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Neuronal acetylcholine receptor subunit alpha-7 is a homopentameric ligand-gated ion channel, part of the Cys-loop receptor family. It is highly expressed in the central nervous system and some peripheral tissues, where it mediates fast synaptic cholinergic transmission, is highly permeable to calcium ions, and regulates neuronal excitability, synaptic plasticity, inflammation, and cell proliferation. CHRNA7 plays key roles in cognition and is involved in pathologies such as Alzheimer’s disease, schizophrenia, cancer, and sepsis. Its pharmacology features rapid desensitization and unique gating properties, and it is targeted by drugs such as nicotine, Varenicline, epibatidine, α-bungarotoxin, and positive allosteric modulators. The α7 subtype is distinguished by singular calcium permeability and is a focus for therapeutic intervention in neurodegenerative, cardiovascular, and inflammatory diseases.
Agonists activate the receptor to facilitate cation (mainly Ca^2+) flow, increase synaptic transmission, and modulate inflammatory response. Antagonists block ion channel gating. Positive allosteric modulators enhance receptor activation and channel conductance.
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