Page last updated: 2024-10-24
acetylcholine-gated channel complex
Definition
Target type: cellularcomponent
A homo- or hetero-pentameric protein complex that forms a transmembrane channel through which ions may pass in response to acetylcholine binding. [GOC:bf, GOC:mah, PMID:12381728, PMID:15579462]
The acetylcholine-gated channel complex, also known as the nicotinic acetylcholine receptor (nAChR), is a transmembrane protein complex found at the neuromuscular junction and in the central nervous system. This complex is responsible for mediating the rapid transmission of nerve impulses across synapses. It is a pentameric structure, meaning it consists of five subunits arranged in a ring-like structure. These subunits are designated as α, β, γ, δ, and ε, with each subunit contributing to the overall structure and function of the complex.
The acetylcholine-gated channel complex is composed of four transmembrane domains (M1, M2, M3, and M4) within each subunit. The M2 domain lines the central pore of the channel, which serves as the pathway for ion conduction. The extracellular domain of the complex binds acetylcholine, initiating a conformational change that opens the channel, allowing the passage of ions across the membrane. This influx of ions, primarily sodium and calcium, depolarizes the postsynaptic membrane, triggering an action potential.
The α subunits contain the binding sites for acetylcholine, and two α subunits are required for the activation of the channel. The binding of acetylcholine to these sites triggers a conformational change that rearranges the transmembrane domains, opening the central pore. The β, γ, δ, and ε subunits play important roles in the assembly, stability, and modulation of the channel complex. They contribute to the overall structure and function of the complex and influence its sensitivity to acetylcholine and other modulators.
The acetylcholine-gated channel complex is a critical component of neuronal signaling and is involved in a wide range of physiological processes, including muscle contraction, neurotransmission, and learning and memory. Dysregulation of this complex can lead to various neurological disorders, highlighting its importance in maintaining normal brain function.
'"
Proteins (16)
| Protein | Definition | Taxonomy |
|---|---|---|
| Neuronal acetylcholine receptor subunit alpha-4 | A neuronal acetylcholine receptor subunit alpha-4 that is encoded in the genome of chicken. [PANTHER:PTHR18945:SF84, PRO:DNx] | Gallus gallus (chicken) |
| Neuronal acetylcholine receptor subunit beta-3 | A neuronal acetylcholine receptor subunit beta-3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q05901] | Homo sapiens (human) |
| Neuronal acetylcholine receptor subunit alpha-6 | A neuronal acetylcholine receptor subunit alpha-6 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q15825] | Homo sapiens (human) |
| Acetylcholine receptor subunit gamma | An acetylcholine receptor subunit gamma that is encoded in the genome of human. [PRO:DNx, UniProtKB:P07510] | Homo sapiens (human) |
| Acetylcholine receptor subunit epsilon | An acetylcholine receptor subunit epsilon that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q04844] | Homo sapiens (human) |
| Neuronal acetylcholine receptor subunit alpha-9 | A neuronal acetylcholine receptor subunit alpha-9 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9UGM1] | Homo sapiens (human) |
| Neuronal acetylcholine receptor subunit alpha-2 | A neuronal acetylcholine receptor subunit alpha-2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q15822] | Homo sapiens (human) |
| Acetylcholine receptor subunit delta | An acetylcholine receptor subunit delta that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q07001] | Homo sapiens (human) |
