The potent behavioral and cognitive effects of nicotine highlight the physiological importance of nicotinic acetylcholine receptors (nAChRs). These receptors are part of the superfamily of neurotransmitter-gated ion channels that are responsible for rapid intercellular communication. Molecular cloning of the protein subunits that make up these receptors has led to greater understanding of the pharmacology and physiology of nAChRs. This review outlines our current understanding of the molecular constituents of these receptors and some of the recent studies of the structural determinants of receptors function.