The cholinergic hypothesis of Alzheimer's disease has spurred the development of numerous structural classes of compounds with different pharmacological profiles aimed at increasing central cholinergic neurotransmission, thus providing a symptomatic treatment for this disease. Indeed, the only drugs currently approved for the treatment of Alzheimer's disease are cholinomimetics with the pharmacological profile of acetylcholinesterase inhibitors. Recent evidence of a potential disease modifying role of acetylcholinesterase inhibitors and M(1) muscarinic agonists have led to a revival of this approach, which might be considered as more than a symptomatic treatment.