| Neuronal acetylcholine receptor subunit alpha-4 | A neuronal acetylcholine receptor subunit alpha-4 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P43681] | Homo sapiens (human) |
| Neuronal acetylcholine receptor subunit alpha-7 | A neuronal acetylcholine receptor subunit alpha-7 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P36544] | Homo sapiens (human) |
| Neuronal acetylcholine receptor subunit alpha-3 | A neuronal acetylcholine receptor subunit alpha-3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P32297] | Homo sapiens (human) |
| Neuronal acetylcholine receptor subunit beta-4 | A neuronal acetylcholine receptor subunit beta-4 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P30926] | Homo sapiens (human) |
| Neuronal acetylcholine receptor subunit alpha-5 | A neuronal acetylcholine receptor subunit alpha-5 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P30532] | Homo sapiens (human) |
| Neuronal acetylcholine receptor subunit beta-2 | A neuronal acetylcholine receptor subunit beta-2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P17787] | Homo sapiens (human) |
| Acetylcholine receptor subunit beta | An acetylcholine receptor subunit beta that is encoded in the genome of human. [PRO:DNx, UniProtKB:P11230] | Homo sapiens (human) |
| Acetylcholine receptor subunit alpha | An acetylcholine receptor subunit alpha that is encoded in the genome of human. [PRO:DNx, UniProtKB:P02708] | Homo sapiens (human) |
Compounds (83)
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| nornicotine | nornicotine: agricultural or horticultural insecticide; RN given refers to (+-)-isomer; structure | ||
| bupropion | bupropion : An aromatic ketone that is propiophenone carrying a tert-butylamino group at position 2 and a chloro substituent at position 3 on the phenyl ring. Bupropion: A propiophenone-derived antidepressant and antismoking agent that inhibits the uptake of DOPAMINE. | aromatic ketone; monochlorobenzenes; secondary amino compound | antidepressant; environmental contaminant; xenobiotic |
| 3-(1-methylpyrrolidin-2-yl)pyridine | 3-(1-methylpyrrolidin-2-yl)pyridine : An N-alkylpyrrolidine that consists of N-methylpyrrolidine bearing a pyridin-3-yl substituent at position 2. | N-alkylpyrrolidine; pyridine alkaloid; pyrrolidine alkaloid | |
| epibatidine | alkaloid | ||
| dimethylphenylpiperazinium iodide | piperazines | ||
| 1,3-dipropyl-8-(4-sulfophenyl)xanthine | 1,3-dipropyl-8-(4-sulfophenyl)xanthine: adenosine receptor antagonist | ||
| tacrine | tacrine : A member of the class of acridines that is 1,2,3,4-tetrahydroacridine substituted by an amino group at position 9. It is used in the treatment of Alzheimer's disease. Tacrine: A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders. | acridines; aromatic amine | EC 3.1.1.7 (acetylcholinesterase) inhibitor |
| anabasine | piperidine alkaloid; pyridine alkaloid | nicotinic acetylcholine receptor agonist; plant metabolite; teratogenic agent | |
| carbamylcholine | |||
| decamethonium | decamethonium : A quaternary ammonium ion that is a depolarising muscle relaxant whose structure comprises a decane-1,10-diamine core in which each amino group carries three methyl substituents. decamethonium: RN given refers to parent cpd | quaternary ammonium ion | muscle relaxant; nicotinic acetylcholine receptor agonist |
| donepezil | 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one : A member of the class of indanones that is 5,6-dimethoxyindan-1-one which is substituted at position 2 by an (N-benzylpiperidin-4-yl)methyl group. donepezil : A racemate comprising equimolar amounts of (R)- and (S)-donepezil. A centrally acting reversible acetylcholinesterase inhibitor, its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine. Donepezil: An indan and piperidine derivative that acts as a selective and reversible inhibitor of ACETYLCHOLINESTERASE. Donepezil is highly selective for the central nervous system and is used in the management of mild to moderate DEMENTIA in ALZHEIMER DISEASE. | aromatic ether; indanones; piperidines; racemate | EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; nootropic agent |
