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The nicotinic acetylcholine receptor α7 subtype is a homopentameric, ligand-gated ion channel embedded in neuronal and immune cell membranes, composed entirely of α7 subunits. When activated by endogenous acetylcholine or exogenous agonists like nicotine, it opens to allow influx of cations—particularly Ca^2+—rapidly altering cell excitability and downstream signaling. This receptor plays major roles in cognition, neuroprotection, cholinergic modulation of inflammation, and is implicated in memory, learning, and several disease processes including neurodegeneration, schizophrenia, inflammation, cardiovascular disease, and cancer. Its pharmacological targeting has therapeutic relevance but is confounded by issues of rapid desensitization and cell-specific effects.
Agonists: Bind to the receptor, causing channel opening and allowing Ca^2+ (and other cations) to flow in, leading to neuronal excitation or immune modulation. Antagonists: Occupy the ligand binding site, preventing activation and channel opening. Positive allosteric modulators: Enhance the receptor response to agonists, increasing channel open probability or conductance.
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