Allosteric uncoupling and up-regulation of benzodiazepine and GABA recognition sites following chronic diazepam treatment of HEK 293 cells stably transfected with α1β2γ2S subunits of GABAA receptors

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 375, Issue 3, 2007, Pages 177-187

  Peričić, Danka ^a   Štrac, Dubravka Švob ^a   Jembrek, Maja Jazvinšćak ^a   Vlainić, Josipa ^a  

^a RUDER BO KOVI INSTITUTE   (Croatia)

Author keywords

3H flunitrazepam; 3H muscimol binding; Chronic diazepam; GABAA receptor, recombinant; Gabazine; HEK 293 cells; Inhibitors of RNA and protein synthesis; Picrotoxin

Indexed keywords

3 AMINO 2 (3 CARBOXYPROPYL) 6 (4 METHOXYPHENYL)PYRIDAZINIUM BROMIDE; 4 AMINOBUTYRIC ACID RECEPTOR; BENZODIAZEPINE; CYCLOHEXIMIDE; DACTINOMYCIN; DIAZEPAM; FLUMAZENIL; FLUNITRAZEPAM; MUSCIMOL; PICROTOXIN; RECEPTOR SUBUNIT;

ARTICLE; CONTROLLED STUDY; DRUG BINDING SITE; DRUG RECEPTOR BINDING; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; LONG TERM EXPOSURE; PROTEIN SYNTHESIS; RECEPTOR AFFINITY; UPREGULATION;

ALLOSTERIC REGULATION; ANIMALS; BENZODIAZEPINES; BINDING SITES; BINDING, COMPETITIVE; CELL LINE; DIAZEPAM; FLUMAZENIL; FLUNITRAZEPAM; GABA ANTAGONISTS; GAMMA-AMINOBUTYRIC ACID; HUMANS; MUSCIMOL; PICROTOXIN; PROTEIN SUBUNITS; PYRIDAZINES; RADIOLIGAND ASSAY; RATS; RECEPTORS, GABA-A; RECEPTORS, GABA-B; TRANSFECTION; UP-REGULATION;

EID: 34047132216     PISSN: 00281298     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00210-007-0152-z     Document Type: Article

References (52)

