Proteins > Neuronal acetylcholine receptor subunit beta-2
Page last updated: 2024-08-07 16:04:10
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]
Synonyms
Research
Bioassay Publications (86)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 6 (6.98) | 18.2507 |
2000's | 27 (31.40) | 29.6817 |
2010's | 49 (56.98) | 24.3611 |
2020's | 4 (4.65) | 2.80 |
Compounds (57)
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 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
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
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
Synthesis and nicotinic receptor activity of chemical space analogues of N-(3R)-1-azabicyclo[2.2.2]oct-3-yl-4-chlorobenzamide (PNU-282,987) and 1,4-diazabicyclo[3.2.2]nonane-4-carboxylic acid 4-bromophenyl ester (SSR180711).Journal of medicinal chemistry, , May-24, Volume: 55, Issue:10, 2012
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
Structure-activity studies and analgesic efficacy of N-(3-pyridinyl)-bridged bicyclic diamines, exceptionally potent agonists at nicotinic acetylcholine receptors.Journal of medicinal chemistry, , Jul-26, Volume: 50, Issue:15, 2007
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
Unique spirocyclopiperazinium salt III: further investigation of monospirocyclopiperazinium (MSPZ) salts as potential analgesics.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 17, Issue:22, 2007
Epibatidine isomers and analogues: structure-activity relationships.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 16, Issue:21, 2006
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
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
Synthesis and nicotinic receptor activity of a hydroxylated tropane.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
5-Azidoepibatidine: an exceptionally potent photoaffinity ligand for neuronal alpha 4 beta 2 and alpha 7 nicotinic acetylcholine receptors.Bioorganic & medicinal chemistry letters, , Feb-10, Volume: 13, Issue:3, 2003
Structural features of azidopyridinyl neonicotinoid probes conferring high affinity and selectivity for mammalian alpha4beta2 and Drosophila nicotinic receptors.Journal of medicinal chemistry, , Jun-20, Volume: 45, Issue:13, 2002
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
Molecular recognition in nicotinic acetylcholine receptors: the importance of pi-cation interactions.Journal of medicinal chemistry, , Aug-12, Volume: 42, Issue:16, 1999
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.Journal of medicinal chemistry, , Jul-28, Volume: 48, Issue:15, 2005
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
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.Bioorganic & medicinal chemistry letters, , Apr-19, Volume: 14, Issue:8, 2004
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
Pyridine alkaloids with activity in the central nervous system.Bioorganic & medicinal chemistry, , 12-15, Volume: 28, Issue:24, 2020
Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
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
Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.Journal of medicinal chemistry, , Jul-28, Volume: 48, Issue:15, 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
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
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Design, synthesis, and biological evaluation of Erythrina alkaloid analogues as neuronal nicotinic acetylcholine receptor antagonists.Journal of medicinal chemistry, , Dec-12, Volume: 56, Issue:23, 2013
Neonicotinic analogues: selective antagonists for α4β2 nicotinic acetylcholine receptors.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
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
Optical control of muscular nicotinic channels with azocuroniums, photoswitchable azobenzenes bearing two N-methyl-N-carbocyclic quaternary ammonium groups.European journal of medicinal chemistry, , Aug-15, Volume: 200, 2020
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-Based Design and Discovery of New MJournal of medicinal chemistry, , 11-22, Volume: 60, Issue:22, 2017
Enantiopure Cyclopropane-Bearing Pyridyldiazabicyclo[3.3.0]octanes as Selective α4β2-nAChR Ligands.ACS medicinal chemistry letters, , Nov-13, Volume: 5, Issue:11, 2014
Design, synthesis and discovery of picomolar selective α4β2 nicotinic acetylcholine receptor ligands.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Chemistry, pharmacology, and behavioral studies identify chiral cyclopropanes as selective α4β2-nicotinic acetylcholine receptor partial agonists exhibiting an antidepressant profile. Part II.Journal of medicinal chemistry, , Jul-11, Volume: 56, Issue:13, 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
Neonicotinic analogues: selective antagonists for α4β2 nicotinic acetylcholine receptors.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
Chemistry and pharmacological studies of 3-alkoxy-2,5-disubstituted-pyridinyl compounds as novel selective α4β2 nicotinic acetylcholine receptor ligands that reduce alcohol intake in rats.Journal of medicinal chemistry, , Apr-11, Volume: 56, Issue:7, 2013
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
Synthesis and nicotinic receptor activity of chemical space analogues of N-(3R)-1-azabicyclo[2.2.2]oct-3-yl-4-chlorobenzamide (PNU-282,987) and 1,4-diazabicyclo[3.2.2]nonane-4-carboxylic acid 4-bromophenyl ester (SSR180711).Journal of medicinal chemistry, , May-24, Volume: 55, Issue:10, 2012
Structure-based design, synthesis and structure-activity relationships of dibenzosuberyl- and benzoate-substituted tropines as ligands for acetylcholine-binding protein.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 22, Issue:3, 2012
