culture: Altered allosteric interactions following prolonged exposure to benzodiazepines, barbiturates, and methylxanthines. Mol Pharmacol 37, 710-719 (1990b)
46. Hu XJ and Ticku MJ: Chronic benzodiazepine agonist treatment produces functional uncoupling of the γ-aminobutyric acid-benzodiazepine receptor ionophore complex in cortical neurons. Mol Pharmacol 45, 618-625 (1994)
47. Rosenberg HC and Chiu TH: Tolerance during chronic benzodiazepine treatment associated with decreased receptor binding. Eur J Pharmacol 70, 453 (1981)
48. Marley RJ and Gallager DW: Chronic diazepam treatment produces regionally-specific changes in GABA-stimulated chloride flux. Eur J Pharmacol 159, 217-223 (1989)
49. A receptor function in cultured cortical neurons. Mol Pharmacol 36, 796-802 (1989)
50. A subunit mRMA in rat brain. J Mol Neurosci 2, 101-107 (1990)
51. A receptor subunit mRNA concentrations following chronic lorazepam administration. Br J Pharmacol 103, 1285-1287 (1991)
52. Zhao TJ, Chiu TH and Rosenberg HC: Reduced expression of γ-aminobutyric acid type A/benzodiazepine receptor γ 2 and α5 subunit mRNAs in brain regions of flurazepam-treated rats. Mol Pharmacol 45, 657-663 (1994)
53. A receptor α subunits after flurazepam treatment. Eur J Pharmacol 226, 335-341 (1992)
54. A receptor subunit mRNA levels are differentially influenced by chronic FG 7142 and diazepam exposure. Eur J Pharmacol (Mol Pharmacol) 226, 21-28 (1992)
55. A receptors in mouse cortical homogenates are phoshorylated by endogenous protein kinase A. Mol Brain Res 24, 55-64 (1994)
56. A receptors by tolerance to and dependence upon pentobarbital. Eur J Pharmacol 236, 23-30 (1993)
57. A receptor γ-2-subunit messenger RNA by tolerance to and withdrawal from pentobarbital-an in situ hybridization study. Life Sci 53, 321-326 (1993)
58. Allan AM, Zhang X and Baier LD: Barbiturate tolerance: Effects on GABA-operated chloride channel function. Brain Res 588, 255-260 (1992)
59. A receptor α1- and β3-subunit mRNAs. J Neurochem 63, 301-309 (1994)
60. Gee KW, Bolger MB, Brinton RE, Coirini H and McEwen BS: Steroid modulationof of the chloride ionophore in rat brain: Structure-activity requirements, regional dependence and mechanism of action. J Pharmacol Exp Ther 246, 803-812 (1988)
61. A receptor function. Mol Pharmacol 46, 977-985 (1994)
62. A receptor regulation: Chronic treatment with pregnanolone uncouples allosteric interactions between steroid and benzodiazepine recognition sites. Mol Pharmacol 44, 191-197 (1993)
63. Yu R and Ticku MK: Chronic neurosteroid treatment produces functional uncoupling of the GABA-benzodiazepine receptor complex in mammalian cortical neurons. Soc Neurosci Abs 20, 505 (1994)
64. Buck KJ and Harris RA: Neuroadaptive responses to chronic ethanol. Alcohol Clin Exp Res 15, 460-470 (1991)
65. Mhatre M and Ticku MK: Chronic ethanol treatment selectively increases the binding of inverse agonists for benzodiazepine binding sites in cultured spinal cord neurons. J Pharmacol Exp Ther 251, 164-168 (1989)
66. A receptor gene expression. Mol Pharmacol 42, 415-422 (1992)
67. DeVries DJ, Johnston GAR, Ward LC, Wilce PA and Shanley BC: Effects of chronic ethanol inhalation on the enhancement of benzodiazepine binding to mouse brain membranes by GABA. Neurochem Int 10, 231-235 (1987)
68. 3H]flunitrazepam binding in rat cortex and hippocampus. J Neurochem 58, 1916-1922 (1992)
69. Rastogi SK, Thyagarajan R, Clothier J and Ticku MK: Effect of chronic treatment with ethanol on benzodiazepine and picrotoxin sites on the GABA receptor complex in regions of the brain of the rat. Neuropharmacology 25, 1179-1184 (1986)
70. A receptor-operated chloride channels. II. Chronic effects of ethanol. J Pharmacol Exp Ther 253, 713-719 (1990)
71. A receptor α subunit mRNAs in rat cerebral cortex. Mol Pharmacol 39, 157-163 (1991)
