Cholinergic receptor system as a target for treating alcohol abuse and dependence

Recent Patents on CNS Drug Discovery

Volumn 7, Issue 2, 2012, Pages 145-150

  Rahman, Shafiqur ^a   Prendergast, Mark A ^b  

^a Avera Health   (United States)

^b UNIVERSITY OF KENTUCKY   (United States)

Author keywords

Alcohol dependence; Drug addiction; Drug development; Nicotinic receptors; Pharmacotherapy; Translational research

Indexed keywords

CP 601932; CYTISINE; LOBELINE; MECAMYLAMINE; PF 4575180; PLACEBO; SAZETIDINE A; UNCLASSIFIED DRUG; VARENICLINE;

ALCOHOL ABUSE; ALCOHOL CONSUMPTION; ALCOHOLISM; CHOLINERGIC SYSTEM; DRINKING BEHAVIOR; DRUG DEPENDENCE TREATMENT; DRUG EFFICACY; DRUG MECHANISM; DRUG RECEPTOR BINDING; HUMAN; MESOLIMBIC DOPAMINERGIC SYSTEM; NONHUMAN; PRIORITY JOURNAL; REVIEW; SMOKING CESSATION;

EID: 84861757581     PISSN: 15748898     EISSN: None     Source Type: Journal    
DOI: 10.2174/157488912800673173     Document Type: Review

References (103)

