α4-Containing GABAA receptors are required for antagonism of ethanol-induced motor incoordination and hypnosis by the imidazobenzodiazepine Ro15-4513

Frontiers in Pharmacology

Volumn APR, Issue , 2011, Pages

  Iyer, Sangeetha V ^a,d   Benavides, Rodrigo A ^a,e   Chandra, Dev ^a,f   Cook, James M ^b   Rallapalli, Sundari ^b   June, Harry L ^c   Homanics, Gregg E ^a  

^a UNIVERSITY OF PITTSBURGH SCHOOL OF MEDICINE   (United States)

^b UNIVERSITY OF WISCONSIN MILWAUKEE   (United States)

^c UNIVERSITY OF MARYLAND SCHOOL OF MEDICINE   (United States)

^d UNIVERSITY OF TEXAS AT AUSTIN   (United States)

^e BRIGHAM AND WOMEN S HOSPITAL   (United States)

^f UNIVERSITY OF CALIFORNIA   (United States)

Author keywords

Alcohol; Alcohol antagonist; Alcohol receptor; Benzodiazepine; Extrasynaptic GABAA receptor; Ro15 4513

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR ALPHA4; 8 AZIDO 5,6 DIHYDRO 5 METHYL 6 OXO 4H IMIDAZO[1,5 A][1,4]BENZODIAZEPINE 3 CARBOXYLIC ACID ETHYL ESTER; ALCOHOL;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; ATAXIA; CONTROLLED STUDY; COORDINATION DISORDER; DRUG MECHANISM; DRUG RESISTANCE; DRUG SENSITIVITY; FEMALE; HYPNOSIS; MALE; MOUSE; NONHUMAN; RIGHTING REFLEX; SEX DIFFERENCE; WILD TYPE;

EID: 84865843661     PISSN: None     EISSN: 16639812     Source Type: Journal    
DOI: 10.3389/fphar.2011.00018     Document Type: Article

References (43)

