Page last updated: 2024-10-24

regulation of acetylcholine secretion, neurotransmission

Definition

Target type: biologicalprocess

Any process that modulates the frequency, rate or extent of the regulated release of acetylcholine. [GOC:ef]

Acetylcholine secretion, a fundamental process in neurotransmission, is meticulously regulated to ensure precise and efficient signaling within the nervous system. This intricate process involves a series of steps, starting with the synthesis of acetylcholine within the presynaptic neuron. Acetylcholine is synthesized from choline and acetyl-CoA by the enzyme choline acetyltransferase. Once synthesized, acetylcholine is packaged into synaptic vesicles, small membrane-bound sacs that store and release neurotransmitters. The arrival of an action potential at the presynaptic terminal triggers the opening of voltage-gated calcium channels, allowing calcium ions to influx into the presynaptic neuron. This calcium influx initiates a cascade of events that lead to the fusion of synaptic vesicles with the presynaptic membrane, releasing acetylcholine into the synaptic cleft, the narrow gap between the presynaptic and postsynaptic neurons. Acetylcholine diffuses across the synaptic cleft and binds to its receptors on the postsynaptic membrane. These receptors can be nicotinic acetylcholine receptors, ionotropic receptors that directly open ion channels upon acetylcholine binding, or muscarinic acetylcholine receptors, metabotropic receptors that initiate intracellular signaling cascades through G-protein activation. The binding of acetylcholine to its receptors elicits a postsynaptic response, which can be excitatory or inhibitory depending on the type of receptor and the downstream signaling pathways involved. To ensure precise and controlled signaling, the effects of acetylcholine are terminated rapidly by the enzyme acetylcholinesterase, which hydrolyzes acetylcholine into choline and acetate. Choline is then taken back up into the presynaptic neuron to be recycled for the synthesis of new acetylcholine, while acetate diffuses away. This continuous cycle of acetylcholine synthesis, packaging, release, binding, and breakdown ensures the rapid and efficient transmission of signals across synapses, facilitating communication within the nervous system and enabling complex brain functions.'
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Proteins (1)

ProteinDefinitionTaxonomy
Neuronal acetylcholine receptor subunit alpha-3A neuronal acetylcholine receptor subunit alpha-3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P32297]Homo sapiens (human)

Compounds (41)

CompoundDefinitionClassesRoles
bupropionbupropion : 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)pyridine3-(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
epibatidinealkaloid
dimethylphenylpiperazinium iodidepiperazines
decamethoniumdecamethonium : 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 ionmuscle relaxant;
nicotinic acetylcholine receptor agonist
granisetronaromatic amide;
indazoles
mecamylamineMecamylamine: 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
ondansetronOndansetron: 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
tiloronetilorone : 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
indopanalpha-methyltryptamine : A tryptamine derivative having a methyl substituent at the alpha-position.

indopan: RN given refers to parent cpd without isomeric designation
tryptamines
cytisinealkaloid;
bridged compound;
lactam;
organic heterotricyclic compound;
secondary amino compound
nicotinic acetylcholine receptor agonist;
phytotoxin;
plant metabolite
anabaseineanabaseine: structure given in first sourcebipyridines
polygodialaldehyde
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)pyridineanxiolytic drug;
biomarker;
immunomodulator;
mitogen;
neurotoxin;
nicotinic acetylcholine receptor agonist;
peripheral nervous system drug;
phytogenic insecticide;
plant metabolite;
psychotropic drug;
teratogenic agent;
xenobiotic
3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole: structure in first source
philanthotoxin 343philanthotoxin 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 4,3,3N-acyl-amino acid
vareniclinevarenicline : 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
tropisetrontropisetron : 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
epibatidine
hmr 3647
abt 594
5-(6-chloro-3-pyridinyl)-9-azabicyclo[4.2.1]non-4-eneazepine
trans-metanicotinemetanicotine: RN given refers to parent cpd with unspecified isomeric designation
a 85380A 85380: structure given in first source; A-85380 is the S-enantiomer; A-159470 is the R-enantiomer
ar-r 17779AR-R 17779: structure in first source
3-(2,4-dimethoxybenzylidene)anabaseine3-(2,4-dimethoxybenzylidene)anabaseine: an alpha7nAChR nicotinic receptor agonistdimethoxybenzene
mg 624triethyl-(beta-4-stilbenoxyethyl)ammonium: inhibits alpha7 nicotinic receptors; structure in first source
a 84543
radafaxineradafaxine: a bupropion metabolite; radafaxine is a (+)-isomer of hydroxybupropion
pnu-282987carbonyl compound;
organohalogen compound
ssr180711SSR180711: a selective alpha7 acetylcholine nicotinic receptor (n-AChRs) partial agonist; structure in first source
isproniclineispronicline: a neuronal nicotinic acetylcholine receptor modulator; has antidepressant, neuroprotective, and cognitive effects; structure in first source
desnitroimidaclopriddesnitroimidacloprid: a nicotinic receptor agonist; structure in first source
dianiclinedianicline: an alpha4beta2 nicotinic receptor agonist; may be useful as an aid in quitting smoking; structure in first source
pnu-282987
3-bromocytisine3-bromocytisine: structure in first source
a-582941A-582941: nicotinic acetylcholine receptor (alpha7 nAChR) agonist
n,n-diallyl-5-methoxytryptamineN,N-diallyl-5-methoxytryptamine: structure in first sourcetryptamines
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