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]

Synonyms

Research

Bioassay Publications (82)

Timeframe	Studies on this Protein(%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	6 (7.32)	18.2507
2000's	25 (30.49)	29.6817
2010's	47 (57.32)	24.3611
2020's	4 (4.88)	2.80

Compounds (56)

Drugs with Inhibition Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
nornicotine	Homo sapiens (human)	Ki	0.0290	1	1
bupropion	Homo sapiens (human)	IC50	9.0039	7	7
3-(1-methylpyrrolidin-2-yl)pyridine	Homo sapiens (human)	Ki	0.0010	1	1
epibatidine	Homo sapiens (human)	IC50	0.0011	1	1
epibatidine	Homo sapiens (human)	Ki	0.0000	8	9
anabasine	Homo sapiens (human)	Ki	0.0920	1	1
carbamylcholine	Homo sapiens (human)	Ki	0.7500	1	1
granisetron	Homo sapiens (human)	Ki	38.0000	1	1
mecamylamine	Homo sapiens (human)	IC50	0.6000	1	1
n-methylcarbamylcholine	Homo sapiens (human)	Ki	0.0230	1	1
ondansetron	Homo sapiens (human)	IC50	66.0000	1	1
ondansetron	Homo sapiens (human)	Ki	46.0000	1	1
tetramethylammonium	Homo sapiens (human)	Ki	0.0240	1	1
indopan	Homo sapiens (human)	Ki	10.0000	3	3
boldine	Homo sapiens (human)	IC50	10.0000	1	1
boldine	Homo sapiens (human)	Ki	3.0000	1	1
cytisine	Homo sapiens (human)	IC50	14.0250	2	2
cytisine	Homo sapiens (human)	Ki	0.0011	5	5
dihydro-beta-erythroidine	Homo sapiens (human)	IC50	0.1470	3	3
dihydro-beta-erythroidine	Homo sapiens (human)	Ki	0.0980	1	1
polygodial	Homo sapiens (human)	IC50	62.5000	1	1
N-methyl-N-(3-pyridylmethyl)amine	Homo sapiens (human)	Ki	10.0000	1	1
nicotine	Homo sapiens (human)	IC50	0.3456	10	12
nicotine	Homo sapiens (human)	Ki	0.3444	30	30
lobeline	Homo sapiens (human)	Ki	0.0050	1	1
philanthotoxin 343	Homo sapiens (human)	IC50	0.0802	1	1
erysodine	Homo sapiens (human)	Ki	0.0500	1	1
varenicline	Homo sapiens (human)	IC50	8.3893	5	6
varenicline	Homo sapiens (human)	Ki	0.5009	9	9
pozanicline	Homo sapiens (human)	Ki	0.0260	1	1
anatoxin a	Homo sapiens (human)	Ki	0.0011	1	1
deformylflustrabromine	Homo sapiens (human)	IC50	150.0000	1	1
tropacocaine	Homo sapiens (human)	Ki	31.6228	1	1
tropisetron	Homo sapiens (human)	IC50	170.0000	1	1
tropisetron	Homo sapiens (human)	Ki	55.0000	1	1
lobeline	Homo sapiens (human)	Ki	0.0047	2	3
anatoxin a	Homo sapiens (human)	Ki	0.0003	1	1
abt 594	Homo sapiens (human)	Ki	0.0000	1	2
5-(6-chloro-3-pyridinyl)-9-azabicyclo[4.2.1]non-4-ene	Homo sapiens (human)	Ki	0.0002	2	2
trans-metanicotine	Homo sapiens (human)	Ki	0.0255	2	2
a 85380	Homo sapiens (human)	IC50	0.0015	1	1
a 85380	Homo sapiens (human)	Ki	0.0000	3	3
ar-r 17779	Homo sapiens (human)	IC50	2,000.0000	1	1
3-(2,4-dimethoxybenzylidene)anabaseine	Homo sapiens (human)	Ki	0.0510	1	1
mg 624	Homo sapiens (human)	Ki	1.5028	2	2
azd 0328	Homo sapiens (human)	Ki	0.1400	1	1
radafaxine	Homo sapiens (human)	IC50	30.5000	4	4
4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride	Homo sapiens (human)	Ki	1.0000	1	1
desnitroimidacloprid	Homo sapiens (human)	Ki	0.0022	1	1
n-methylepibatidine	Homo sapiens (human)	Ki	0.0001	2	2
sazetidine-a	Homo sapiens (human)	IC50	0.0079	4	4
sazetidine-a	Homo sapiens (human)	Ki	0.0001	1	1
a-582941	Homo sapiens (human)	Ki	100.0000	1	1
n,n-diallyl-5-methoxytryptamine	Homo sapiens (human)	Ki	10.0000	3	3
imidacloprid	Homo sapiens (human)	Ki	0.7200	1	1
3-(4-hydroxy-2-methoxybenzylidene)anabaseine	Homo sapiens (human)	Ki	0.0190	1	1

