Proteins > Neuronal acetylcholine receptor subunit beta-4
Page last updated: 2024-08-07 16:26:53
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]
Synonyms
Research
Bioassay Publications (53)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 3 (5.66) | 18.2507 |
2000's | 16 (30.19) | 29.6817 |
2010's | 29 (54.72) | 24.3611 |
2020's | 5 (9.43) | 2.80 |
Compounds (34)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for smoking cessation.Journal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 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 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
Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.Journal of medicinal chemistry, , Jul-28, Volume: 48, Issue:15, 2005
Pyridine alkaloids with activity in the central nervous system.Bioorganic & medicinal chemistry, , 12-15, Volume: 28, Issue:24, 2020
Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine.Journal of natural products, , 04-27, Volume: 81, Issue:4, 2018
Pyridinyl- and pyridazinyl-3,6-diazabicyclo[3.1.1]heptane-anilines: Novel selective ligands with subnanomolar affinity for αEuropean journal of medicinal chemistry, , May-25, Volume: 152, 2018
Structure-activity relationships of N-substituted ligands for the alpha7 nicotinic acetylcholine receptor.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 20, Issue:1, 2010
Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 19, Issue:6, 2009
Synthesis and structure-activity relationship studies of 3,6-diazabicyclo[3.2.0]heptanes as novel alpha4beta2 nicotinic acetylcholine receptor selective agonists.Journal of medicinal chemistry, , Nov-01, Volume: 50, Issue:22, 2007
Epibatidine isomers and analogues: structure-activity relationships.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 16, Issue:21, 2006
Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Coaxing a pyridine nucleus to give up its aromaticity: synthesis and pharmacological characterization of novel conformationally restricted analogues of nicotine and anabasine.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
Synthesis and nicotinic receptor activity of a hydroxylated tropane.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
exo-2-(Pyridazin-4-yl)-7-azabicyclo[2.2.1]heptanes: syntheses and nicotinic acetylcholine receptor agonist activity of potent pyridazine analogues of (+/-)-epibatidine.Journal of medicinal chemistry, , Jan-04, Volume: 44, Issue:1, 2001
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Discovery of benzamide analogs as negative allosteric modulators of human neuronal nicotinic receptors: pharmacophore modeling and structure-activity relationship studies.Bioorganic & medicinal chemistry, , Aug-01, Volume: 21, Issue:15, 2013
Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.Journal of medicinal chemistry, , Jul-28, Volume: 48, Issue:15, 2005
Structure activity studies of ring E analogues of methyllycaconitine. Part 2: Synthesis of antagonists to the alpha3beta4* nicotinic acetylcholine receptors through modifications to the ester.Bioorganic & medicinal chemistry letters, , Jul-16, Volume: 14, Issue:14, 2004
Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
(+)-Laburnamine, a natural selective ligand and partial agonist for the α4β2 nicotinic receptor subtype.Journal of natural products, , Apr-26, Volume: 76, Issue:4, 2013
Deconstructing cytisine: The syntheses of (+/-)-cyfusine and (+/-)-cyclopropylcyfusine, fused ring analogs of cytisine.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 18, Issue:7, 2008
Epibatidine isomers and analogues: structure-activity relationships.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 16, Issue:21, 2006
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
In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 15, Issue:12, 2005
Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation.Journal of medicinal chemistry, , May-19, Volume: 48, Issue:10, 2005
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Modifications at C(5) of 2-(2-Pyrrolidinyl)-Substituted 1,4-Benzodioxane Elicit Potent α4β2 Nicotinic Acetylcholine Receptor Partial Agonism with High Selectivity over the α3β4 Subtype.Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Pyridine alkaloids with activity in the central nervous system.Bioorganic & medicinal chemistry, , 12-15, Volume: 28, Issue:24, 2020
Discovery and Development of 3-(6-Chloropyridine-3-yloxymethyl)-2-azabicyclo[3.1.0]hexane Hydrochloride (SUVN-911): A Novel, Potent, Selective, and Orally Active Neuronal Nicotinic Acetylcholine α4β2 Receptor Antagonist for the Treatment of Depression.Journal of medicinal chemistry, , 03-26, Volume: 63, Issue:6, 2020
From pyrrolidinyl-benzodioxane to pyrrolidinyl-pyridodioxanes, or from unselective antagonism to selective partial agonism at α4β2 nicotinic acetylcholine receptor.European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
Novel 5-substituted 3-hydroxyphenyl and 3-nitrophenyl ethers of S-prolinol as α4β2-nicotinic acetylcholine receptor ligands.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 26, Issue:23, 2016
Chemistry and Pharmacology of a Series of Unichiral Analogues of 2-(2-Pyrrolidinyl)-1,4-benzodioxane, Prolinol Phenyl Ether, and Prolinol 3-Pyridyl Ether Designed as α4β2-Nicotinic Acetylcholine Receptor Agonists.Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
(+)-Laburnamine, a natural selective ligand and partial agonist for the α4β2 nicotinic receptor subtype.Journal of natural products, , Apr-26, Volume: 76, Issue:4, 2013
Novel nicotinic acetylcholine receptor agonists containing carbonyl moiety as a hydrogen bond acceptor.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 23, Issue:13, 2013
From α4β2 Nicotinic Ligands to the Discovery of σ1 Receptor Ligands: Pharmacophore Analysis and Rational Design.ACS medicinal chemistry letters, , Dec-13, Volume: 3, Issue:12, 2012
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
Discovery of 3-(5-chloro-2-furoyl)-3,7-diazabicyclo[3.3.0]octane (TC-6683, AZD1446), a novel highly selective α4β2 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders.Journal of medicinal chemistry, , Nov-08, Volume: 55, Issue:21, 2012