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 (2S,3R)-N-[2-(pyridin-3-ylmethyl)-1-azabicyclo[2.2.2]oct-3-yl]benzo[b]furan-2-carboxamide (TC-5619), a selective α7 nicotinic acetylcholine receptor agonist, for the treatment of cognitive disorders.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 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
Chemistry and behavioral studies identify chiral cyclopropanes as selective α4β2-nicotinic acetylcholine receptor partial agonists exhibiting an antidepressant profile.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
Discovery of isoxazole analogues of sazetidine-A as selective α4β2-nicotinic acetylcholine receptor partial agonists for the treatment of depression.Journal of medicinal chemistry, , Oct-27, Volume: 54, Issue:20, 2011
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
Chemistry and pharmacological characterization of novel nitrogen analogues of AMOP-H-OH (Sazetidine-A, 6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol) as α4β2-nicotinic acetylcholine receptor-selective partial agonists.Journal of medicinal chemistry, , Oct-14, Volume: 53, Issue:19, 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
Octahydropyrrolo[3,4-c]pyrrole: a diamine scaffold for construction of either alpha4beta2 or alpha7-selective nicotinic acetylcholine receptor (nAChR) ligands. Substitutions that switch subtype selectivity.Journal of medicinal chemistry, , Jul-23, Volume: 52, Issue:14, 2009
Structure-activity studies and analgesic efficacy of N-(3-pyridinyl)-bridged bicyclic diamines, exceptionally potent agonists at nicotinic acetylcholine receptors.Journal of medicinal chemistry, , Jul-26, Volume: 50, Issue:15, 2007
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
Synthesis and nicotinic acetylcholine receptor binding properties of bridged and fused ring analogues of epibatidine.Journal of medicinal chemistry, , Dec-13, Volume: 50, Issue:25, 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
2-(Arylmethyl)-3-substituted quinuclidines as selective alpha 7 nicotinic receptor ligands.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 15, Issue:8, 2005
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
Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.Journal of medicinal chemistry, , Jul-28, Volume: 48, Issue:15, 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
alpha4beta2 nACh receptor pharmacophore models.Bioorganic & medicinal chemistry letters, , Apr-19, Volume: 14, Issue:8, 2004
Synthesis and nicotinic receptor activity of a hydroxylated tropane.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.Bioorganic & medicinal chemistry letters, , Jul-16, Volume: 14, Issue:14, 2004
Structural features of azidopyridinyl neonicotinoid probes conferring high affinity and selectivity for mammalian alpha4beta2 and Drosophila nicotinic receptors.Journal of medicinal chemistry, , Jun-20, Volume: 45, Issue:13, 2002
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
Molecular recognition in nicotinic acetylcholine receptors: the importance of pi-cation interactions.Journal of medicinal chemistry, , Aug-12, Volume: 42, Issue:16, 1999
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
Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Design, synthesis and discovery of picomolar selective α4β2 nicotinic acetylcholine receptor ligands.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Chemistry and pharmacological studies of 3-alkoxy-2,5-disubstituted-pyridinyl compounds as novel selective α4β2 nicotinic acetylcholine receptor ligands that reduce alcohol intake in rats.Journal of medicinal chemistry, , Apr-11, Volume: 56, Issue:7, 2013
Ion channels as therapeutic targets: a drug discovery perspective.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
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
Synthesis and nicotinic receptor activity of chemical space analogues of N-(3R)-1-azabicyclo[2.2.2]oct-3-yl-4-chlorobenzamide (PNU-282,987) and 1,4-diazabicyclo[3.2.2]nonane-4-carboxylic acid 4-bromophenyl ester (SSR180711).Journal of medicinal chemistry, , May-24, Volume: 55, Issue:10, 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
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
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.Bioorganic & medicinal chemistry letters, , Apr-19, Volume: 14, Issue:8, 2004
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
The twin drug approach for novel nicotinic acetylcholine receptor ligands.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
Exploration of the molecular architecture of the orthosteric binding site in the α4β2 nicotinic acetylcholine receptor with analogs of 3-(dimethylamino)butyl dimethylcarbamate (DMABC) and 1-(pyridin-3-yl)-1,4-diazepane.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
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
Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.Journal of medicinal chemistry, , Jul-28, Volume: 48, Issue:15, 2005
Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.Journal of medicinal chemistry, , Feb-12, Volume: 41, Issue:4, 1998
Synthesis and binding affinity at α4β2 and α7 nicotinic acetylcholine receptors of new analogs of epibatidine and epiboxidine containing the 7-azabicyclo[2.2.1]hept-2-ene ring system.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 22, Issue:2, 2012
Synthesis and nicotinic binding of novel phenyl derivatives of UB-165. Identifying factors associated with alpha7 selectivity.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 13, Issue:17, 2003
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
3-(4-Aminobutyn-1-yl)pyridines: binding at alpha 4 beta 2 nicotinic cholinergic receptors.Bioorganic & medicinal chemistry letters, , Jan-19, Volume: 14, Issue:2, 2004
