Proteins > Acetylcholine receptor subunit alpha
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Acetylcholine receptor subunit alpha
An acetylcholine receptor subunit alpha that is encoded in the genome of human. [PRO:DNx, UniProtKB:P02708]
Synonyms
Research
Bioassay Publications (18)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (11.11) | 18.2507 |
| 2000's | 7 (38.89) | 29.6817 |
| 2010's | 9 (50.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (18)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| epibatidine | Homo sapiens (human) | EC50 | 0.0001 | 1 | 1 |
| mecamylamine | Homo sapiens (human) | EC50 | 30.0000 | 1 | 1 |
| cytisine | Homo sapiens (human) | EC50 | 0.0110 | 1 | 1 |
| nicotine | Homo sapiens (human) | EC50 | 25.3333 | 3 | 3 |
| varenicline | Homo sapiens (human) | EC50 | 1.0000 | 1 | 1 |
Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation.Journal of medicinal chemistry, , Jun-24, Volume: 53, Issue:12, 2010
Nicotinic acetylcholine receptor efficacy and pharmacological properties of 3-(substituted phenyl)-2β-substituted tropanes.Journal of medicinal chemistry, , Dec-09, Volume: 53, Issue:23, 2010
Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for smoking cessation.Journal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 2010
3,5-Bicyclic aryl piperidines: a novel class of alpha4beta2 neuronal nicotinic receptor partial agonists for smoking cessation.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 15, Issue:22, 2005
Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 15, Issue:4, 2005
Discovery of highly potent and selective α4β2-nicotinic acetylcholine receptor (nAChR) partial agonists containing an isoxazolylpyridine ether scaffold that demonstrate antidepressant-like activity. Part II.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
A novel series of [3.2.1] azabicyclic biaryl ethers as alpha3beta4 and alpha6/4beta4 nicotinic receptor agonists.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 20, Issue:16, 2010
3,5-Bicyclic aryl piperidines: a novel class of alpha4beta2 neuronal nicotinic receptor partial agonists for smoking cessation.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 15, Issue:22, 2005
The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist.Bioorganic & medicinal chemistry letters, , Feb-12, Volume: 11, Issue:3, 2001
Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors.Journal of agricultural and food chemistry, , Volume: 48, Issue:12, 2000
(S)-(-)-5-ethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine maleate (SIB-1508Y): a novel anti-parkinsonian agent with selectivity for neuronal nicotinic acetylcholine receptors.Journal of medicinal chemistry, , Aug-16, Volume: 39, Issue:17, 1996
Discovery of highly potent and selective α4β2-nicotinic acetylcholine receptor (nAChR) partial agonists containing an isoxazolylpyridine ether scaffold that demonstrate antidepressant-like activity. Part II.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
A novel series of [3.2.1] azabicyclic biaryl ethers as alpha3beta4 and alpha6/4beta4 nicotinic receptor agonists.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 20, Issue:16, 2010
Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationshJournal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
Enables
This protein enables 2 target(s):
| Target | Category | Definition |
|---|
| acetylcholine-gated monoatomic cation-selective channel activity | molecular function | Selectively enables the transmembrane transfer of a cation by a channel that opens upon binding acetylcholine. [GOC:mah, PMID:2466967] |
| transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential | molecular function | Any transmitter-gated ion channel activity that is involved in regulation of postsynaptic membrane potential. [GO_REF:0000061, GOC:TermGenie, PMID:20200227] |
Located In
This protein is located in 5 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| cell surface | cellular component | The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm] |
| neuromuscular junction | cellular component | The junction between the axon of a motor neuron and a muscle fiber. In response to the arrival of action potentials, the presynaptic button releases molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane of the muscle fiber, leading to a change in post-synaptic potential. [GOC:nln] |
| postsynaptic membrane | cellular component | A specialized area of membrane facing the presynaptic membrane on the tip of the nerve ending and separated from it by a minute cleft (the synaptic cleft). Neurotransmitters cross the synaptic cleft and transmit the signal to the postsynaptic membrane. [ISBN:0198506732] |
| postsynaptic specialization membrane | cellular component | The membrane component of the postsynaptic specialization. This is the region of the postsynaptic membrane in which the population of neurotransmitter receptors involved in synaptic transmission are concentrated. [GOC:dos] |