| granisetron | aromatic amide; indazoles | ||
| isoflurane | Isoflurane: A stable, non-explosive inhalation anesthetic, relatively free from significant side effects. | organofluorine compound | inhalation anaesthetic |
| kynurenic acid | kynurenic acid : A quinolinemonocarboxylic acid that is quinoline-2-carboxylic acid substituted by a hydroxy group at C-4. Kynurenic Acid: A broad-spectrum excitatory amino acid antagonist used as a research tool. | monohydroxyquinoline; quinolinemonocarboxylic acid | G-protein-coupled receptor agonist; human metabolite; neuroprotective agent; nicotinic antagonist; NMDA receptor antagonist; Saccharomyces cerevisiae metabolite |
| mecamylamine | Mecamylamine: A nicotinic antagonist that is well absorbed from the gastrointestinal tract and crosses the blood-brain barrier. Mecamylamine has been used as a ganglionic blocker in treating hypertension, but, like most ganglionic blockers, is more often used now as a research tool. | primary aliphatic amine | |
| n-methylcarbamylcholine | N-methylcarbamylcholine: structure given in first source | ||
| ondansetron | Ondansetron: A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties. | carbazoles | |
| sb 206553 | SB 206553: a high-affinity 5-HT(2C/2B) antagonist; structure given in first source | pyrroloindole | |
| tilorone | tilorone : A member of the class of fluoren-9-ones that is 9H-fluoren-9-one which is substituted by a 2-(diethylamino)ethoxy group at positions 2 and 7. It is an interferon inducer and a selective alpha7 nicotinic acetylcholine receptor (alpha7 nAChR) agonist. Its hydrochloride salt is used as an antiviral drug. Tilorone: An antiviral agent used as its hydrochloride. It is the first recognized synthetic, low-molecular-weight compound that is an orally active interferon inducer, and is also reported to have antineoplastic and anti-inflammatory actions. | aromatic ether; diether; fluoren-9-ones; tertiary amino compound | anti-inflammatory agent; antineoplastic agent; antiviral agent; interferon inducer; nicotinic acetylcholine receptor agonist |
| tetramethylammonium | tetramethylammonium : The simplest quaternary ammonium cation, comprising a central nitrogen linked to four methyl groups. tetramethylammonium: RN given refers to parent cpd | quaternary ammonium ion | |
| indopan | alpha-methyltryptamine : A tryptamine derivative having a methyl substituent at the alpha-position. indopan: RN given refers to parent cpd without isomeric designation | tryptamines | |
| boldine | aporphine alkaloid | ||
| cytisine | alkaloid; bridged compound; lactam; organic heterotricyclic compound; secondary amino compound | nicotinic acetylcholine receptor agonist; phytotoxin; plant metabolite | |
| anatabine | anatabine: alkaloid found in tobacco; structure | bipyridines | |
| laudanosine | laudanosine: opium alkaloid | isoquinolines | |
| 5-hydroxyindole | hydroxyindoles | human metabolite | |
| anabaseine | anabaseine: structure given in first source | bipyridines | |
| dihydro-beta-erythroidine | dihydro-beta-erythroidine : An organic heterotetracyclic compound resulting from the partial hydrogenation of the 1,3-diene moiety of beta-erythroidine to give the corresponding 2-ene. Dihydro-beta-Erythroidine: Dihydro analog of beta-erythroidine, which is isolated from the seeds and other plant parts of Erythrina sp. Leguminosae. It is an alkaloid with curarimimetic properties. | delta-lactone; organic heterotetracyclic compound; tertiary amino compound | nicotinic antagonist |
| polygodial | aldehyde | ||
| N-methyl-N-(3-pyridylmethyl)amine | aralkylamine | ||