72. Mhatre MC and Ticku MK: Chronic ethanol treatment upregulates the GABA receptor β subunit expression. Mol Brain Res 23, 246-252 (1994)
73. A receptor α1-subunit mRNA in mouse brain following continuous ethanol inhalation. Eur J Pharmacol 247, 127-130 (1993)
74. A receptor α subunits reveal that chronic alcohol treatment down-regulates α-subunit expression in rat brain regions. J Neurochem 61, 1620-1625 (1993)
75. - uptake in cerebral cortical synaptoneurosomes. J Pharmacol Exp Ther 246, 158-164 (1988)
76. A receptor function: Molecular and physiological determinants. In GABAergic Synaptic Transmission, Edited by Biggio G, Concas A and Costa E, pp 269-279, Raven Press, New York (1992)
77. Allan AM and Harris RA: Acute and chronic ethanol treatments alter GABA-receptor operated chloride channels. Pharmacol Biochem Behav 27, 665-670 (1987)
78. Yu SS, Lefkowitz RJ and Hausdorff WP: β-Adrenergic sequestration. J Biol Chem 268, 337-341 (1993)
79. 2-adrenergic receptor are involved in distinct pathways of receptor desensitization. J Biol Chem 264, 12657-12665 (1989)
80. 2-adrenergic receptors. J Biol Chem 268, 3201-3208 (1993)
81. 2-adrenergic receptor sequestration. J Biol Chem 269, 2790-2795 (1994)
82. 2-adrenergic receptor in agonist-induced down-regulation of the receptor. Proc Natl Acad Sci USA 87, 5089-5093 (1990)
83. 2A-adrenergic receptor confer short term agonist-promoted desensitization. J Biol Chem 267, 4740-4746 (1992)
84. 3-adrenergic receptor. J Pharmacol Exp Ther 271, 1253-1258 (1994)
85. Filtz TM, Artymyshyn RP, Guan W and Molinoff PB: Paradoxical regulation of dopamine receptors in transfected 293 cells. Mol Pharmacol 44, 371-379 (1993)
86. 2L dopamine receptor isoforms are differentially regulated in Chinese hamster ovary cells. Mol Pharmacol 45, 878-889 (1994)
87. 2L dopamine receptors by agonists and antagonists in transfected HEK-293 cells. J Pharmacol Exp Ther 271, 1574-1582 (1994)
88. 2A receptors in heterologous expression systems. J Neurochem 63, 1255-1260 (1994)
89. 2 receptors in transfected fibroblast B82 cells. Eur J Pharmacol (Mol Pharmacol) 268, 381-391 (1994)
90. Yang J, Logsdon CD, Johansen TE and Williams JA: Human m3 muscarinic acetylcholine receptor carboxyl-terminal threonine residues are required for agonist-induced receptor down-regulation. Mol Pharmacol 44, 1158-1154 (1993)
91. Law PT, McGinn TM, Wick MJ, Erikson LJ, Evans C and Loh HH: Analysis of delta-opioid receptor activities stably expressed in CHO cell lines: function of receptor density? J Pharmacol Exp Ther 271, 1686-1694 (1994)
92. Peng X, Gerzanich V, Amand R, Whiting PJ and Lindstrom J: Nicotine-induced increase in neuronal nicotinic receptors results from a decrease in the rate of receptor turnover. Mol Pharmacol 46, 523-530 (1994)
93. Hadingham KL, Harkness PC, McKernan RM, Quirk K, Le Bourdelles B, Horne AL, Kemp JA, Barnard EA, Ragan CI and Whiting PJ: Stable expression of mammalian type A γ-aminobutyric acid receptors in mouse cells: Demonstration of functional assembly of benzodiazepine-responsive sites. Proc Natl Acad Sci USA 89, 6378-6382 (1992)
94. A receptors by GABAergic drugs. J Pharmacol Exp Ther 274, 1484-1492 (1995)
95. A receptors expressed in stably transfected cells. J Neurochem 63, 2349-2352 (1994)
96. A receptor function and binding in stably transfected cells: chronic ethanol treatment. Alcohol Clin Exp Res 19, 1338-1344 (1995)
97. A receptor-activated current and benzodiazepine modulation. Mol Neuropharmacol 1, 59-64 (1991)
98. Mishina M, Takai T, Imoto K, Noda M, Takahashi T, Numa S, Methfessel C and Sakmann B: Distinction between fetal and adult forms of muscle acetylcholine receptor. Nature 321, 406-411 (1986)
99. A receptor subtypes expressed in cerebellar granule cells: a developmental study. J Neurochem 62, 2037-2044 (1994)
100. A-benzodiazepine receptor ionophore complex in primary cultures of cortical neurons. Dev Brain Res 80, 137-140 (1994)
