The positive allosteric modulator of the GABAB receptor, rac-BHFF, suppresses alcohol self-administration

Drug and Alcohol Dependence

Volumn 109, Issue 1-3, 2010, Pages 96-103

  Maccioni, Paola ^a   Thomas, Andrew W ^b   Carai, Mauro A M ^a   Gessa, Gian Luigi ^a   Malherbe, Pari ^b   Colombo, Giancarlo ^a  

^a CNR   (Italy)

^b F HOFFMANN LA ROCHE LTD   (Switzerland)

Author keywords

GABAB receptor; Operant oral alcohol self administration; Positive allosteric modulators of the GABAB receptor; Rac BHFF; Reinforcing properties of alcohol; Sardinian alcohol preferring (sP) rats

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; 5,7 DI TERT BUTYL 3 HYDROXY 3 TRIFLUOROMETHYL 3H BENZOFURAN 2 ONE; GABAERGIC RECEPTOR AFFECTING AGENT; SUCROSE; UNCLASSIFIED DRUG;

ALCOHOL BLOOD LEVEL; ALCOHOL CONSUMPTION; ALLOSTERISM; ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG DOSE COMPARISON; LATENT PERIOD; LOCOMOTION; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; REINFORCEMENT;

ALCOHOL DRINKING; ANALYSIS OF VARIANCE; ANIMALS; BENZOFURANS; CENTRAL NERVOUS SYSTEM DEPRESSANTS; CONDITIONING, OPERANT; ETHANOL; GABA MODULATORS; MALE; MOTOR ACTIVITY; RATS; RECEPTORS, GABA-B; REINFORCEMENT SCHEDULE; SUCROSE;

RATTUS;

EID: 77953023396     PISSN: 03768716     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.drugalcdep.2009.12.019     Document Type: Article

References (63)