Active In
This protein is active in 4 target(s):
| Target | Category | Definition |
|---|
| neuromuscular junction | cellular component | The junction between the axon of a motor neuron and a muscle fiber. In response to the arrival of action potentials, the presynaptic button releases molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane of the muscle fiber, leading to a change in post-synaptic potential. [GOC:nln] |
| synapse | cellular component | The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| neuron projection | cellular component | A prolongation or process extending from a nerve cell, e.g. an axon or dendrite. [GOC:jl, http://www.cogsci.princeton.edu/~wn/] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| acetylcholine-gated channel complex | cellular component | 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] |
Involved In
This protein is involved in 15 target(s):
| Target | Category | Definition |
|---|
| skeletal muscle contraction | biological process | A process in which force is generated within skeletal muscle tissue, resulting in a change in muscle geometry. Force generation involves a chemo-mechanical energy conversion step that is carried out by the actin/myosin complex activity, which generates force through ATP hydrolysis. In the skeletal muscle, the muscle contraction takes advantage of an ordered sarcomeric structure and in most cases it is under voluntary control. [GOC:mtg_cardio, GOC:mtg_muscle] |
| monoatomic cation transport | biological process | The directed movement of a monoatomic cation, into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Monatomic cations (also called simple cations) are positively charged ions consisting of exactly one atom. [GOC:ai] |
| neuronal action potential | biological process | An action potential that occurs in a neuron. [GOC:dph, GOC:isa_complete, GOC:tb] |
| monoatomic ion transmembrane transport | biological process | A process in which a monoatomic ion is transported across a membrane. Monatomic ions (also called simple ions) are ions consisting of exactly one atom. [GOC:mah] |
| regulation of membrane potential | biological process | Any process that modulates the establishment or extent of a membrane potential, the electric potential existing across any membrane arising from charges in the membrane itself and from the charges present in the media on either side of the membrane. [GOC:jl, GOC:mtg_cardio, GOC:tb, ISBN:0198506732] |
| muscle cell cellular homeostasis | biological process | The cellular homeostatic process that preserves a muscle cell in a stable functional or structural state. [GOC:mah, PMID:3091429, PMID:7781901] |
| skeletal muscle tissue growth | biological process | The increase in size or mass of a skeletal muscle. This may be due to a change in the fiber number or size. [GOC:lm, PMID:15726494, PMID:15907921] |
| musculoskeletal movement | biological process | The movement of an organism or part of an organism using mechanoreceptors, the nervous system, striated muscle and/or the skeletal system. [GOC:dph] |
| neuromuscular process | biological process | Any process pertaining to the functions of the nervous and muscular systems of an organism. [GOC:ai] |
| excitatory postsynaptic potential | biological process | A process that leads to a temporary increase in postsynaptic potential due to the flow of positively charged ions into the postsynaptic cell. The flow of ions that causes an EPSP is an excitatory postsynaptic current (EPSC) and makes it easier for the neuron to fire an action potential. [GOC:dph, GOC:ef] |
| neuron cellular homeostasis | biological process | The cellular homeostatic process that preserves a neuron in a stable, differentiated functional and structural state. [GOC:BHF, GOC:mah] |
| membrane depolarization | biological process | The process in which membrane potential decreases with respect to its steady-state potential, usually from negative potential to a more positive potential. For example, the initial depolarization during the rising phase of an action potential is in the direction from the negative steady-state resting potential towards the positive membrane potential that will be the peak of the action potential. [GOC:dh, Wikipedia:Depolarization] |
| acetylcholine receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of an acetylcholine receptor binding to one of its physiological ligands. [GOC:mah] |
| response to nicotine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a nicotine stimulus. [GOC:bf, GOC:ef, ISBN:0198506732, ISBN:0582227089] |
| synaptic transmission, cholinergic | biological process | The vesicular release of acetylcholine from a presynapse, across a chemical synapse, the subsequent activation of dopamine receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:dos, Wikipedia:Cholinergic] |