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Muscarinic acetylcholine receptors M1 and M2 are subtypes of G protein-coupled receptors that bind acetylcholine and transmit signals predominantly in the parasympathetic nervous system for a wide range of physiological responses. M1 receptors are primarily expressed in the central nervous system and mediate cognitive and memory functions, while M2 receptors are mainly found in the heart, where they control heart rate and contractility. Clinically, they are targets for drugs addressing neurological disorders, cardiac arrhythmias, and various autonomic dysfunctions. Agonists and antagonists targeting these receptors are widely used therapeutically, but careful management of side effects and selectivity is necessary due to their broad expression and critical roles in homeostasis[1][2][5][7].
Agonists: Mimic acetylcholine to activate muscarinic receptors, leading to parasympathetic effects (e.g., smooth muscle contraction, increased gland secretion, slowing heart rate, CNS modulation)[2][4] Antagonists: Competitively inhibit acetylcholine binding and block muscarinic signaling, thereby reducing parasympathetic tone (e.g., increased heart rate, reduced smooth muscle contraction, reduced glandular secretions)[5]
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