1. Becker, H. C., and Hale, R. L. (1991). RO15-4513 antagonizes the anxiolytic effects of ethanol in a nonshock conflict task at doses devoid of anxiogenic activity. Pharmacol. Biochem. Behav. 39, 803-807.
2. Bonetti, E. P., Burkard, W. P., Gabl, M., Hunkeler, W., Lorez, H. P., Martin, J. R., Moehler, H., Osterrieder, W., Pieri, L., Polc, P., Richards, J. G., Schaffner, R., Scherschlicht, R., Schoch, P., and Haefely, W. E. (1988). Ro 15-4513: partial inverse agonism at the BZR and interaction with ethanol. Pharmacol. Biochem. Behav. 31, 733-749.
3. Borghese, C. M., Storustovu, S., Ebert, B., Herd, M. B., Belelli, D., Lambert, J. J., Marshall, G., Wafford, K. A., and Harris, R. A. (2006). The δ subunit of γ-aminobutyric acid type A receptors does not confer sensitivity to low concentrations of ethanol. J. Pharmacol. Exp. Ther. 316, 1360-1368.
4. Casagrande, S., Cupello, A., Pellistri, F., and Robello, M. (2007). Only high concentrations of ethanol affect GABAA receptors of rat cerebellum granule cells in culture. Neurosci. Lett. 414, 273-276.
5. Chandra, D., Halonen, L. M., Linden, A. M., Procaccini, C., Hellsten, K., Homanics, G. E., and Korpi, E. R. (2010). Prototypic GABA(A) receptor agonist muscimol acts preferentially through forebrain high-affinity binding sites. Neuropsychopharmacology 35, 999-1007.
6. Chandra, D., Jia, F., Liang, J., Peng, Z., Suryanarayanan, A., Werner, D. F., Spigelman, I., Houser, C. R., Olsen, R. W., Harrison, N. L., and Homanics, G. E. (2006). GABAA receptor α4 subunits mediate extrasynaptic inhibition in thalamus and dentate gyrus and the action of gaboxadol. Proc. Natl. Acad. Sci. U.S.A. 103, 15230-15235.
7. Chandra, D., Werner, D. F., Olsen, R. W., Harrison, N. L., and Homanics, G. E. (2008). Normal acute behavioral responses to moderate/high dose ethanol in GABAA receptor α4 subunit knockout mice. Alcohol. Clin. Exp. Res. 32, 10-18.
8. Cook, J. B., Foster, K. L., Eiler, W. J. II, McKay, P. F., Woods, J. II, Harvey, S. C., Garcia, M., Grey, C., McCane, S., Mason, D., Cummings, R., Li, X., Cook, J. M., and June, H. L. (2005). Selective GABAA alpha5 benzodiazepine inverse agonist antagonizes the neurobehavioral actions of alcohol. Alcohol. Clin. Exp. Res. 29, 1390-1401.
9. Dar, M. S. (1995). Antagonism by intracerebellar Ro15-4513 of acute ethanol-induced motor incoordination in mice. Pharmacol. Biochem. Behav. 52, 217-223.
10. Fleming, R. L., Wilson, W. A., and Swartzwelder, H. S. (2007). The magnitude and ethanol sensitivity of tonic GABAA receptor mediated inhibition in dentate gyrus changes from adolescence to adulthood. J. Neurophysiol. 97, 3806-3811.
11. Glowa, J. R., Crawley, J., Suzdak, P. D., and Paul, S. M. (1988). Ethanol and the GABA receptor complex: studies with the partial inverse benzodiazepine receptor agonist Ro 15-4513. Pharmacol. Biochem. Behav. 31, 767-772.
12. A receptors. Proc. Natl. Acad. Sci. U.S.A. 103, 8546-8551.
13. Hanchar, H. J., Dodson, P. D., Olsen, R. W., Otis, T. S., and Wallner, M. (2005). Alcohol-induced motor impairment caused by increased extrasynaptic GABA(A) receptor activity. Nat. Neurosci. 8, 339-345.
14. Harris, B. D., Moody, E. J., Gu, Z. Q., and Skolnick, P. (1995). Contribution of " diazepam-insensitive" GABAA receptors to the alcohol antagonist properties of Ro 15-4513 and related imidazobenzodiazepines. Pharmacol. Biochem. Behav. 52, 113-118.
15. Hoffman, P. L., Tabakoff, B., Szabo, G., Suzdak, P. D., and Paul, S. M. (1987). Effect of an imidazobenzodiazepine, Ro15-4513, on the incoordination and hypothermia produced by ethanol and pentobarbital. Life Sci. 41, 611-619.
16. Homanics, G. E., Ferguson, C., Quinlan, J. J., Daggett, J., Snyder, K., Lagenaur, C., Mi, Z. P., Wang, X. H., Grayson, D. R., and Firestone, L. L. (1997). Gene knockout of the α6 subunit of the γ-aminobutyric acid type A receptor: lack of effect on responses to ethanol, pentobarbital, and general anesthetics. Mol. Pharmacol. 51, 588-596.
17. Hu, W. Y., Reiffenstein, R. J., and Wong, L. (1987). Interaction between flurazepam and ethanol. Alcohol Drug Res. 7, 107-117.
18. Khanna, J. M., Kalant, H., Chau, A., and Shah, G. (1998). Rapid tolerance and crosstolerance to motor impairment effects of benzodiazepines, barbiturates, and ethanol. Pharmacol. Biochem. Behav. 59, 511-519.