1. World Health Organization. Alcohol and Injuries: Emergency department Studies in an International Perspective. Author 2009.
2. World Health Organization. Global Status report on Alcohol and Drugs of abuse. Author 2004.
3. Niccols A. Fetal alcohol syndrome and the developing socioemotional brain. Brain Cognition 2007; 65: 135-42.
4. National Institute on Alcohol Abuse and Alcoholism. Five year strategic plan FY07-11: Alcohol across the lifespan. Washington, DC: Department of Health and Human Services. 2007.
5. Koob GF, Volkow ND. Neurocircuitry of addiction. Neuropsychopharmacol 2010; 35: 217-38.
6. Lê AD, Corrigall WA, Harding JW, Juzytsch W, Li TK. Involvement of nicotinic receptors in alcohol self-administration. Alcohol Clin Exp Res 2000; 24: 155-63.
7. Narahashi T, Aistrup GL, Marszalec W, Nagata K. Neuronal acetylcholine nicotinic receptors: a new target site of ethanol. Neurochem Int 1999; 35: 131-41.
8. Soderpalm B, Ericson M, Olausson P, Blomqvist O, Engel, JA. Nicotinic mechanisms involved in the dopamine activating and reinforcing properties of ethanol. Behav Brain Res 2000; 113: 85-96.
9. Tizabi Y, Copeland Jr RL, Louis VA, Taylor RE. Effects of combined systemic alcohol and central nicotine administration into ventral tegmental area on dopamine release in the nucleus accumbens. Alcohol Clin Exp Res 2002; 26: 394-9.
10. Larsson A, Svensson L, Söderpalm B, Engel JA. Role of different nicotinic acetylcholine receptors in mediating behavioral and neurochemical effects of ethanol in mice. Alcohol 2002; 28: 157-67.
11. Steensland P, Simms JA, Holgate J, Richards JK, Bartlett SE. Varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, selectively decreases ethanol consumption and seeking. Proc Natl Acad Sci USA 2007; 104: 12518-23.
12. Ericson M, Löf E, Stomberg R, Söderpalm B. The smoking cessation medication varenicline attenuates alcohol and nicotine interactions in the rat mesolimbic dopamine system. J Pharmacol Exp Ther 2009; 329: 225-30.
13. Kamens HM, Anderson J, Picciotto MR. Modulation of ethanol consumption by genetic and pharmacological manipulation of nico tinic acetylcholine receptors in mice. Psychopharmacol 2010; 208: 613-26.
14. Le Novere N, Zoli M, Changeux JP. Neuronal nicotinic receptor alpha 6 subunit mRNA is selectively concentrated in catecholaminergic nuclei of the rat brain. Eur J Neurosci 1996; 8: 2428-39.
15. Gotti C, Moretti M, Gaimarri A, Zanardi A, Clementi F, Zoli M. Heterogeneity and complexity of native brain nicotinic receptors. Biochem Pharmacol 2007; 74: 1102-11.
16. Millar NS, Gotti C. Diversity of vertebrate nicotinic acytylcholine receptors. Neuropharmacol 2009; 56: 237-46.
17. Livingstone PD, Wonnacott S. Nicotinic acetylcholine receptors and the ascending dopamine pathways. Biochem Pharmacol 2009; 78: 744-55.
18. Picciotto MR, Addy NA, Mineur YS, Brunzell DH. It is not "either/or": activation and desensitization of nicotinic acetylcholine receptors both contribute to behaviors related to nicotine addiction and mood. Prog Neurobiol 2008; 84: 329-42.
19. Fowler CD, Arends MA, Kenny PJ. Subtypes of nicotinic acetylcholine receptors in nicotine reward, dependence, and withdrawal: evidence from genetically modified mice. Behav Pharmacol 2008; 19: 461-84.
20. Rahman S, Lopez-Hernandez G, Corrigall WA, Papke RL. Neuronal nicotinic receptors as brain targets for the pharmacotherapy of drug addiction. CNS Neurol Disord Drug Targets 2008; 7: 422-41.
21. Chatterjee S, Bartlett SE. Neuronal nicotinic acetylcholine receptors as pharmacotherapeutic targets for the treatment of alcohol use disorders. CNS Neurol Disord Drug Targets 2010; 9: 60-76.
22. Kuzmin A, Jerlhag E, Liljequist S, Engel JA. Effects of subunit selective nAChR receptors on operant ethanol self-administration and relapse-like ethanol-drinking behavior. Psychopharmacol 2009; 203: 99-108.
23. Hendrickson LM, Zhao-Shea R, Pang X, Gardner PD, Tapper AR. Activation of alpha4* nAChRs is necessary and sufficient for varenicline-induced reduction of alcohol consumption. J Neurosci 2010; 30: 10169-76.
24. Buisson B, Bertrand D. Nicotine addiction: the possible role of functional upregulation. Trends Pharmacol Sci 2002; 23:130-36.
25. López-Hernández GY, Sánchez-Padilla J, Ortiz-Acevedo A, Lizardi-Ortiz J, Salas-Vincenty Rojas LV, Lasalde-Dominicci JA. Nicotine-induced up-regulation and desensitization of alpha4beta2 neuronal nicotinic receptors depend on subunit ratio. J Biol Chem 2004; 279: 38007-15.