1. Addolorato G., Caputo F., Capristo E., Colombo G., Gessa G.L., Gasbarrini G. Ability of baclofen in reducing alcohol craving and intake: II-preliminary clinical evidence. Alcohol. Clin. Exp. Res. 2000, 24:67-71.
2. Addolorato G., Caputo F., Capristo E., Domenicali M., Bernardi M., Janiri L., Agabio R., Colombo G., Gessa G.L., Gasbarrini G. Baclofen efficacy in reducing alcohol craving and intake-a preliminary double-blind randomised controlled study. Alcohol Alcohol. 2002, 37:504-508.
3. Addolorato G., Caputo F., Capristo E., Janiri L., Bernardi M., Agabio R., Colombo G., Gessa G.L., Gasbarrini G. Rapid suppression of alcohol withdrawal syndrome by baclofen. Am. J. Med. 2002, 112:226-229.
4. Addolorato G., Leggio L., Abenavoli L., DeLorenzi G., Parente A., Caputo F., Janiri L., Capristo E., Rapaccini G.L., Gasbarrini G. Suppression of alcohol delirium tremens by baclofen administration: a case report. Clin. Neuropharmacol. 2003, 26:258-262.
5. Addolorato G., Leggio L., Abenavoli L., Agabio R., Caputo F., Capristo E., Colombo G., Gessa G.L., Gasbarrini G. Baclofen in the treatment of alcohol withdrawal syndrome: a randomized comparative study versus diazepam. Am. J. Med. 2006, 119:27613-27618.
6. Addolorato G., Leggio L., Ferrulli A., Cardone S., Vonghia L., Mirijello A., Abenavoli L., D'Angelo C., Caputo F., Zambon A., Haber P.S., Gasbarrini G. Effectiveness and safety of baclofen for maintenance of alcohol abstinence in alcohol-dependent patients with liver cirrhosis: randomised, double-blind controlled study. Lancet 2007, 370:1915-1922.
7. Agabio R., Marras P., Addolorato G., Carpiniello B., Gessa G.L. Baclofen suppresses alcohol intake and craving for alcohol in a schizophrenic alcohol-dependent patient: a case report. J. Clin. Psychopharmacol. 2007, 27:319-320.
8. Ameisen O. Complete and prolonged suppression of symptoms and consequences of alcohol-dependence using high-dose baclofen: a self-case report of a physician. Alcohol Alcohol. 2005, 40:147-150.
9. Anstrom K.K., Cromwell H.C., Markowski T., Woodward D.J. Effect of baclofen on alcohol and sucrose self-administration in rats. Alcohol. Clin. Exp. Res. 2003, 27:900-908.
10. Arias C., Mlewski E.C., Molina J.C., Spear N.E. Naloxone and baclofen attenuate ethanol's locomotor-activating effects in preweanling Sprague-Dawley rats. Behav. Neurosci. 2009, 123:172-180.
11. Bechtholt A.J., Cunningham C.L. Ethanol-induced conditioned place preference is expressed through a ventral tegmental area dependent mechanism. Behav. Neurosci. 2005, 119:213-223.
12. B receptor agonists reduce operant ethanol self-administration and enhance ethanol sedation in C57BL/6J mice. Psychopharmacology 2004, 174:358-366.
13. B receptor modulation of ethanol-stimulated activity in mice. Neuroscience 2002, 115:185-200.
14. B agonists on sensitization to the locomotor stimulant effects of ethanol in DBA/2 J mice. Psychopharmacology 1999, 141:197-205.
15. Bucknam W. Suppression of symptoms of alcohol dependence and craving using high dose baclofen. Alcohol Alcohol. 2007, 42:158-160.
16. B receptor mRNAs in the rat brain and peripheral organs. Life Sci. 1999, 64:1321-1328.
17. Chester J.A., Cunningham C.L. Baclofen alters ethanol-stimulated activity but not conditioned place preference or taste aversion in mice. Pharmacol. Biochem. Behav. 1999, 63:325-331.
18. Colombo G., Agabio R., Lobina C., Reali R., Zocchi A., Fadda F., Gessa G.L. Sardinian alcohol-preferring rats: a genetic animal model of anxiety. Physiol. Behav. 1995, 57:1181-1185.
19. Colombo G., Agabio R., Carai M.A.M., Lobina C., Pani M., Reali R., Addolorato G., Gessa G.L. Ability of baclofen in reducing alcohol intake and withdrawal severity: I-preclinical evidence. Alcohol. Clin. Exp. Res. 2000, 24:58-66.
20. B receptor agonists baclofen and CGP 44532 prevent acquisition of alcohol drinking behaviour in alcohol-preferring rats. Alcohol Alcohol. 2002, 37:499-503.
21. Colombo G., Serra S., Brunetti G., Vacca G., Carai M.A.M., Gessa G.L. Suppression by baclofen of alcohol deprivation effect in Sardinian alcohol-preferring (sP) rats. Drug Alcohol Depend. 2003, 70:105-108.
22. Colombo G., Vacca G., Serra S., Brunetti G., Carai M.A.M., Gessa G.L. Baclofen suppresses motivation to consume alcohol in rats. Psychopharmacology 2003, 167:221-224.
23. Colombo G., Serra S., Vacca G., Carai M.A.M., Gessa G.L. Baclofen-induced suppression of alcohol deprivation effect in Sardinian alcohol-preferring (sP) rats exposed to different alcohol concentrations. Eur. J. Pharmacol. 2006, 550:123-126.
24. Cott J., Carlsson A., Engel J., Lindqvist M. Suppression of ethanol-induced locomotor stimulation by GABA-like drugs. Naunyn Schmiedeberg's Arch. Pharmacol. 1976, 295:203-209.
25. B receptor-positive modulator GS39783 (N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine): anxiolytic-like activity without side effects associated with baclofen or benzodiazepines. J. Pharmacol. Exp. Ther. 2004, 310:952-963.
26. B agonist baclofen in rats. Alcohol. Clin. Exp. Res. 2006, 30:812-818.
27. Daoust M., Saligaut C., Lhuintre J.P., Moore N., Flipo J.L., Boismare F. GABA transmission, but not benzodiazepine receptor stimulation, modulates ethanol intake by rats. Alcohol 1987, 4:469-472.
28. Evans S.M., Bisaga A. Acute interaction of baclofen in combination with alcohol in heavy social drinkers. Alcohol. Clin. Exp. Res. 2009, 33:19-30.
