Target intelligence / Profile preview

Neuronal Acetylcholine Receptor Subunit Alpha (nAChR alpha subunit)

Target
nAChR alpha subunit
Molecular classification
Ligand-gated ion channel, Receptor, Neuronal receptor, Acetylcholine receptor
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Overview

Neuronal acetylcholine receptor (nAChR) subunit alpha refers to a family of protein subunits that form part of the nicotinic acetylcholine receptors in the nervous system. These receptors are ligand-gated ion channels activated by the neurotransmitter acetylcholine and are crucial for fast synaptic transmission in both central and peripheral nervous systems. There are ten known neuronal alpha subunits in mammals, named α2 through α10 (α1 is primarily found in muscle-type nAChRs). Each nAChR is a pentamer composed of five subunits, which can be either homomeric (all identical, e.g., α7) or heteromeric (combinations of different alpha and beta subunits). Upon binding acetylcholine, these receptors undergo conformational changes that open an ion channel permeable to cations such as Na(+), K(+), and Ca(2+). This leads to depolarization of neurons or muscle cells, facilitating neurotransmission. Different combinations of alpha subunits confer distinct pharmacological properties and physiological roles. Alterations or mutations in genes encoding neuronal nAChR alpha subunits have been linked with neurodegenerative diseases, cognitive deficits, and attention-deficit/hyperactivity disorder (ADHD). Pharmacological targeting of specific nAChR alpha-containing complexes is being explored for therapeutic interventions against these conditions.

Other names
Neuronal Nicotinic Acetylcholine Receptor Alpha SubunitnAChR alphaCHRNA (various subtypes, e.g., CHRNA4, CHRNA5, CHRNA7)
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Mechanism of action

Agonist or antagonist binding to the receptor, leading to ion channel opening or blockade, respectively.

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Biological functions

NeurotransmissionSynaptic transmissionIon channel activityNeuromodulationRegulation of neuronal excitabilityCognitive function (attention, learning, memory)Signal transduction
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Disease associations

Neurodegenerative diseasesCognitive deficitsAttention-deficit/hyperactivity disorder (ADHD)Nicotine addictionInflammationPain
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Safety considerations

Potential for seizuresCardiovascular effectsNeuropsychiatric effectsAddiction (for nicotine)Off-target effects due to subunit promiscuity
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Interacting drugs

Acetylcholine

5 more in the full profile.

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