26. Lindstrom JM. Nicotinic acetylcholine receptors of muscles and nerves: comparison of their structures, functional roles, and vulnerability to pathology. Ann N Y Acad Sci 2003; 998: 41-52.
27. Gotti C, Clementi F. 2004 Neuronal nicotinic receptors: from structure to pathology. Prog Neurobiol 2004; 74: 363-96.
28. McBride WJ, Li TK. Animal models of alcoholism: neurobiology of high alcohol-drinking behavior in rodents. Crit Rev Neurobiol 1998; 12: 339-69.
29. Tizabi Y, Bai L, Copeland RL Jr, Taylor RE. Combined effects of systemic alcohol and nicotine on dopamine release in the nucleus accumbens shell. Alcohol Alcohol 2007; 42: 413-6.
30. Larsson A, Engel, JA. Neurochemical and behavioral studies on ethanol and nicotine interactions. Neurosci Biobehav Rev 2004; 27: 713-20.
31. Schlaepfer IR, Hoft NR, Ehringer MA. The genetic components of alcohol and nicotine co-addiction: from genes to behavior. Curr Drug Abuse Rev 2008; 1: 124-34.
32. Crunelle CL, Miller ML, Booji J, Van den Brink W. The nicotinic acetylcholen receptor partial agonist varencline and the treatment of drug dependence: a review. Eur Neuropsychopahrmacol 2010; 20: 69-79.
33. Blomqvist O, Ericson M, Johnson DH, Engel JA, Söderpalm B. Voluntary ethanol intake in the rat: effects of nicotinic acetylcholine receptor blockade or subchronic nicotine treatment. Eur J Pharmacol 1996; 314: 257-67.
34. Ericson M, Blomqvist O, Engel JA, Söderpalm B. Voluntary ethanol intake in the rat and the associated accumbal dopamine overflow are blocked by ventral tegmental mecamylamine. Eur J Pharmacol 1998; 358: 189-96.
35. McKee SA, Harrison EL, O'Malley SS, Krishnan-Sarin S, Shi J, Tetrault JM, et al. Varenicline reduces alcohol self-administration in heavy-drinking smokers. Biol Psychiatry 2009; 66:185-90.
36. Hendrickson LM, Zhao-Shea R, Tapper AR. Modulation of ethanol drinking-in-the-dark by mecamylamine and nicotinic acetylcholine receptor agonists in C57BL/6J mice. Psychopharmacol 2009; 204: 563-72.
37. Sajja RK, Dwivedi C, Rahman S. Nicotinic ligands modulate ethanol-induced dopamine function in mice. Pharmacol 2010; 86: 168-73.
38. Farook JM, Lewis B, Gaddis JG, Littleton JM, Barron S. Lobeline, a nicotinic partial agonist attenuates alcohol consumption and preference in male C57BL/6J mice. Physiol Behav 2009; 97: 503-6.
39. Bell RL, Eiler BJ, Cook JB, Rahman S. Nicotinic receptor ligands reduce ethanol intake by high alcohol-drinking HAD-2 rats. Alcohol 2009; 43: 581-92.
40. Aistrup GL, Marszalec W, Narahashi T. Ethanol modulation of nicotinic acetylcholine receptor currents in cultured cortical neurons. Mol Pharmacol 1999; 55: 39-49.
41. Blomqvist O, Engel JA, Nissbrandt H, Soderpalm B. The mesolimbic dopamine-activating properties of ethanol are antagonized by mecamylamine. Eur J Pharmacol 1993; 249: 207-13.
42. Blomqvist O, Hernandez-Avila CA, Van Kirk J, Rose JE, Kranzler HR. Mecamylamine modifies the pharmacokinetics and reinforcing effects of alcohol. Alcohol Clin Exp Res 2002; 26: 326-31.
43. Chi H, de Wit H. Mecamylamine attenuates the subjective stimulant-like effects of alcohol in social drinkers. Alcohol Clin Exp Res 2003; 27: 780-6.
44. Gulick D, Gould TJ. Varenicline ameliorates ethanol-induced deficits in learning in C57BL/6 mice. Neurobiol Learn Mem 2008; 90: 230-6.
45. Shytle RD, Penny E, Silver AA, Goldman J, Sanberg PR. Mecamylamine (Inversine): an old antihypertensive with new research directions. J Hum Hyperten 2002; 16: 453-7.
46. Young EM, Mahler S, Chi H, de Wit H. Mecamylamine and ethanol preference in healthy volunteers. Alcohol Clin Exp Res 2005; 29: 58-65.
47. Marks JL, Hill EM, Pomerleau CS, Mudd SA, Blow FC. Nicotine dependence and withdrawal in alcoholic and nonalcoholic eversmokers. J Subst Abuse Treat 1997; 14: 521-7.
48. Reich MS, Dietrich MS, Finlayson AJ, Fischer EF, Martin PR. Coffee and cigarette consumption and perceived effects in recovering alcoholics participating in Alcoholics Anonymous in Nashville, Tennessee, USA Alcohol Clin Exp Res 2008; 32: 1799-806.
49. Mihalak KB, Carroll FI, Luetje CW. Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. Mol Pharmacol 2006; 70: 801-5.
50. Parker MJ, Beck A, Luetje CW. Neuronal nicotinic receptor 2 and 4 subunits confer large differences in agonist binding affinity. Mol Pharmacol 1998; 54: 1132-9.
51. Xiao Y, Baydyuk M, Wang HP, Davis HE, Kellar KJ. Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells. Bioorg Med Chem Lett 2004; 14: 1845-8.