101. A receptor. Proc Natl Acad Sci USA 87, 1315-1318 (1990).
102. A receptor by cAMP-dependent protein kinase and protein kinase C. Neurochem Res 18, 95-100 (1993)
103. Moss SJ, Doherty CA and Huganir RL: Identification of the cAMP-dependent protein kinase and protein kinase C phosphorylation sites within the major intracellular domains of the β1, γ2S, and γ2L subunits of the γ-aminobutyric acid type A receptor. J Biol Chem 267, 14470-14476 (1992)
104. - uptake by brain microsacs. J Neurochem 57, 722-725 (1991)
105. A receptors by cAMP-dependent protein phosphorylation. Science 257, 661-665 (1992)
106. A-channels. FEBS Lett 291, 150-152 (1991)
107. A receptor. J Neurochem 60, 1972-1975 (1993)
108. Kellenberger S, Malherbe P and Sigel E: Function of the α1β2γ2S γ-aminobutyric acid type A receptor is modulated by protein kinase C via multiple phosphorylation sites. J Biol Chem 267, 25660-25663 (1992)
109. A receptor function by protein kinase C phosphorylation. Neuron 12, 1081-1095 (1994)
110. A receptor single-channel currents expressed in L929 cells. Soc Neurosci Abs 20, 503 (1994)
111. McDonald BJ and Moss SJ: Differential phosphorylation of intracellular domains of γ-aminobutyric type A receptor subunits by calcium/calmodulin type 2-dependent protein kinase and cGMP-dependent protein kinase. J Biol Chem 269, 18111-18117 (1994)
112. AR) function. The Pharmacologist 35, 171 (1993)
113. A receptor currents in L929 cells. Soc Neurosci Abs 20, 503 (1994)
114. A receptors. Mol Brain Res 31, 165-172 (1995)
115. A-mediated synaptic currents in hippocampal CA1 neurons. Brain Res 665, 307-310 (1994)
116. A-mediated synaptic current by ethanol in hippocampal CA1 neurons: Possible role of protein kinase C. J Pharmacol Exp Ther 268, 1388-1395 (1994)
117. A receptor subunit mRNAs in chick cortical neurons. Mol Brain Res 26, 9-17 (1994)
118. A receptors in the chick embryo. Mol Brain Res 26, 18-25 (1994)
119. --induced depolarization and NMDA exposure. J Neurochem 64, 558-565 (1995)
120. Jalilian Tehrani MH and Barnes EM Jr: Chronic administration of lorazepam to mice promotes transfer of GABA/benzodiazepine receptors to clatharin-coated vesicles. Soc Neurosci Abs 20, 496 (1994)
121. Haigh JRM and Feely M: Tolerance to the anticonvulsant effect of benzodiazepines. Trends Pharmacol Sci 9, 361-366 (1988)
122. Lister RG and Nutt DJ: Mice and rats are sensitized to the proconvulsant action of a benzodiazepine-receptor inverse agonist (FG 7142) following a single dose of lorazepam. Brain Res 379, 364-366 (1986)
123. Crabbe JC, Merrill C and Belknap JK: Acute dependence on depressant drugs is determined by common genes in mice. J Pharmacol Exp Ther 257, 663-667 (1991)
124. Crawford TO, Mitchell WG and Snodgrass SR: Lorazepam in childhood status epilepticus and serial seizures: Effectiveness and tachyphylaxis. Neurology 37, 190-195 (1987)