Reduction of excessive alcohol drinking by a novel GABAB receptor positive allosteric modulator ADX71441 in mice

Psychopharmacology

Volumn 231, Issue 2, 2014, Pages 333-343

  Hwa, Lara S ^a   Kalinichev, Mikhail ^c   Haddouk, Hasnaà ^c   Poli, Sonia ^c   Miczek, Klaus A ^a,b  

^a TUFTS UNIVERSITY   (United States)

^b TUFTS UNIVERSITY SCHOOL OF MEDICINE   (United States)

^c Addex Therapeutics SA   (Switzerland)

Author keywords

Drinking in the dark; Ethanol; GABAB receptor; intermittent access to alcohol; Naltrexone; Positive allosteric modulator

Indexed keywords

4 AMINOBUTYRIC ACID B RECEPTOR; ADX 71441; DRUGS USED IN THE TREATMENT OF ADDICTION; NALTREXONE; UNCLASSIFIED DRUG; 4 AMINOBUTYRIC ACID B RECEPTOR STIMULATING AGENT; ADX71441; BACTERIAL PROTEIN; TRANSCRIPTION FACTOR;

ALCOHOL CONSUMPTION; ALCOHOLISM; ALLOSTERISM; ANIMAL BEHAVIOR; ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG BLOOD LEVEL; DRUG DOSE COMPARISON; DRUG ELIMINATION; DRUG HALF LIFE; DRUG MEGADOSE; DRUG POTENCY; FLUID INTAKE; MALE; MAXIMUM PLASMA CONCENTRATION; MOTOR ACTIVITY; MOUSE; NONHUMAN; PRIORITY JOURNAL; REPEATED DRUG DOSE; TIME TO MAXIMUM PLASMA CONCENTRATION; ANIMAL; BINGE DRINKING; DISEASE MODEL; DOSE RESPONSE; DRINKING; DRINKING BEHAVIOR; DRUG EFFECTS; DRUG THERAPY;

ALCOHOL DETERRENTS; ALCOHOL DRINKING; ALLOSTERIC REGULATION; ANIMALS; BACTERIAL PROTEINS; BINGE DRINKING; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRINKING; GABA-B RECEPTOR AGONISTS; MALE; MICE; NALTREXONE; TRANSCRIPTION FACTORS;

EID: 84892820843     PISSN: 00333158     EISSN: 14322072     Source Type: Journal    
DOI: 10.1007/s00213-013-3245-z     Document Type: Article

References (74)