19. Kolata, G. (1986). New drug counters alcohol intoxication. Science 234, 1198-1199.
20. A receptor subtypes? the current evidence is ambiguous. Alcohol 41, 163-176.
21. A receptor α4 subunit deletion on synaptic and extrasynaptic currents in mouse dentate granule cells. Alcohol. Clin. Exp. Res. 32, 19-26.
22. A receptors. Front. Neurosci. 5:3. doi: 10.3389/fnins.2011.00003
23. Lister, R. G., and Nutt, D. J. (1988). Ro15-4513 and its interaction with ethanol. Adv. Alcohol Subst. Abuse 7, 119-123.
24. Lovinger, D. M., and Homanics, G. E. (2007). Tonic for what ails us? high-affinity GABA(A) receptors and alcohol. Alcohol 41, 139-143.
25. McGinnis, J. M., and Foege, W. H. (1999). Mortality and morbidity attributable to use of addictive substances in the United States. Proc. Assoc. Am. Physicians 111, 109-118.
26. Mehta, A. K., Marutha Ravindran, C. R., and Ticku, M. K. (2007). Low concentrations of ethanol do not affect radioligand binding to the δ-subunit-containing GABAA receptors in the rat brain. Brain Res. 1165, 15-20.
27. Mihalek, R. M., Bowers, B. J., Wehner, J. M., Kralic, J. E., VanDoren, M. J., Morrow, A. L., and Homanics, G. E. (2001). GABAa-receptor delta subunit knockout mice have multiple defects in behavioral responses to ethanol. Alcohol. Clin. Exp. Res. 25, 1708-1718.
28. Mody, I., Glykys, J., and Wei, W. (2007). A new meaning for " Gin & Tonic" : tonic inhibition as the target for ethanol action in the brain. Alcohol 41, 145-153.
29. Olsen, R. W., Hanchar, H. J., Meera, P., and Wallner, M. (2007). GABAA receptor subtypes: the " one glass of wine" receptors. Alcohol 41, 201-209.
30. Samson, H. H., Haraguchi, M., Tolliver, G. A., and Sadeghi, K. G. (1989). Antagonism of ethanol-reinforced behavior by the benzodiazepine inverse agonists Ro15-4513 and FG 7142: relation to sucrose reinforcement. Pharmacol. Biochem. Behav. 33, 601-608.
31. A receptors to increase tonic inhibition. Alcohol 41, 211-221.
32. Stephens, D. N., Pistovcakova, J., Worthing, L., Atack, J. R., and Dawson, G. R. (2005). Role of GABAA alpha5-containing receptors in ethanol reward: the effects of targeted gene deletion, and a selective inverse agonist. Eur. J. Pharmacol. 526, 240-250.
33. Stinchcomb, A., Bowers, B. J., and Wehner, J. M. (1989). The effects of ethanol and Ro 15-4513 on elevated plus-maze and rotarod performance in long-sleep and short-sleep mice. Alcohol 6, 369-376.
34. A receptors: functional selectivity for extrasynaptic receptors is dependent on the absence of gamma2. J. Pharmacol. Exp. Ther. 316, 1351-1359.
35. A receptors are a target for alcohol. Nat. Neurosci. 5, 721-722.
36. Suzdak, P. D., Glowa, H. R., Crawley, J. N., Schwartz, R. D., Skolnick, P., and Paul, S. M. (1986). A selective imidazobenzodiazepine antagonist of ethanol in the rat. Science 234, 1243-1247.
37. Suzdak, P. D., Paul, S. M., and Crawley, J. N. (1988). Effects of Ro15-4513 and other benzodiazepine receptor inverse agonists on alcohol-induced intoxication in the rat. J. Pharmacol. Exp. Ther. 245, 880-886.
38. Wallner, M., Hanchar, H. J., and Olsen, R. W. (2003). Ethanol enhances α4β3δ and α6β3δ γ-aminobutyric acid type A receptors at low concentrations known to affect humans. Proc. Natl. Acad. Sci. U.S.A. 100, 15218-15223.
39. Wallner, M., Hanchar, H. J., and Olsen, R. W. (2006a). Low dose acute alcohol effects on GABAA receptor subtypes. Pharmacol. Ther. 112, 513-528.
40. Wallner, M., Hanchar, H. J., and Olsen, R. W. (2006b). Low-dose alcohol actions on α4β3δ GABAA receptors are reversed by the behavioral alcohol antagonist Ro15-4513. Proc. Natl. Acad. Sci. U.S.A. 103, 8540-8545.
41. Wallner, M., and Olsen, R. W. (2008). Physiology and pharmacology of alcohol: the imidazobenzodiazepine alcohol antagonist site on subtypes of GABAA receptors as an opportunity for drug development? Br. J. Pharmacol. 154, 288-298.
42. Wei, W., Faria, L. C., and Mody, I. (2004). Low ethanol concentrations selectively augment the tonic inhibition mediated by δ subunit-containing GABAA receptors in hippocampal neurons. J. Neurosci. 24, 8379-8382.
43. Yamashita, M., Marszalec, W., Yeh, J. Z., and Narahashi, T. (2006). Effects of ethanol on tonic GABA currents in cerebellar granule cells and mammalian cells recombinantly expressing GABA(A) receptors. J. Pharmacol. Exp. Ther. 319, 431-438.