Muscarinic acetylcholine receptors mediate diverse central and peripheral physiological functions. At present, five receptor subtypes (M1 to M5) have been identified. Recent gene targeting approaches have unravelled the specific function of these muscarinic receptor subtypes. Based on these findings, muscarinic receptors have been emerging as an important therapeutic target for various diseases, including dry mouth, incontinence (overactive bladder) and chronic obstructive pulmonary disease. Activation of the M1 subtype muscarinic receptor is thought to have the most potential for improving cognitive processing due to the predominance of M1 receptors in areas of the brain involved in cognition and memory. Selective M1 agonists, therefore, could be useful in treatment of schizophrenia and Alzheimer’s disease. Muscarinic receptor antagonists are widely used for treatment of urinary incontinence, but older agents suffer from anticholinergic side effects at muscarinic receptors distant from the target organ. Newer developments are targeting selectively the M3 muscarinic receptor to improve tolerability. While muscarinic receptor antagonists with selectivity for the M3 receptor subtype were shown to be well tolerated, further improvement can be achieved with long-acting M3 antagonists for once-daily inhalation in combination with long-acting beta2 agonists (LABA).

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