Identification of novel α4β2-nicotinic acetylcholine receptor (nAChR) agonists based on an isoxazole ether scaffold that demonstrate antidepressant-like activity.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 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
Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 19, Issue:6, 2009
Synthesis and structure-activity relationship studies of 3,6-diazabicyclo[3.2.0]heptanes as novel alpha4beta2 nicotinic acetylcholine receptor selective agonists.Journal of medicinal chemistry, , Nov-01, Volume: 50, Issue:22, 2007
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
In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 15, Issue:12, 2005
Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation.Journal of medicinal chemistry, , May-19, Volume: 48, Issue:10, 2005
Coaxing a pyridine nucleus to give up its aromaticity: synthesis and pharmacological characterization of novel conformationally restricted analogues of nicotine and anabasine.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
Synthesis and nicotinic receptor activity of a hydroxylated tropane.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
Synthesis and structure-activity relationships of pyridine-modified analogs of 3-[2-((S)-pyrrolidinyl)methoxy]pyridine, A-84543, a potent nicotinic acetylcholine receptor agonist.Bioorganic & medicinal chemistry letters, , Feb-03, Volume: 8, Issue:3, 1998
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
(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
Identification of novel α4β2-nicotinic acetylcholine receptor (nAChR) agonists based on an isoxazole ether scaffold that demonstrate antidepressant-like activity.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 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
Structure-activity studies of 7-heteroaryl-3-azabicyclo[3.3.1]non-6-enes: a novel class of highly potent nicotinic receptor ligands.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Discovery of novel α7 nicotinic acetylcholine receptor ligands via pharmacophoric and docking studies of benzylidene anabaseine analogs.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 22, Issue:2, 2012
Docking studies of benzylidene anabaseine interactions with α7 nicotinic acetylcholine receptor (nAChR) and acetylcholine binding proteins (AChBPs): application to the design of related α7 selective ligands.European journal of medicinal chemistry, , Volume: 46, Issue:11, 2011
Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.Journal of medicinal chemistry, , Jul-28, Volume: 48, Issue:15, 2005
Synthesis of 2-(substituted phenyl)-3,5,5-trimethylmorpholine analogues and their effects on monoamine uptake, nicotinic acetylcholine receptor function, and behavioral effects of nicotine.Journal of medicinal chemistry, , Mar-10, Volume: 54, Issue:5, 2011
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
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
Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo effJournal of medicinal chemistry, , Feb-11, Volume: 53, Issue:3, 2010
Enables
This protein enables 4 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] |
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] |
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] |
specific granule membrane | cellular component | The lipid bilayer surrounding a specific granule, a granule with a membranous, tubular internal structure, found primarily in mature neutrophil cells. Most are released into the extracellular fluid. Specific granules contain lactoferrin, lysozyme, vitamin B12 binding protein and elastase. [GOC:bf, PMID:7334549] |
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] |
tertiary granule membrane | cellular component | The lipid bilayer surrounding a tertiary granule. [GOC:BHF, GOC:mah, GOC:rl, PMID:12070036] |
cholinergic synapse | cellular component | A synapse that uses acetylcholine as a neurotransmitter. [GOC:dos] |
Active In
This protein is active in 3 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] |
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/] |
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] |
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 16 target(s):
Target | Category | Definition |
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] |
smooth muscle contraction | biological process | A process in which force is generated within smooth 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. Smooth muscle differs from striated muscle in the much higher actin/myosin ratio, the absence of conspicuous sarcomeres and the ability to contract to a much smaller fraction of its resting length. [GOC:ef, GOC:jl, GOC:mtg_muscle, ISBN:0198506732] |
regulation of smooth muscle contraction | biological process | Any process that modulates the frequency, rate or extent of smooth muscle contraction. [GOC:go_curators] |
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] |
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] |
locomotory behavior | biological process | The specific movement from place to place of an organism in response to external or internal stimuli. Locomotion of a whole organism in a manner dependent upon some combination of that organism's internal state and external conditions. [GOC:dph] |
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] |
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] |
regulation of neurotransmitter secretion | biological process | Any process that modulates the frequency, rate or extent of the regulated release of a neurotransmitter from a cell. [GOC:ai] |
positive regulation of transmission of nerve impulse | biological process | Any process that activates, maintains or increases the frequency, rate or extent of transmission of a nerve impulse, the sequential electrochemical polarization and depolarization that travels across the membrane of a neuron in response to stimulation. [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] |
synaptic transmission involved in micturition | biological process | The process of communication from a neuron to a smooth muscle in the bladder that contributes to the expulsion of urine from the body. [GOC:dph, PMID:15827347] |
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] |
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] |
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] |