1. Addolorato G, Leggio L (2010) Safety and efficacy of baclofen in the treatment of alcohol-dependent patients. Current pharmaceutical design 16(19):2113-2117
2. Addolorato G, Caputo F, Capristo E, Demonicali M, Bernardi M, Janiri L, Agabio R, Colombo G, Gessa GL, Gasbarrini G (2002) Baclofen efficacy in reducing alcohol craving and intake: a preliminary double-blind randomized controlled study. Alcohol and Alcoholism 37(5):504-508
3. Addolorato G, Leggio L, Ferrulli A, Cardone S, Vonghia L, Mirijello A, Abenavoli L, D'Angelo C, Caputo F, Zambon A, Haber PS, Gasbarrini G (2007) Effectiveness and safety of baclofen for maintenance of alcohol abstinence in alcohol-dependent patients with liver cirrhosis: randomised, double-blind controlled study. Lancet 370(9603):1915-1922
4. Anstrom KK, Cromwell HC, Markowski T, Woodward DJ (2003) Effect of baclofen and alcohol and sucrose self-administration in rats. Alcohol Clin Exp Res 27(6):900-908
5. Anton RF, O'Malley SS, Ciraulo DA, Cisler RA, Couper D, Donavan DM, Gastfriend DR, Hosking JD et al (2006) Combined pharmacotherapies and behavioral interventions for alcohol dependence. JAMA 295(17):2003-2017
6. Bell RL, Rodd ZA, Lumeng L, Murphy JM, McBride WJ (2006) Review: the alcohol-preferring P rat and animal models of excessive alcohol drinking. Addict Biol 11(3):270-288
7. Bowery NG (2006) GABAB receptor: a site of therapeutic benefit. Current opinion in pharmacology 6(1):37-43
8. Carmen B, Angeles M, Ana M, Maria AJ (2004) Efficacy and safety of naltrexone and acamprosate in the treatment of alcohol dependence: a systematic review. Addiction 99(7):811-828
9. Ciccarelli A, Calza A, Panzanelli P, Concas A, Giustetto M, Sassoè-Pognetto M (2012) Organization of GABAergic synaptic circuits in the rat ventral tegmental area. PloS One 7(10):e46250
10. Colombo G, Lobina C, Carai MA, Gessa GL (2006) Review: phenotypic characterization of genetically selected Sardinian alcohol-preferring (sP) and-non-preferring (sNP) rats. Addict Biol 11(3):324-338
11. Colombo G, Vacca G, Serra S, Brunetti G, Carai MA, Gessa GL (2003). Baclofen suppresses motivation to consume alcohol in rats. Psychopharmacology 167(3): 221-224
12. Conn PJ, Christopoulos A, Lindsley CW (2009) Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nature reviews Drug discovery 8(1):41-54
13. Cousins MS, Roberts D, de Wit HD (2002) GABAB receptor agonists for the treatment of drug addiction: a review of recent findings. Drug and alcohol dependence 65(3):209-220
14. Cox BR, Olney JJ, Lowery-Gionta EG, Sprow GM, Rinker JA, Navarro M, Kash TL, Thiele TE (2013) Repeated cycles of binge-like ethanol (EtOH)-drinking in male C57BL/6J mice augments subsequent voluntary etOH intake but not other dependence-like phenotypes. Alcohol Clin Exp Res. doi: 10.1111/acer.12145
15. Crabbe JC, Harkness JH, Spence SE, Huang LC, Metten P (2012) Intermittent availability of ethanol does not always lead to elevated drinking in mice. Alcohol and alcoholism 47(5):509-517
16. Cryan JF, Kelly PH, Chaperon F, Gentsch C, Mombereau C, Lingenhoehl K, Froestl W, Bettler B, Kaupmann K, Spooren WP (2004) Behavioral characterization of the novel GABAB receptor-positive modulator GS39783 (N, N′- dicyclopentyl-2-methyulsulfanyl-5natro-pyrimidine-4,6-diamine): anxiolytic-like activity without side effects associated with baclofen or benzodiazepines. J Pharmacol Exp Ther 310:952-963
17. Czachowski CL, Legg BH, Stansfield KH (2006) Ethanol and sucrose seeking and consumption following repeated administration of the GABAB agonist baclofen in rats. Alcohol Clin Exp Res 30(5):812-818