Drugs with Activation Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
epibatidine	Homo sapiens (human)	EC50	0.0356	7	9
dimethylphenylpiperazinium iodide	Homo sapiens (human)	EC50	2.5000	1	1
tilorone	Homo sapiens (human)	EC50	10.0000	2	2
cytisine	Homo sapiens (human)	EC50	13.3335	3	3
anatabine	Homo sapiens (human)	EC50	2.6500	1	1
nicotine	Homo sapiens (human)	EC50	3.1424	20	24
3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole	Homo sapiens (human)	EC50	10.6000	1	1
varenicline	Homo sapiens (human)	EC50	0.7850	6	7
epibatidine	Homo sapiens (human)	Kd	0.0000	1	1
abt 594	Homo sapiens (human)	EC50	0.0200	1	1
trans-metanicotine	Homo sapiens (human)	EC50	4.3000	1	1
a 85380	Homo sapiens (human)	EC50	0.7016	4	5
3-(2,4-dimethoxybenzylidene)anabaseine	Homo sapiens (human)	EC50	10.0000	2	2
5-ia-85380	Homo sapiens (human)	EC50	0.7000	1	1
a 84543	Homo sapiens (human)	EC50	0.7500	2	2
ispronicline	Homo sapiens (human)	EC50	5.0530	2	2
dianicline	Homo sapiens (human)	EC50	100.0000	1	1
sazetidine-a	Homo sapiens (human)	EC50	0.0120	5	5
ns 9283	Homo sapiens (human)	EC50	0.8900	2	2
a-582941	Homo sapiens (human)	EC50	100.0000	1	1

Drugs with Other Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
bupropion	Homo sapiens (human)	Concentration	12.0000	2	3
3-(1-methylpyrrolidin-2-yl)pyridine	Homo sapiens (human)	ED50	4.0000	1	1
epibatidine	Homo sapiens (human)	Activity	0.0050	1	1
epibatidine	Homo sapiens (human)	ED50	0.0170	1	1
epibatidine	Homo sapiens (human)	INH	0.0001	1	1
mecamylamine	Homo sapiens (human)	Concentration	1.4100	2	4
abt 594	Homo sapiens (human)	Rmax	130.0000	1	1

Enables

This protein enables 5 target(s):

Target	Category	Definition
protein binding	molecular function	Binding to a protein. [GOC:go_curators]
ligand-gated monoatomic ion channel activity	molecular function	Enables the transmembrane transfer of an ion by a channel that opens when a specific ligand has been bound by the channel complex or one of its constituent parts. [GOC:mtg_transport, ISBN:0815340729]
acetylcholine receptor activity	molecular function	Combining with an acetylcholine receptor ligand and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity. [GOC:jl, GOC:signaling]
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]
acetylcholine binding	molecular function	Binding to acetylcholine, an acetic acid ester of the organic base choline that functions as a neurotransmitter, released at the synapses of parasympathetic nerves and at neuromuscular junctions. [GOC:ai]