1. A receptors uncouples allosteric binding: studies on possible mechanisms. J Neurochem 79:1100-1108
2. A receptors: classification on the basis of subunit structure and receptor function. Pharmacol Rev 50:291-313
3. Bateson AN (2002) Basic pharmacologic mechanisms involved in benzodiazepine tolerance and withdrawal. Curr Pharmaceut Des 8:5-21
4. A receptors. J Recept Signal Transduct Res 17:99-113
5. A receptor modulators. Eur Neuropsychopharmacol 13:411-423
6. Boileau AJ, Kucken AM, Evers AR, Czajkowski C (1998) Molecular dissection of benzodiazepine binding and allosteric coupling using chimeric gamma-aminobutyric acid A receptor subunits. Mol Pharmacol 53:295-303
7. A receptor function is desensitised in rat cultured cerebellar granule cells following chronic flunitrazepam treatment. J Neurochem 71:1232-1240
8. Costa E, Guidotti A (1996) Benzodiazepines on trial: a research strategy for their rehabilitation. Trends Pharmacol Sci 17:192-200
9. A receptors and benzodiazepines: a role for dendritic resident subunit mRNAs. Neuropharmacology 43:925-937
10. A receptors supports an allosteric model of modulation. Brit J Pharmacol 145:894-906
11. Farrar SJ, Whiting PJ, Bonnert TP, McKernan RM (1999) Stoichiometry of a ligand-gated ion channel determined by fluorescence energy transfer. J Biol Chem 274:10100-10104
12. Filtz TM, Guan W, Artymyshyn RP, Facheco M, Ford C, Molinoff PB (1994) Mechanisms of up-regulation of D2L dopamine receptors by agonists and antagonists in transfected HEK-293 cells. J Pharmacol Exp Ther 271:1574-1582
13. Friedman LK, Gibbs TT, Farb DH (1996) γ-Aminobutyric acid A receptor regulation: heterologous uncoupling of modulatory site interactions induced by chronic steroid, barbiturate, benzodiazepine, or GABA treatment in culture. Brain Res 707:100-109
14. 3H] flunitrazepam binding in human embryonic kidney cell. Eur J Pharmacol Mol Pharmacol Section 289:87-95
15. Gallager DW, Lakoski JM, Gonsalves SF, Rauch SL (1984) Chronic benzodiazepine treatment decreases postsynaptic GABA sensitivity. Nature 308:74-77
16. Garattini S, Mussini E, Marcucci F, Guaitani A (1973) Metabolic studies on benzodiazepines in various animal species. In: Garattini S, Mussini E, Randall LO (eds) Benzodiazepines. Raven Press, New York, pp 75-98
17. Haefely W (1986) Biological basis of drug-induced tolerance, rebound, and dependence. Contribution of recent research on benzodiazepines. Pharmacopsychiatry 19:353-361
18. Hollister LE, Conley FK, Britt RH, Shuer L (1981) Long-term use of diazepam. J Am Med Assoc 246:1568-1570
19. Holmgren P, Jones AW (2003) Coexistence and concentrations of ethanol and diazepam in post-mortem blood specimens: risk for enhanced toxicity? J Forensic Sci 48:1416-1421
20. Hu XJ, Ticku MK (1994) Chronic benzodiazepine agonist treatment reduces functional uncoupling of the γ-aminobutyric acid-benzodiazepine receptor ionophore complex in cortical neurons. Mol Pharmacol 45:618-625
21. Jatlow P, Dobular K, Bailey D (1979) Serum diazepam concentrations in overdose. Am J Clin Pathol 72:571-577
22. A receptors expressed in stably transfected cells. J Neurochem 63:2349-2352
23. A and benzodiazepine agonists. J Pharmacol Exp Ther 274:1484-1492
24. Korpi ER, Grunder G, Lüddens H (2002) Drug interactions at GABA (A) receptors. Prog Neurobiol 67:113-159
25. Kulkarni SK, Ticku MK (1990) Chronic benzodiazepine antagonist treatment and its withdrawal upregulates components of GABA-benzodiazepine receptor ionophore complex in cerebral cortex of rat. Brain Res 519:6-11
26. Lowry OH, Rosebrough NJ, Farr AL, Randall RJ (1951) Protein measurement with the Folin phenol reagent. J Biol Chem 193:265-275
27. Maksay G, Ticku MK (1984) Pretreatment with GABA and modulatory ligands enhances GABA receptor binding. Eur J Pharmacol 104:185-188
28. McKernan RM, Whiting PJ (1996) Which GABA (A)-receptor subtypes really occur in the brain. Trends Neurosci 19:139-143
29. Medina JH, Novas ML, De Robertis E (1983) Chronic Ro 15-1788 treatment increases the number of benzodiazepine receptors in rat cerebral cortex and hippocampus. Eur J Pharmacol 90:125-128
30. A receptors. Brain Res Brain Res Rev 29:196-217
31. A receptor function by chronic exposure to GABA-neutral and GABA-negative benzodiazepine ligands in cultured cortical neurons. Biochem Pharmacol 40:1337-1344
32. O'Brien CP (2005) Benzodiazepine use, abuse, and dependence. J Clin Psychiat 66(Suppl 2):28-33
33. 3H]muscimol binding in the human brain post mortem. Eur J Pharmacol 235:267-274
34. A receptors. Eur J Pharmacol 482:117-125
35. A receptors to benzodiazepine antagonist flumazenil enhances the maximum number of benzodiazepine binding sites. Life Sci 76:303-317
36. Peričić D, Jazvinšćak Jembrek M, Švob Štrac D, Lazić J, Rajčan Špoljarić I (2005a) Enhancement of benzodiazepine binding sites following chronic treatment with flumazenil. Eur J Pharmacol 507:7-13
37. A receptors. Biomed Pharmacother 59:408-414
38. A receptor subunit expression in rat neocortical areas. Neuroscience 79:477-487
39. A receptors expressed in Sf9 cells: ligand efficacy and subtype selectivity. J Pharmacol Exp Ther 276:882-890
40. Robertson JR, Treasure W (1996) Benzodiazepine abuse-Nature and extent of the problem. CNS Drugs 5:137-146
41. A receptor regulation in culture: altered allosteric interactions following prolonged exposure to benzodiazepines, barbiturates, and methylxanthines. Mol Pharmacol 37:710-719
42. 7(a) receptors in HEK-293F cells demonstrates lack of silent properties for reported neutral antagonists. Naunyn Schmiedebergs Arch Pharmacol 374:31-39
43. A receptor subtypes mediate the anxiolytic, abuse-related, and motor effects of benzodiazepine-like drugs in primates. Proc Natl Acad Sci USA 102:915-920
44. Rudolph U, Crestani F, Möhler H (2001) GABA (A) receptor subtypes: dissecting their pharmacological functions. Trends Pharmacol Sci 22:402-403
45. A receptors. Neurochem Int 34:379-385
46. Strang J, Griffiths P, Abbey J, Gossop M (1994) Survey of use of injected benzodiazepines among drug users in Britain. Brit Med J 308:1082
47. Urbancic M, Marczynski TJ (1989) Chronic exposure to Ro 15-1788: differential effect on flunitrazepam binding to cortex and hippocampus. Eur J Pharmacol 171:1-7
48. A receptor subtypes: any clues to the mechanism of benzodiazepine dependence? Curr Opinion Pharmacol 5:47-52
49. A receptors via two distinct and separable mechanisms. Nature Neuroscience 3:1274-1281
50. Whiting PJ (1999) The GABA-A receptor gene family: new targets for therapeutic intervention. Neurochem Int 34:387-390
51. A/Benzodiazepine receptors in a transfected cell line. Mol Pharmacol 42:996-1003
52. Wong G, Lyon T, Skolnick P (1994) Chronic exposure to benzodiazepine receptor ligands uncouples the γ-aminobutyric acid type A receptor in WSS-1 cells. Mol Pharmacol 46:1056-1062