The parasympathetic system and its associated muscarinic receptors have been the subject of a renaissance of interest for the following two main reasons: (1) the association of endothelial muscarinic receptors and the nitric oxide (NO) pathway; (2) the discovery of several muscarinic receptor subtypes and drugs interacting with them. In the present survey modern insights into the subdivision of muscarinic receptors have been dealt with as the basis for a description of the muscarinic receptor agonists and antagonists thus far known. There are at least four pharmacologically defined M receptors (M1, M2, M3, M4) in primary tissues, and five muscarinic receptors have been cloned (m1, m2, m3, m4, m5). Selective agonists for M-receptor subtypes hardly exist, and all classical agonists (acetylcholine, carbachol, etc.) are clearly nonselective. A few selective antagonists for M1 (pirenzepine) and M2 receptors (AF-DX 116) have been introduced, although selective M3 receptors are hardly available. Finally, the potential therapeutic use of M-receptor agonists (myocardial ischemia, hypertension) and muscarinic antagonists (certain forms of bradycardia, coronary spasm) has been critically discussed. Although only in a preliminary stage, this development appears to be promising and at least of great fundamental interest.