Located In

This protein is located in 6 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]
external side of plasma membrane	cellular component	The leaflet of the plasma membrane that faces away from the cytoplasm and any proteins embedded or anchored in it or attached to its surface. [GOC:dos, GOC:tb]
membrane	cellular component	A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194]
dendrite	cellular component	A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732]
neuronal cell body	cellular component	The portion of a neuron that includes the nucleus, but excludes cell projections such as axons and dendrites. [GOC:go_curators]
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]

Active In

This protein is active in 3 target(s):

Target	Category	Definition
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]
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/]
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]

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 22 target(s):

Target	Category	Definition
action potential	biological process	A process in which membrane potential cycles through a depolarizing spike, triggered in response to depolarization above some threshold, followed by repolarization. This cycle is driven by the flow of ions through various voltage gated channels with different thresholds and ion specificities. [GOC:dph, GOC:go_curators, GOC:tb, ISBN:978-0-07-139011-8]
response to hypoxia	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 stimulus indicating lowered oxygen tension. Hypoxia, defined as a decline in O2 levels below normoxic levels of 20.8 - 20.95%, results in metabolic adaptation at both the cellular and organismal level. [GOC:hjd]
DNA repair	biological process	The process of restoring DNA after damage. Genomes are subject to damage by chemical and physical agents in the environment (e.g. UV and ionizing radiations, chemical mutagens, fungal and bacterial toxins, etc.) and by free radicals or alkylating agents endogenously generated in metabolism. DNA is also damaged because of errors during its replication. A variety of different DNA repair pathways have been reported that include direct reversal, base excision repair, nucleotide excision repair, photoreactivation, bypass, double-strand break repair pathway, and mismatch repair pathway. [PMID:11563486]
monoatomic ion transport	biological process	The directed movement of a monoatomic ion into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Monatomic ions (also called simple ions) are ions consisting of exactly one atom. [GOC:ai]
calcium ion transport	biological process	The directed movement of calcium (Ca) ions into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai]
response to oxidative stress	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 oxidative stress, a state often resulting from exposure to high levels of reactive oxygen species, e.g. superoxide anions, hydrogen peroxide (H2O2), and hydroxyl radicals. [GOC:jl, PMID:12115731]
signal transduction	biological process	The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11]
chemical synaptic transmission	biological process	The vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter 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:jl, MeSH:D009435]
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]
regulation of dopamine secretion	biological process	Any process that modulates the frequency, rate or extent of the regulated release of dopamine. [GOC:ef]
sensory perception of pain	biological process	The series of events required for an organism to receive a painful stimulus, convert it to a molecular signal, and recognize and characterize the signal. Pain is medically defined as the physical sensation of discomfort or distress caused by injury or illness, so can hence be described as a harmful stimulus which signals current (or impending) tissue damage. Pain may come from extremes of temperature, mechanical damage, electricity or from noxious chemical substances. This is a neurological process. [GOC:curators]
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]
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]
behavioral response to nicotine	biological process	Any process that results in a change in the behavior of an organism as a result of a nicotine stimulus. [GOC:bf, ISBN:0198506732]
B cell activation	biological process	The change in morphology and behavior of a mature or immature B cell resulting from exposure to a mitogen, cytokine, chemokine, cellular ligand, or an antigen for which it is specific. [GOC:mgi_curators, ISBN:0781735149]
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]
nervous system process	biological process	A organ system process carried out by any of the organs or tissues of neurological system. [GOC:ai, GOC:mtg_cardio]
cognition	biological process	The operation of the mind by which an organism becomes aware of objects of thought or perception; it includes the mental activities associated with thinking, learning, and memory. [ISBN:0721619908]
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]
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]
inhibitory postsynaptic potential	biological process	A process that causes a temporary decrease in postsynaptic membrane potential due to the flow of negatively charged ions into the postsynaptic cell. The flow of ions that causes an IPSP is an inhibitory postsynaptic current (IPSC) and makes it more difficult for the neuron to fire an action potential. [GOC:dph, GOC:ef]
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]