Abstract
Alcohol and drug dependence are serious public health problems worldwide. The prevalence of alcohol and drug dependence in the United States and other parts of the world is significant. Given the limitations in the efficacy of current pharmacotherapies to treat these disorders, research in developing alternative pharmacotherapies continues. Preclinical and clinical evidence thus far has indicated that brain nicotinic acetylcholine receptors (nAChRs) are important pharmacological targets for the development of medications to treat alcohol and drug dependence. The nAChRs are a super family of ligand gated ion channels, and are expressed throughout the brain with twelve neuronal nAChR subunits (α2–α10 and β2–β4) identified. Here, we review preclinical and clinical evidence involving a number of nAChR ligands that target different nAChR subtypes in alcohol and nicotine addiction. The important ligands include cytisine, lobeline, mecamylamine, varenicline, sazetidine A and others that target α4β2* nAChR subtypes as small molecule modulators of the brain nicotinic cholinergic system are also discussed. Taken together, both preclinical and clinical data exist that support nAChR–based ligands as promising therapeutic agents for the treatment of alcohol and drug dependence.
Highlights
The current review aims to cover the currently available pharmacological and therapeutic approaches involving nicotinic acetylcholine receptors relevant to alcohol and drug dependence
Significant progress has been made in determining the role that the nicotinic cholinergic system plays in alcohol and drug dependence through both preclinical and clinical studies
Recent studies support the clinical management of alcohol dependence with varenicline and other nicotinic acetylcholine receptors (nAChRs) partial agonists and/or antagonists, such as mecamylamine, especially among heavy smokers
Summary
Preclinical and clinical evidence far has indicated that brain nicotinic acetylcholine receptors (nAChRs) are important pharmacological targets for the development of medications to treat alcohol and drug dependence. Additional nAChR ligands such as cytisine, a partial agonist at α4β2∗ and lobeline, a non-selective antagonist were found to reduce alcohol consumption and nicotine-induced alcohol drinking (Bell et al, 2009; Hendrickson et al, 2009; Chatterjee et al, 2011; Sajja and Rahman, 2011, 2012, 2013a).
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