52. Chavez-Noriega LE, Gillespie A, Stauderman KA, Crona JH, Claeps BO, Elliott KJ, et al. Characterization of the recombinant human neuronal nicotinic acetylcholine receptors alpha3beta2 and alpha4beta2 stably expressed in HEK293 cells. Neuropharmacology 2000; 39: 2543-60.
53. Slater YE, Houlihan LM, Maskell PD, Exley R, Bermudez I, Lukas RJ, et al. Halogenated cytisine derivatives as agonists at human neuronal nicotinic acetylcholine receptor subtypes. Neuropharmacol 2003; 44: 503-15.
54. Carbonnelle E, Sparatore F, Canu-Boido C, Salvagno C, Baldani-Guerra B, Terstappen G, et al. Nitrogen substitution modifies the activity of cytisine on neuronal nicotinic receptor subtypes. Eur J Pharmacol 2003; 471: 85-96.
55. Papke RL, Porter-Papke JK. Comparative pharmacology of rat and human alpha7 nAChR conducted with net charge analysis. Br J Pharmacol 2002; 137: 49-61.
56. Tutka P, Zatoski W. Cytisine for the treatment of nicotine addiction: from a molecule to therapeutic efficacy. Pharmacol Rep 2006; 53: 777-98.
57. Coe JW, Brooks PR, Vetelino MG, Wirtz MC, Arnold EP, Huang J, et al. Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation. J Med Chem 2005; 48: 3474-77.
58. Sajja RK, Rahman S. Lobeline and cytisine reduce voluntary ethanol drinking behavior in male C57BL/6J mice. Prog Neuropsychopharmacol Biol Psychiatry 2011; 35: 257-64.
59. Damaj MI, Patrick GS, Creasy KR, Martin BR. Pharmacology of lobeline, a nicotinic receptor ligand. J Pharmacol Exp Ther 1997; 282: 410-9.
60. Dwoskin LP, Crooks PA. A novel mechanism of action and potential use for lobeline as a treatment for psychostimulant abuse. Biochem Pharmacol 2002; 63: 89-98.
61. 3H] dopamine uptake. J Pharmacol Exp Ther 1997; 280: 1432-44.
62. Wilhelm CJ, Johnson RA, Lysko PG, Eshleman AJ, Janowsky A. Effects of methamphetamine and lobeline on vesicular monoamine and dopamine transporter-mediated dopamine release in a cotransfected model system. J Pharmacol Exp Ther 2004; 310: 1142-51.
63. Miller DK, Crooks PA, Teng L, Witkin JM, Munzar P, Goldberg SR, et al. Lobeline inhibits the neurochemical and behavioral effects of amphetamine. J Pharmacol Exp Ther 2001; 296: 1023-34.
64. Harrod SB, Dwoskin LP, Crooks PA, Klebaur JE, Bardo MT. Lobeline attenuates d-methamphetamine self-administration in rats. J Pharmacol Exp Ther 2001; 298: 172-79.
65. Miller DK, Lever JR, Rodvelt KR, Baskett JA, Will MJ, Kracke GR. Lobeline, a potential pharmacotherapy for drug addiction, binds to mu opioid receptors and diminishes the effects of opioid receptor agonists. Drug Alcohol Depend 2007; 89: 282-91.
66. Xiao Y, Fan H, Musachio JL, Wei ZL, Chellappan SK, Kozikowski AP, et al. Sazetidine-A, a novel ligand that desensitizes alpha4beta2 nicotinic acetylcholine receptors without activating them. Mol Pharmacol 2006; 70: 1454-60.
67. Levin ED, Rezvani AH, Xiao Y, Slade S, Cauley M, Wells C, et al. Sazetidine-A, a selective alpha4beta2 nicotinic receptor desensitizing agent and partial agonist, reduces nicotine self-administration in rats. J Pharmacol Exp Ther 2010; 332: 933-9.
68. Rezvani AH, Slade S, Wells C, Petro A, Lumeng L, Li TK, et al. Effects of sazetidine-A, a selective alpha4beta2 nicotinic acetylcholine receptor desensitizing agent on alcohol and nicotine selfadministration in selectively bred alcohol-preferring (P) rats. Psychopharmacol 2010; 211: 161-74.
69. Chatterjee S, Steensland P, Simms JA, Holgate J, Coe JW, Hurst RS, et al. Partial agonists of the alpha3beta4 neuronal nicotinic acetylcholine receptor reduce ethanol consumption and seeking in rats. Neuropsychopharmacol 2011; 36: 603-15.
70. Kozikowski, A.P., Musachio, J.L., Kellar, K.J., Xiao, Y., Wei, Z.-L. Ligands for nicotinic acetylcholine receptors, and methods of making and using them. WO2005000806 (2005).
71. Kozikowski, A.P., Musachio, J.L., Kellar, K.J., Xiao, Y., Wei, Z.-L., Fan, H. Ligands for nicotinic acetylcholine receptors, and methods of making and using them. US8030300 (2011).
72. Wu, J. Method for decreasing nicotine and other substance use in humans. US7341745 (2008).
73. Peters, D., Olsen, G.M., Nielsen, S.F., Nielsen, E. Ø. Azaring-ether derivatives and their use as nicotinic ACh receptor modulators. US6756386 (2004).
74. Mazurov, A.A., Klucik, J., Miao, L., Seamans, A.S., Phillips, T.Y., Schmitt, J.D., Miller, C.H. 3-substituted-2-(arylalkyl)-1-azabicycloalkanes and methods of use thereof. US8084462 (2011).
