Nicotinic acetylcholine receptors (nAChRs) are a member of the “Cys-loop” receptor superfamily of ligand-gated ion channels including GABAA, glycine, as well as serotonin (5-HT3) receptors. These subunits combine to constitute various nAChR subtypes with diverse expression patterns, functional properties, and pharmacological characteristics. Since cholinergic innervation is pervasive and the nAChR expression is extremely wide, virtually all brain area is influenced by nicotinic mechanisms. nAChRs can be classified into neuronal and non-neuronal subtypes. The neuronal subtypes of these receptors, such as, the α7 and α4β2 isoforms, are involved in neurobehavioral processes that involve anxiety, nicotine-seeking behavior, the central processing of pain, food intake, and several cognitive functions like learning and memory. Neuronal nAChR dysfunction is implicated in the pathophysiology of lots of neurological disorders, and animal behavioral studies are helpful models to assess the effects of compounds that react on these receptors.
There are sixteen homologous nAChR subunits in mammalian encoded by a multigene family. Here shows the part of neuronal nAChRs in humans. nAChRs consist of five subunits arranged around a water-filled pore. Based on the adjacent cysteine (Cys) groups in the extracellular domain of only α subunits, neuronal subtypes are divided into the alpha (α2-α7, α9, and α10) and beta (β2-β4) classifications. Much of the structural and functional diversity of neuronal nAChRs derives from kinds of possible subunit combinations.
|Human Neuronal nAChR Family Members|
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