18. Daoust M, Saligaut C, Lhuintre JP, Moore N, Flipo JL, Boismare F (1987) GABA transmission, but not benzodiazepine receptor stimulation, modulates ethanol intake by rats. Alcohol 4(6):469-472
19. Evans SM, Bisaga A (2009) Acute interaction of baclofen in combination with alcohol in heavy social drinkers. Alcohol Clin Exp Res 33(1):19-30
20. Fadda P, Scherma M, Fresu A, Collu M, Fratta W (2003) Baclofen antagonizes nicotine-, cocaine-, and morphine-induced dopamine release in the nucleus accumbens of rat. Synapse 50(1):1-6
21. Heilig M, Goldman D, Berrettini W, O'Brien CP (2011) Pharmacogenetic approaches to the treatment of alcohol addiction. Nat Rev Neurosci 12(11):670-684
22. Hwa LS, Chu A, Levinson SA, Kayyali TM, DeBold JF, Miczek KA (2011) Persistent escalation of alcohol drinking in C57BL/6J mice with intermittent access to 20% ethanol. Alcohol Clin Exp Res 35(11):1938-1947
23. Hwa LS, DeBold JF, Miczek KA (2013) Alcohol in excess: CRF1 receptors in the rat and mouse VTA and DRN. Psychopharmacology 225(2):313-327
24. B receptor positive allosteric modulator CGP7930 in rodents. Neuropharmacology 54(5):854-862
25. B receptor, with potential for treatment of anxiety, pain and spasticity. J Pharmacol Exp Ther (under review).
26. B receptor, shows efficacy in rodent models of overactive bladder. The British Journal of Pharmacology (under revision).
27. Kalivas PW, Duffy P, Eberhardt H (1990) Modulation of A10 dopamine neurons by gamma-aminobutyric agonists. J Pharmacol Exp Ther 253(2):858-866
28. Kamdar NK, Miller SA, Syed YM, Bhayana R, Gupta T, Rhodes JS (2007) Acute effects of naltrexone and GBR12909 on ethanol drinking-in-the-dark in C57BL/6J mice. Psychopharmacology 192(2):207-217
29. Kranzler HR, Kirk J (2001) Efficacy of naltrexone and acamprosate for alcoholism treatment: a meta-analysis. Alcohol Clin Exp Res 25(9):1335-1341
30. Langmead CJ, Christopolous A (2006) Allosteric agonists of 7TM receptors: expanding the pharmacological toolbox. Trends Pharmacol Sci 27(9):475-481
31. Leggio L, Ferrulli A, Zambon Z, Caputo F, Kenna GA, Swift RM, Addolorato G (2012) Baclofen promotes alcohol abstinence in alcohol dependent cirrhotic patients with hepatitis C virus (HCV) infection. Addict Behav 37(4):561-564
32. Leggio L, Zywiak WH, McGeary JE, Edwards S, Fricchhione SR, Shoaff JF, Addolorato G, Swift RM, Kenna GA (2013) A human laboratory pilot study with baclofen in alcoholic individuals. Pharmacol Biochem Behav 103(4):784-791
33. Leite-Morris KA, Kerestes HB, Colombo G (2009) Intra-ventral tegmental area injection of the GABA B receptor positive allosteric modulator GS39783 inhibits ethanol seeking behavior in rats. Alcohol: Clinical and Experimental Research 33:226A
34. Li X, Risbrough VB, Cates-Gatto C, Kaczanowska K, Finn MG, Roberts AJ, Markou A (2013) Comparison of the effects of the GABAB receptor positive modulator BHF177 and the GABAB receptor agonist baclofen on anxiety-like behavior, learning, and memory in mice. Neuropharmacology 70:156-167
35. Liang JH, Chen F, Krstew E, Cowen MS, Carroll FY, Crawford D, Beart P, Lawrence AJ (2006) The GABAB receptor allosteric modulator CGP7930, like baclofen, reduces operant self-administration of ethanol in alcohol-preferring rats. Neuropharmacology 50(5):632-639
36. B receptor, rac-BHFF, in alcohol-preferring rats. Alcohol 47(1):69-73
37. Maccioni P, Bienkowski P, Carai MA, Gessa GL, Colombo G (2008a) Baclofen attenuates cue-induced reinstatement of alcohol-seeking behavior in Sardinian alcohol-preferring (sP) rats. Drug and Alcohol Dependence 95(3):284-287