| nicotine | (S)-nicotine : A 3-(1-methylpyrrolidin-2-yl)pyridine in which the chiral centre has S-configuration. The naturally occurring and most active enantiomer of nicotine, isolated from Nicotiana tabacum. | 3-(1-methylpyrrolidin-2-yl)pyridine | anxiolytic drug; biomarker; immunomodulator; mitogen; neurotoxin; nicotinic acetylcholine receptor agonist; peripheral nervous system drug; phytogenic insecticide; plant metabolite; psychotropic drug; teratogenic agent; xenobiotic |
| lobeline | (-)-lobeline : An optically active piperidine alkaloid having a 2-oxo-2-phenylethyl substituent at the 2-position and a 2-hydroxy-2-phenylethyl group at the 6-position. | aromatic ketone; piperidine alkaloid; tertiary amine | nicotinic acetylcholine receptor agonist |
| thiacloprid | (Z)-thiacloprid : The (Z)-stereoisomer of thiacloprid. thiacloprid : A nitrile that is cyanamide in which the hydrogens are replaced by a 1,3-thiazolidin-2-ylidene group which in turn is substituted by a (6-chloropyridin-3-yl)methyl group at the ring nitrogen. thiacloprid: structure in first source | monochloropyridine; nitrile; thiazolidines | environmental contaminant; neonicotinoid insectide; xenobiotic |
| 3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole | 3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole: structure in first source | ||
| philanthotoxin 343 | philanthotoxin 343: structure given in first source (see article's footnote); identical to philanthotoxin 433 except that the number of methylene groups between the respective amine moieties is 3,4,3 instead of 4,3,3 | N-acyl-amino acid | |
| erysodine | erysodine : An erythrina alkaloid with formula C18H21NO3 isolated from several erythrina plant species. It is a competitive antagonist of nicotinic acetylcholine receptors and exhibits antiparasitic and insecticidal activities. erysodine: structure given in first source | aromatic ether; diether; Erythrina alkaloid; organic heterotetracyclic compound; phenols | antiparasitic agent; nicotinic antagonist; phytogenic insecticide |
| varenicline | varenicline : An organic heterotetracyclic compound that acts as a partial agonist for nicotinic cholinergic receptors and is used (in the form of its tartate salt) as an aid to giving up smoking. Varenicline: A benzazepine derivative that functions as an ALPHA4-BETA2 NICOTINIC RECEPTOR partial agonist. It is used for SMOKING CESSATION. | ||
| pozanicline | |||
| prizes | (E)-acetamiprid : The (E)-stereoisomer of acetamiprid. acetamiprid : A carboxamidine that is acetamidine in which the amino hydrogens are substituted by a (6-chloropyridin-3-yl)methyl and a methyl group while the hydrogen attached to the imino nitrogen is replaced by a cyano group. acetamiprid: structure in first source | carboxamidine; monochloropyridine; nitrile | environmental contaminant; neonicotinoid insectide; xenobiotic |
| pnu 120596 | 1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)urea: an alpha7nAChR agonist; structure in first source | ureas | |
| harmicine | harmicine: structure in first source | ||
| anatoxin a | anatoxin a: found in Anabaena; was indexed to cyanobacterial toxin (MARINE TOXINS) 1978-2006; also see anatoxin-a(s) | tropane alkaloid | |
| bisabolol | Kamillosan: drug combination containing chamomile and bisabolol; used to treat dermatitis | sesquiterpenoid | |
| deformylflustrabromine | deformylflustrabromine: has antineoplastic activity; isolated from Flustra folicea; structure in first source | tryptamines | |
| tropacocaine | tropacocaine: RN given refers to (exo)-isomer; structure | ||
| isoliquiritigenin | chalcones | antineoplastic agent; biological pigment; EC 1.14.18.1 (tyrosinase) inhibitor; GABA modulator; geroprotector; metabolite; NMDA receptor antagonist | |
| tropisetron | tropisetron : An indolyl carboxylate ester obtained by formal condensation of the carboxy group of indole-3-carboxylic acid with the hydroxy group of tropine. Tropisetron: An indole derivative and 5-HT3 RECEPTOR antagonist that is used for the prevention of nausea and vomiting. | indolyl carboxylic acid | |
