Acetylcholinesterase and cholinergic receptors (AChE; AChR)

Acetylcholinesterase is a serine hydrolase enzyme critical for terminating cholinergic signaling by hydrolyzing acetylcholine in synaptic clefts. It is present in neural, muscle, and some blood cell membranes, ensuring precise control of muscle contraction and neuronal communication. Acetylcholine receptors, or cholinergic receptors, are integral membrane proteins activated by acetylcholine. They are divided into two classes: nicotinic receptors (ligand-gated ion channels), mediating fast synaptic transmission at neuromuscular junctions and autonomic ganglia, and muscarinic receptors (GPCRs), modulating effects of acetylcholine in smooth muscle, cardiac tissue, glands, and the CNS. Both acetylcholinesterase and cholinergic receptors are prominent drug targets for neurological, muscular, and autonomic disorders.

Other names

cholinesteraseAChEAChRcholinergic receptornicotinic receptor (nAChR)muscarinic receptor (mAChR)

Acetylcholinesterase inhibitors: Block enzymatic degradation of acetylcholine, leading to increased synaptic acetylcholine and prolonged receptor activation. Cholinergic receptor agonists: Directly activate nicotinic or muscarinic receptors, mimicking acetylcholine effects. Cholinergic receptor antagonists: Block receptor activation, inhibiting acetylcholine effects. Partial agonists: Activate receptor sub-maximally (e.g., varenicline at nAChRs).