38. Maccioni P, Carai MA, Kaupmann K, Guery S, Froestl W, Leite-Morris KA, Gessa GL, Colombo G (2009) Reduction of alcohol's reinforcing and motivational properties by the positive allosteric modulator of the GABAB receptor, BHF177, in alcohol-preferring rats. Alcohol Clin Exp Res 33(10):1749-1756
39. Maccioni P, Fantini N, Froestl W, Carai MA, Gessa GL, Colombo G (2008b) Specific reduction of alcohol's motivational properties by the positive allosteric modulator of the GABAB receptor, GS39783 - comparison with the effect of the GABAB receptor direct agonist, baclofen. Alcohol Clin Exp Res 32(9):1558-1564
40. Maccioni P, Pes D, Orrù A, Froestl W, Gessa GL, Carai MA, Colombo G (2007) Reducing effect of the positive allosteric modulator of the GABAB receptor, GS39783, on alcohol self-administration in alcohol-preferring rats. Psychopharmacology 193(2):171-178
41. Maccioni P, Serra S, Vacca G, Orrù A, Pes D, Agabio R, Addolorato G, Carai MAM, Gessa GL, Colombo G (2005) Baclofen-induced reduction of alcohol reinforcement in alcohol-preferring rats. Alcohol 36(3):161-168
42. B receptor, rac-BHFF, suppresses alcohol self-administration. Drug and alcohol dependence 109(1):96-103
43. Maccioni P, Zaru A, Loi B, Lobina C, Carai MA, Gessa GL, Capra A, Mugnaini C, Pasquini S, Corelli F, Hyytiä P, Lumeng L, Colombo G (2012) Comparison of the effect of the GABAB receptor agonist, baclofen, and the positive allosteric modulator of the GABAB receptor, GS39783, on alcohol self-administration in 3 different lines of alcohol-preferring rats. Alcohol Clin Exp Res 36(10):1748-1766
44. May LT, Christopoulos A (2003) Allosteric modulators of G-protein-coupled receptors. Curr Opin Pharmacol 3(5):551-556
45. Melendez RI (2011) Intermittent (every-other-day) drinking induces rapid escalation of ethanol intake and preference in adolescent and adult C57BL/6J mice. Alcohol Clin Exp Res 35(4):652-658
46. Mohapatra S, Patra J, Popova S, Duhig A, Rehm J (2010) Social cost of heavy drinking and alcohol dependence in high-income countries. International Journal of Public Health 55(3):149-157
47. Mombereau C, Kaupmann K, van der Putten H, Cryan JF (2004a) Altered response to benzodiazepine anxiolytics in mice lacking GABA B(1) receptors. Eur J Pharmacol 497:119-120
48. Mombereau C, Kaupmann K, Froestl W, Sansig G, van der Putten H, Cryan JF (2004b) Genetic and pharmacological evidence of a role for GABAB receptors in the modulation of anxiety- and antidepressant-like behavior. Neuropsychopharmacology 29:1050-1062
49. Moore EM, Boehm SL (2009) Site-specific microinjection of baclofen into the anterior ventral tegmental area reduces binge-like ethanol intake in male C57BL/6J mice. Behavioral neuroscience 123(3):555
50. Moore EM, Serio KM, Goldfarb KJ, Stepanovska S, Linsenbardt DN, Boehm SL II (2007) GABAergic modulation of binge-like ethanol intake in C57BL/6J mice. Pharmacol Biochem Behav 88(1):105-113
51. National Research Council (2011) Guide for the care and use and laboratory animals: eighth edition. National Academies Press, Washington
52. O'Malley SS, Jaffe AJ, Chang G, Schottenfeld RS, Meyer RE, Rounsaville B (1992) Naltrexone and coping skills therapy for alcohol dependence - a controlled study. Arch Gen Psychiatry 49(11):881-887
53. Omelchenko N, Sesack SR (2009) Ultrastructural analysis of local collaterals of rat ventral tegmental area neurons: GABA phenotype and synapses onto dopamine and GABA cells. Synapse 63(10):895-906
54. Orrù A, Fujani D, Cassina C, Conti M, Di Clemente A, Cervo L (2012) Operant, oral alcoholic beer self-administration by C57BL/6J mice: effect of BHF177, a positive allosteric modulator of GABAB receptors. Psychopharmacology 222(4):685-700