| lobeline | |||
| epibatidine | |||
| hmr 3647 | |||
| anatoxin a | anatoxin I: found mainly in ANABAENA; was indexed to cyanobacterial toxin (MARINE TOXINS). isolated from many salt-tolerant freshwater cyanobacteria | ||
| abt 594 | |||
| 5-(6-chloro-3-pyridinyl)-9-azabicyclo[4.2.1]non-4-ene | azepine | ||
| naringenin chalcone | 2',4,4',6'-tetrahydroxychalcone : A member of the class of chalcones that is trans-chalcone substituted by hydroxy groups at positions 2' ,4, 4', and 6' respectively. naringenin chalcone: RN given refers to cpd with unspecified stereoisomer & from CA Vol 92 Form Index; RN for cpd not in Chemline 7/6/83; structure in first source | chalcones; polyphenol | anti-allergic agent; anti-inflammatory agent; metabolite |
| trans-metanicotine | metanicotine: RN given refers to parent cpd with unspecified isomeric designation | ||
| a 85380 | A 85380: structure given in first source; A-85380 is the S-enantiomer; A-159470 is the R-enantiomer | ||
| ar-r 17779 | AR-R 17779: structure in first source | ||
| 3-(2,4-dimethoxybenzylidene)anabaseine | 3-(2,4-dimethoxybenzylidene)anabaseine: an alpha7nAChR nicotinic receptor agonist | dimethoxybenzene | |
| 2,4,2'-trihydroxychalcone | 2,4,2'-trihydroxychalcone: structure in first source | ||
| mg 624 | triethyl-(beta-4-stilbenoxyethyl)ammonium: inhibits alpha7 nicotinic receptors; structure in first source | ||
| 5-ia-85380 | aromatic ether | ||
| a 84543 | |||
| azd 0328 | spiro(1-azabicyclo(2.2.2)octane-3,2'(3H)-furo(2,3-b)pyridine): AZD-0328 is the (2'R)-isomer and D-tartrate salt; an alpha7 neuronal nicotinic receptor agonist; structure in first source | ||
| radafaxine | radafaxine: a bupropion metabolite; radafaxine is a (+)-isomer of hydroxybupropion | ||
| pnu-282987 | carbonyl compound; organohalogen compound | ||
| ssr180711 | SSR180711: a selective alpha7 acetylcholine nicotinic receptor (n-AChRs) partial agonist; structure in first source | ||
| ispronicline | ispronicline: a neuronal nicotinic acetylcholine receptor modulator; has antidepressant, neuroprotective, and cognitive effects; structure in first source | ||
| 4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | |||
| desnitroimidacloprid | desnitroimidacloprid: a nicotinic receptor agonist; structure in first source | ||
| dianicline | dianicline: an alpha4beta2 nicotinic receptor agonist; may be useful as an aid in quitting smoking; structure in first source | ||
| crispine a | crispine A: pyrrolo(2,1-a)isoquinoline alkaloid from Carduus crispus; structure in first source | ||
| pnu-282987 | |||
| amd 070 | mavorixafor: a derivative of AMD3100; a CXCR4 blocker | aminoquinoline | |
| n-methylepibatidine | N-methylepibatidine: structure in first source | ||
| sazetidine-a | sazetidine-A: a ligand that desensitizes alpha4beta2 nicotinic acetylcholine receptors without activating them; structure in first source | ||
| ns 9283 | 3-(3-(pyridine-3-yl)-1,2,4-oxadiazol-5-yl)benzonitrile: an alpha4beta2 nAChR agonist | ||
| 3-bromocytisine | 3-bromocytisine: structure in first source | ||
| a 867744 | 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide: positive modulator of alpha7 nicotinic acetylcholine receptor; structure in first source | ||
| a-582941 | A-582941: nicotinic acetylcholine receptor (alpha7 nAChR) agonist | ||
| evp-6124 | |||
| n,n-diallyl-5-methoxytryptamine | N,N-diallyl-5-methoxytryptamine: structure in first source | tryptamines | |
| imidacloprid | (E)-imidacloprid : The E-isomer of imidacloprid. | imidacloprid; imidazolidines; monochloropyridine | environmental contaminant; genotoxin; neonicotinoid insectide; nicotinic acetylcholine receptor agonist; xenobiotic |
| 3-(4-hydroxy-2-methoxybenzylidene)anabaseine |