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Discovery of novel 2-((pyridin-3-yloxy)methyl)piperazines as α7 nicotinic acetylcholine receptor modulators for the treatment of inflammatory disorders.Journal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
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
Complementary three-dimensional quantitative structure-activity relationship modeling of binding affinity and functional potency: a study on alpha4beta2 nicotinic ligands.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Synthesis and nicotinic acetylcholine receptor in vivo binding properties of 2-fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine: a new positron emission tomography ligand for nicotinic receptors.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.Journal of medicinal chemistry, , Feb-12, Volume: 41, Issue:4, 1998
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
Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.Journal of medicinal chemistry, , Jul-28, Volume: 48, Issue:15, 2005
From 2-Triethylammonium Ethyl Ether of 4-Stilbenol (MG624) to Selective Small-Molecule Antagonists of Human α9α10 Nicotinic Receptor by Modifications at the Ammonium Ethyl Residue.Journal of medicinal chemistry, , 07-28, Volume: 65, Issue:14, 2022
Potent Antiglioblastoma Agents by Hybridizing the Onium-Alkyloxy-Stilbene Based Structures of an α7-nAChR, α9-nAChR Antagonist and of a Pro-Oxidant Mitocan.Journal of medicinal chemistry, , 12-13, Volume: 61, Issue:23, 2018
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
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
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
Synthesis and nicotinic acetylcholine receptor binding properties of bridged and fused ring analogues of epibatidine.Journal of medicinal chemistry, , Dec-13, Volume: 50, Issue:25, 2007
Molecular recognition in nicotinic acetylcholine receptors: the importance of pi-cation interactions.Journal of medicinal chemistry, , Aug-12, Volume: 42, Issue:16, 1999
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
Enantiopure Cyclopropane-Bearing Pyridyldiazabicyclo[3.3.0]octanes as Selective α4β2-nAChR Ligands.ACS medicinal chemistry letters, , Nov-13, Volume: 5, Issue:11, 2014
Design, synthesis and discovery of picomolar selective α4β2 nicotinic acetylcholine receptor ligands.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Chemistry and pharmacological studies of 3-alkoxy-2,5-disubstituted-pyridinyl compounds as novel selective α4β2 nicotinic acetylcholine receptor ligands that reduce alcohol intake in rats.Journal of medicinal chemistry, , Apr-11, Volume: 56, Issue:7, 2013
Chemistry and behavioral studies identify chiral cyclopropanes as selective α4β2-nicotinic acetylcholine receptor partial agonists exhibiting an antidepressant profile.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
Structure-activity relationships of N-substituted ligands for the alpha7 nicotinic acetylcholine receptor.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 20, Issue:1, 2010
Octahydropyrrolo[3,4-c]pyrrole: a diamine scaffold for construction of either alpha4beta2 or alpha7-selective nicotinic acetylcholine receptor (nAChR) ligands. Substitutions that switch subtype selectivity.Journal of medicinal chemistry, , Jul-23, Volume: 52, Issue:14, 2009
Enables
This protein enables 8 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] |
protein-containing complex binding | molecular function | Binding to a macromolecular complex. [GOC:jl] |
quaternary ammonium group binding | molecular function | Binding to a quaternary ammonium group, including glycine betaine, choline, carnitine and proline. A quaternary ammonium group is any compound that can be regarded as derived from ammonium hydroxide or an ammonium salt by replacement of all four hydrogen atoms of the NH4+ ion by organic groups. [GOC:ai] |
heterocyclic compound binding | molecular function | Binding to heterocyclic compound. [GOC:TermGenie] |
Located In
This protein is located in 7 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] |
presynaptic membrane | cellular component | A specialized area of membrane of the axon terminal that faces the plasma membrane of the neuron or muscle fiber with which the axon terminal establishes a synaptic junction; many synaptic junctions exhibit structural presynaptic characteristics, such as conical, electron-dense internal protrusions, that distinguish it from the remainder of the axon plasma membrane. [GOC:jl, ISBN:0815316194] |
plasma membrane raft | cellular component | A membrane raft that is part of the plasma membrane. [GOC:jl] |
cholinergic synapse | cellular component | A synapse that uses acetylcholine as a neurotransmitter. [GOC:dos] |
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 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 42 target(s):
Target | Category | Definition |
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] |
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] |
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] |
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] |
visual perception | biological process | The series of events required for an organism to receive a visual stimulus, convert it to a molecular signal, and recognize and characterize the signal. Visual stimuli are detected in the form of photons and are processed to form an image. [GOC:ai] |
sensory perception of sound | biological process | The series of events required for an organism to receive an auditory stimulus, convert it to a molecular signal, and recognize and characterize the signal. Sonic stimuli are detected in the form of vibrations and are processed to form a sound. [GOC:ai] |
