SummaryIt is widely accepted that tobacco use is primarily a problem of drug dependence, with nicotine serving as the addictive agent. Nicotine itself is of some value as a therapeutic aid for people trying to give up smoking. The possible applications in this area of a different class of drug, nicotine antagonists, are reviewed. The receptor mediating the main central effects of nicotine resembles nicotinic‐cholinoceptive sites in ganglia of the autonomic nervous system; drugs which block ganglionic transmission also block the central effects of nicotine, including the positively reinforcing effect sought by smokers. Possible sub‐populations of smokers who might benefit from antagonist therapy are proposed, and the advantages and limitations of such an approach are discussed. Future prospects probably depend on the development of agents with more selective effects than those presently availa