Drug addiction is a chronic neuropsychiatric disorder which is characterized by a compulsion to take drugs and
loss of control in limiting intake. The worldwide impact of drug addiction on morbidity and mortality is very high.
Evidence from preclinical and clinical studies suggests that brain nicotinic acetylcholine receptors (nAChRs), play a
critical role in various addictive disorders, including nicotine addiction and alcoholism. Thus, there is an increasing
impetus in developing new therapeutics for addictive disorders by targeting brain nAChRs. This review highlights the
important preclinical findings involving nAChR ligands in regulating nicotine, alcohol and other addictive drug-induced
neurobiological changes in animal models and humans. A number of partial agonists or antagonists targeting nAChRs
have shown therapeutic benefit in nicotine addiction and alcohol use disorders are also discussed. Furthermore, the role of
nAChRs in other addictive disorders is reviewed. Overall, novel pharmacological agents that target brain nAChRs for
future drug development are discussed.
Keywords: Drug addiction, nicotinic receptors, nicotine addiction, alcoholism, cocaine, opioids, pharmacotherapy, drug
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