29. File S.E., Zharkovsky A., Gulati K. Effects of baclofen and nitrendipine on ethanol withdrawal responses in the rat. Neuropharmacology 1991, 30:183-190.
30. Flannery B.A., Garbutt J.C., Cody M.W., Renn W., Grace K., Osborne M., Crosby K., Morreale M., Trivette A. Baclofen for alcohol dependence: a preliminary open-label study. Alcohol. Clin. Exp. Res. 2004, 28:1517-1523.
31. B receptor ligands in animal tests of depression and anxiety. Pharmacol. Rep. 2007, 59:645-655.
32. B receptors. Bioorg. Med. Chem. Lett. 2007, 17:6206-6211.
33. B, receptor agonist. Alcohol. Clin. Exp. Res. 2009, 33:108-120.
34. B receptors in mediating the stimulatory effects of ethanol in mice. Psychopharmacology 1993, 111:219-224.
35. B receptor positive modulator CGP7930 in rodents. Neuropharmacology 2008, 54:854-862.
36. Janak P.H., Gill T.M. Comparison of the effects of allopregnanolone with direct GABAergic agonists on ethanol self-administration with and without concurrently available sucrose. Alcohol 2003, 30:1-7.
37. Kelley A.E. Locomotor activity and exploration. Behavioural Neuroscience: A Practical Approach 1993, vol. II:1-21. IRL Press, Oxford.
38. Knapp D.J., Overstreet D.H., Breese G.R. Baclofen blocks expression and sensitization of anxiety-like behavior in an animal model of repeated stress and ethanol withdrawal. Alcohol. Clin. Exp. Res. 2007, 31:582-595.
39. Langmead C.J., Christopoulos A. Allosteric agonists of 7TM receptors: expanding the pharmacological toolbox. Trends Pharmacol. Sci. 2006, 27:475-481.
40. Leite-Morris K.A. The effects of ventral tegmental baclofen on ethanol-induced motor stimulation and sensitization in DBA/2 mice. Alcohol. Clin. Exp. Res. 2004, 28:182A.
41. Leite-Morris K.A., Czachowski C.L. Intra-ventral tegmental area microinjections of a GABA receptor agonist dose-dependently attenuate ethanol seeking in rats. Alcohol. Clin. Exp. Res. 2006, 30:182A.
42. Leite-Morris K.A., Kerestes H.B., Colombo G. Intra-ventral tegmental area injection of the GABA B receptor positive allosteric modulator GS39783 inhibits ethanol seeking behavior in rats. Alcohol. Clin. Exp. Res. 2009, 33:226A.
43. B receptor allosteric modulator CGP7930, like baclofen, reduces operant self-administration of ethanol in alcohol-preferring rats. Neuropharmacology 2006, 50:632-639.
44. Maccioni P., Serra S., Vacca G., Orr A., Pes D., Agabio R., Addolorato G., Carai M.A.M., Gessa G.L., Colombo G. Baclofen-induced reduction of alcohol reinforcement in alcohol-preferring rats. Alcohol 2005, 36:161-168.
45. B receptor, GS39783, on alcohol self-administration in alcohol-preferring rats. Psychopharmacology 2007, 193:171-178.
46. Maccioni P., Bienkowski P., Carai M.A.M., Gessa G.L., Colombo G. Baclofen attenuates cue-induced reinstatement of alcohol-seeking behavior in Sardinian alcohol-preferring (sP) rats. Drug Alcohol Depend. 2008, 95:284-287.
47. B receptor direct agonist, baclofen. Alcohol. Clin. Exp. Res. 2008, 32:1558-1564.
48. B receptor, BHF177, in alcohol-preferring rats. Alcohol. Clin. Exp. Res. 2009, 33:1749-1756.
49. B receptors. Br. J. Pharmacol. 2008, 154:797-811.
50. B receptors in the modulation of anxiety- and antidepressant-like behavior. Neuropsychopharmacology 2004, 29:1050-1062.
51. Moore E.M., Boehm S.L. Site-specific microinjection of baclofen into the anterior ventral tegmental area reduces binge-like ethanol intake in male C57BL/6J mice. Behav. Neurosci. 2009, 123:555-563.
52. B receptors in the rat gastrointestinal tract. Neurochem. Res. 1996, 21:211-215.
53. B receptor, CGP7930 and GS39783, on alcohol intake in alcohol-preferring rats. Eur. J. Pharmacol. 2005, 525:105-111.
54. Pandey S.C., Zhang H., Roy A., Xu T. Deficits in amygdaloid cAMP-responsive element-binding protein signaling play a role in genetic predisposition to anxiety and alcoholism. J. Clin. Invest. 2005, 115:2762-2773.
55. B receptors decreased nicotine self-administration and counteracted nicotine-induced enhancement of brain reward function in rats. J. Pharmacol. Exp. Ther. 2008, 326:306-314.
56. Perfumi M., Santoni M., Ciccocioppo R., Massi M. Blockade of γ-aminobutyric acid receptors does not modify the inhibition of ethanol intake induced by Hypericum perforatum in rats. Alcohol Alcohol. 2002, 37:540-546.
57. Quintanilla M.E., Perez E., Tampier L. Baclofen reduces ethanol intake in high-alcohol-drinking University of Chile bibulous rats. Addict. Biol. 2008, 13:326-336.
58. Shen E.H., Dorow J., Harland R., Burkhart-Kasch S., Phillips T.J. Seizure sensitivity and GABAergic modulation of ethanol sensitivity in selectively bred FAST and SLOW mouse lines. J. Pharmacol. Exp. Ther. 1998, 287:606-615.
59. Stromberg M.F. The effect of baclofen alone and in combination with naltrexone on ethanol consumption in the rat. Pharmacol. Biochem. Behav. 2004, 78:743-750.
60. B receptors by 2,6-di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501. Mol. Pharmacol. 2001, 60:963-971.
61. Urwyler S., Pozza M.F., Lingenhoehl K., Mosbacher J., Lampert C., Froestl W., Koller M., Kaupmann K. N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of gamma-aminobutyric acidB receptor function. J. Pharmacol. Exp. Ther. 2003, 307:322-330.
62. Walker B.M., Koob G.F. The γ-aminobutyric acid-B receptor agonist baclofen attenuates responding for ethanol in ethanol-dependent rats. Alcohol. Clin. Exp. Res. 2007, 31:11-18.
63. B receptors play a role in the development of tolerance to ethanol in mice. Psychopharmacology 2001, 153:415-424.