55. Orrù A, Lai P, Lobina C, Maccioni P, Piras P, Scanu L, Froestl W, Gessa GL, Carai MA, Colombo G (2005) Reducing effect of the positive allosteric modulators of the GABAB receptor, CGP7930 and GS39783, on alcohol intake in alcohol-preferring rats. Eur J Pharmacol 525(1):105-111
56. B receptor positive allosteric modulator, 2-{1-[2-(4-chlorophenyl)-5- methylpyrazolo[1,5-a]pyrimidin-7-yl]-2-piperidinyl}ethanol (CMPPE). Neuropharmacology 61(5):957-966
57. Petry NM (1997) Benzodiazepine-GABA modulation of concurrent ethanol and sucrose reinforcement in the rat. Experimental and clinical psychopharmacology 5(3):183
58. Rhodes JS, Best K, Belknap JK, Finn DA, Crabbe JC (2005) Evaluation of a simple model of ethanol drinking to intoxication in C57BL/6J mice. Physiology & behavior 84(1):53-63
59. Rhodes JS, Ford MM, Yu CH, Brown LL, Finn DA, Garland T, Crabbe JC (2007) Mouse inbred strain differences in ethanol drinking to intoxication. Genes, Brain and Behavior 6(1):1-18
60. B receptor. Pharmacol Biochem Behav 102(2):224-232
61. Rosenwasser AM, Fixaris MC, Crabbe JC, Brooks PC, Ascheid S (2012) Escalation of intake under intermittent ethanol access in diverse mouse genotypes. Addict Biol 18(3):496-507
62. Smith BR, Boyle AE, Amit Z (1999) The effects of the GABAB agonist baclofen on the temporal and structural characteristics of ethanol intake. Alcohol 17(3):231-240
63. Smith BR, Robidoux J, Amit Z (1992) GABAergic involvement in the acquisition of voluntary ethanol intake in laboratory rats. Alcohol and Alcoholism 27(3):227-231
64. Swift R, Oslin DW, Alexander M, Forman R (2011) Adherence monitoring in naltrexone pharmacotherapy trials: a systematic review. Journal of Studies on Alcohol and Drugs 72(6):1012
65. Tanchuck MA, Yoneyama N, Ford MM, Fretwell AM, Finn DA (2011) Assessment of GABA-B, metabotropic glutamate, and opioid receptor involvement in an animal model of binge drinking. Alcohol 45(1):33-44
66. B receptor positive allosteric modulators for the treatment of pain. ACS Medicinal Chemistry Letters (submitted).
67. Urwyler S (2011) Allosteric modulation of family C G-protein-coupled receptors: from molecular insights to therapeutic perspectives. Pharmacol Rev 63(1):59-126
68. Villas Boas GR, Zamboni CG, Peretti MC, Correia D, Rueda AVL, Camarini R, Brunialti-Godard AL, Boerngen-Lacerda R (2012) GABAB receptor agonist only reduces ethanol drinking in light-drinking mice. Pharmacol Biochem Behav 102(2):233-240
69. Vlachou S, Guery S, Froestl W, Bannerjee D, Benedict J, Finn MG, Markou A (2011) Repeated administration of the GABAB receptor positive modulator BHF177 decreased nicotine self-administration, and acute administration decreased cue-induced reinstatement of nicotine seeking in rats. Psychopharmacology 215(1):117-128
70. Volpicelli JR, Alterman AI, Hayashida M, O'Brien CP (1992) Naltrexone in the treatment of alcohol dependence. Arch Gen Psychiatry 49(11):876
71. Walker BM, Koob GF (2007) The γ-aminobutryric acid-B receptor agonist baclofen attenuates responding for ethanol in ethanol-dependent rats. Alcohol Clin Exp Res 31(1):11-18
72. Weiss RD (2004) Adherence to pharmacology in patients with alcohol and opioid dependence. Addiction 99(11):1382-1392
73. Xi ZX, Stein EA (1999) Baclofen inhibits heroin self-administration behavior and mesolimbic dopamine release. J Pharmacol Exp Ther 290(3):1369-1374
74. Yoneyama N, Crabbe JC, Ford MM, Murillo A, Finn DA (2008) Voluntary ethanol consumption in 22 inbred mouse strains. Alcohol 42(3):149-160