learning | biological process | Any process in an organism in which a relatively long-lasting adaptive behavioral change occurs as the result of experience. [ISBN:0582227089, ISBN:0721662544] |
memory | biological process | The activities involved in the mental information processing system that receives (registers), modifies, stores, and retrieves informational stimuli. The main stages involved in the formation and retrieval of memory are encoding (processing of received information by acquisition), storage (building a permanent record of received information as a result of consolidation) and retrieval (calling back the stored information and use it in a suitable way to execute a given task). [GOC:curators, ISBN:0582227089] |
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] |
associative learning | biological process | Learning by associating a stimulus (the cause) with a particular outcome (the effect). [ISBN:0582227089] |
visual learning | biological process | Any process in an organism in which a change in behavior of an individual occurs in response to repeated exposure to a visual cue. [GOC:jid, ISBN:0582227089] |
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] |
vestibulocochlear nerve development | biological process | The process whose specific outcome is the progression of the vestibulocochlear nerve over time, from its formation to the mature structure. This sensory nerve innervates the membranous labyrinth of the inner ear. The vestibular branch innervates the vestibular apparatus that senses head position changes relative to gravity. The auditory branch innervates the cochlear duct, which is connected to the three bony ossicles which transduce sound waves into fluid movement in the cochlea. [GO_REF:0000021, GOC:cls, GOC:dgh, GOC:dph, GOC:jid, ISBN:0838580343] |
optic nerve morphogenesis | biological process | The process in which the anatomical structure of the optic nerve is generated and organized. The sensory optic nerve originates from the bipolar cells of the retina and conducts visual information to the brainstem. The optic nerve exits the back of the eye in the orbit, enters the optic canal, and enters the central nervous system at the optic chiasm (crossing) where the nerve fibers become the optic tract just prior to entering the hindbrain. [GO_REF:0000021, GOC:cls, GOC:dgh, GOC:dph, GOC:jid, ISBN:0838580343] |
lateral geniculate nucleus development | biological process | The progression of the lateral geniculate nucleus over time from its initial formation until its mature state. The lateral geniculate nucleus is the primary processor of visual information received from the retina. [GO_REF:0000021, GOC:cls, GOC:dgh, GOC:dph, GOC:jid, ISBN:0878937420] |
central nervous system projection neuron axonogenesis | biological process | Generation of a long process of a CNS neuron, that carries efferent (outgoing) action potentials from the cell body towards target cells in a different central nervous system region. [GO_REF:0000021, GOC:cls, GOC:dgh, GOC:dph, GOC:jid] |
positive regulation of B cell proliferation | biological process | Any process that activates or increases the rate or extent of B cell proliferation. [GOC:mah] |
regulation of synaptic transmission, dopaminergic | biological process | Any process that modulates the frequency, rate or extent of dopaminergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter dopamine. [GOC:mah] |
positive regulation of dopamine secretion | biological process | Any process that activates or increases the frequency, rate or extent of the regulated release of dopamine. [GOC:sl] |
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] |
social behavior | biological process | Behavior directed towards society, or taking place between members of the same species. Occurs predominantly, or only, in individuals that are part of a group. [GOC:jh2, PMID:12848939, Wikipedia:Social_behavior] |
regulation of dopamine metabolic process | biological process | Any process that modulates the frequency, rate or extent of the chemical reactions and pathways involving dopamine. [GOC:go_curators] |
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] |
response to cocaine | 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 cocaine stimulus. Cocaine is a crystalline alkaloid obtained from the leaves of the coca plant. [GOC:ef, GOC:jl] |
regulation of circadian sleep/wake cycle, REM sleep | biological process | Any process that modulates the frequency, rate or extent of rapid eye movement (REM) sleep. [GOC:jl, PMID:11506998] |
response to ethanol | 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 an ethanol stimulus. [GOC:go_curators] |
negative regulation of action potential | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of action potential creation, propagation or termination. This typically occurs via modulation of the activity or expression of voltage-gated ion channels. [GOC:go_curators] |
regulation of dendrite morphogenesis | biological process | Any process that modulates the frequency, rate or extent of dendrite morphogenesis. [GOC:ai] |
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] |
regulation of synapse assembly | biological process | Any process that modulates the frequency, rate or extent of synapse assembly, the aggregation, arrangement and bonding together of a set of components to form a synapse. [GOC:ai, GOC:pr] |
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] |
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 acetylcholine | 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 an acetylcholine stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:21238497] |
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] |