75. Nielson, S.F., Peters, D., Nielsen, E.O., Olsen, G.M. Heteroaryl diazacycloalkanes, their preparation and use. US7064118 (2001).
76. Peters, D., Olsen, G.M., Nielsen, S.F., Nielsen, E. Ø. Certain heteroaryl diazacycloalkanes as cholinergic ligands at nicotinic acetylcholine receptors. US6825189 (2004).
77. Peters, D., Olsen, G.M., Nielsen, S.F., Nielsen, E. Ø. Heteroaryl diazacycloalkanes, their preparation and use. US6897219 (2005).
78. Schrimpf, M.R., Tietje, K.R., Toupence, R.B., Ji, J., Basha, A., Bunnelle, W.H., Daanen, J.F., Frost, J.M., Sippy, K.B. Diazabicyclic central nervous system active agents. US7598236 (2009).
79. Xie, W., Herbert, B., Ma, J., Nguyen, T.M., Schumacher, R., Gauss, C.M., Tehim, A. Indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, and preparation and uses thereof. US7790722 (2010).
80. Asmussen, B., Hille, T., Hoffmann, H.-R., Opitz, K. Pharmaceutical composition containing desoxypeganine for the treatment of alcoholism. WO0048600 (2000).
81. Asmussen, B., Hille, T., Hoffmann, H.-R., Opitz, K. Pharmaceutical composition containing desoxypeganine for the treatment of alcoholism. US6627631 (2003).
82. Asmussen, B., Hille, T., Hoffmann, H.-R., Opitz, K. Pharmaceutical composition containing desoxypeganine for the treatment of alcoholism. EP1154776 (2005).
83. Patent Holder. Pharmaceutical composition containing desoxypeganine for the treatment of alcoholism. KR648767 (2006).
84. Madhat, M.N. Buccal and sublingual administration of physostigmine. US6264974 (2001).
85. Levay, G., Gacsalyi, I., Harsing, L.G., Simig, G. Combined pharmaceutical composition for the inhibition of the decline of cognitive functions. WO2005087212 (2005).
86. Buccafusco, J.J., Terry, A.V., Beach, J.W., Jonnala, R.R. Analogs of choline for neuroprotection and cognitive enhancement in neurogenerative disorders. US6881738 (2005).
87. Dey, D., Singh, G., Neogi, P., Ramachandran, U., Santhanagopalan, C. MAO A inhibitors with a diphenyl ether-substructure. WO2009030968 (2009).
88. Hilke, W. Combination of desoxypeganine and mecamylamine for the treatment of alcohol abuse. MX011249 (2005).
89. Hilke, W., Joachim, M., Klaus, O. Combination of desoxypeganine and mecamylamine for the treatment of alcohol abuse. KR006946 (2006).
90. Hilke, W., Joachim, M., Klaus, O. Combination of desoxypeganine and mecamylamine for the treatment of alcohol abuse. ZA0507213 (2006).
91. Mucke, H., Opitz, K., Moormann, J. Active ingredient combination for treating a dependence on addictive substances or narcotics using medicaments. CA2450787 (2002).
92. Opitz, K. Active ingredient combination for treating a dependence on addictive substances or narcotics using medicaments. MX011825 (2005).
93. Patent Holder. Combination of desoxypeganine and mecamylamine for the treatment of alcohol abuse. CA2523331 (2004).
94. Patent Holder. Combination of galantamine or desoxypeganine and substance with anti-excitatory action, use of composition (variants) for treating dependence on addictive substances or narcotics. UA0076753 (2004).
95. Winterhoff, H., Moormann, J., Opitz, K. Combination of desoxypeganine and mecamylamine for the treatment of alcohol abuse. WO2004096200 (2004).
96. Propes, M.J. Composition and method for treating alcoholism and other substance addictions. WO2008045641 (2008).
97. Propes, M.J. Composition and method for treating alcoholism and other substance addictions. US0005367 (2009).
98. Moormann, J., Mucke, H., Opitz, K. Active ingredient combination of e.g., galanthamine or deoxypeganine and e.g., acamprosate or memantine for treating an addiction such as alcoholism. WO2003102388 (2003).
99. Moormann, J., Mucke, H., Opitz, K. Active ingredient combination for treating an addiction such as alcoholism. SK0301565 (2004).
100. Moormann, J., Mucke, H., Opitz, K. Active ingredient combination of (e.g. galanthamine or desoxypeganine with acamprosate or memantine) for treating narcotic or alcohol addiction. NZ0529944 (2007).
101. Moormann, J., Mucke, H., Opitz, K. Active ingredient combination for treating a dependence on addictive substances or narcotics using medicaments. CZ0299951 (2009).
102. Moormann, J., Mucke, H., Opitz, K. Active ingredient combination for treating a dependence on addictive substances or narcotics using medicaments. SK0287180 (2010).
103. Opitz, K., Moormann, J., Mucke, H. Active ingredient combination of e.g., galanthamine or deoxypeganine and e.g., acamprosate or memantine for treating an addiction such as alcoholism. AU2323873 (2006).