An understanding of muscarinic receptors is tantamount to an understanding of overactive bladder. The M(3) muscarinic receptor subtype is responsible for detrusor smooth muscle contraction and it exerts an exocrine function in the salivary glands. Alterations in the receptor's response to acetylcholine as a result of injury may lead to hypersensitivity and overactivity. The M(2) receptor subtype, which is mainly responsible for cardiac function, is the muscarinic receptor of highest proportion in the detrusor. M(2) also may play a role in detrusor contraction in injury and pathologic states. Muscarinic antagonists are the mainstay of pharmacotherapy for overactive bladder, but those that are available are not tissue specific. Growing knowledge of the nuances of receptor-ligand behavior and interaction between muscarinic receptors subtypes may provide novel targets for future drug development, improve efficacy, and reduce bothersome side effects.