Proteins > Neuronal acetylcholine receptor subunit alpha-3
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Neuronal acetylcholine receptor subunit alpha-3
A neuronal acetylcholine receptor subunit alpha-3 that is encoded in the genome of rat. [OMA:P04757, PRO:DNx]
Synonyms
Research
Bioassay Publications (55)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 2 (3.64) | 18.7374 |
| 1990's | 8 (14.55) | 18.2507 |
| 2000's | 17 (30.91) | 29.6817 |
| 2010's | 25 (45.45) | 24.3611 |
| 2020's | 3 (5.45) | 2.80 |
Compounds (33)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| epibatidine | Rattus norvegicus (Norway rat) | Affinity | 0.0005 | 1 | 1 |
| epibatidine | Rattus norvegicus (Norway rat) | K app | 0.0000 | 1 | 3 |
| cytisine | Rattus norvegicus (Norway rat) | Affinity | 0.2200 | 1 | 1 |
| nicotine | Rattus norvegicus (Norway rat) | K app | 0.0062 | 1 | 3 |
Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine.Journal of natural products, , 04-27, Volume: 81, Issue:4, 2018
Novel α3β4 nicotinic acetylcholine receptor-selective ligands. Discovery, structure-activity studies, and pharmacological evaluation.Journal of medicinal chemistry, , Nov-25, Volume: 53, Issue:22, 2010
Synthesis and biological evaluation of novel carbon-11 labeled pyridyl ethers: candidate ligands for in vivo imaging of alpha4beta2 nicotinic acetylcholine receptors (alpha4beta2-nAChRs) in the brain with positron emission tomography.Bioorganic & medicinal chemistry, , Jul-01, Volume: 17, Issue:13, 2009
Discovery of (-)-7-methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane, a radiolabeled antagonist for cerebral nicotinic acetylcholine receptor (alpha4beta2-nAChR) with optimal positron emission tomography imaging propertJournal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity.Journal of medicinal chemistry, , May-04, Volume: 49, Issue:9, 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
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
Ligand selectivity for the acetylcholine binding site of the rat alpha4beta2 and alpha3beta4 nicotinic subtypes investigated by molecular docking.Journal of medicinal chemistry, , Aug-11, Volume: 48, Issue:16, 2005
Epibatidine analogues as selective ligands for the alpha(x)beta2-containing subtypes of nicotinic acetylcholine receptors.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 15, Issue:19, 2005
Epibatidine structure-activity relationships.Bioorganic & medicinal chemistry letters, , Apr-19, Volume: 14, Issue:8, 2004
Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.Bioorganic & medicinal chemistry letters, , Apr-19, Volume: 14, Issue:8, 2004
Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors.Bioorganic & medicinal chemistry letters, , Apr-19, Volume: 14, Issue:8, 2004
Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues.Journal of medicinal chemistry, , Mar-13, Volume: 46, Issue:6, 2003
Synthesis and pharmacological characterization of novel analogues of the nicotinic acetylcholine receptor agonist (+/-)-UB-165.Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 2002
Synthesis and nicotinic acetylcholine receptor binding properties of exo-2-(2'-fluoro-5'-pyridinyl)-7-azabicyclo-[2.2.1]heptane: a new positron emission tomography ligand for nicotinic receptors.Journal of medicinal chemistry, , Jul-18, Volume: 40, Issue:15, 1997
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors.Journal of medicinal chemistry, , Feb-16, Volume: 39, Issue:4, 1996
Novel α3β4 nicotinic acetylcholine receptor-selective ligands. Discovery, structure-activity studies, and pharmacological evaluation.Journal of medicinal chemistry, , Nov-25, Volume: 53, Issue:22, 2010
Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity.Journal of medicinal chemistry, , May-04, Volume: 49, Issue:9, 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
Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.Bioorganic & medicinal chemistry letters, , Apr-19, Volume: 14, Issue:8, 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
Synthesis and Pharmacological Evaluation of DHβE Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists.ACS medicinal chemistry letters, , Jul-10, Volume: 5, Issue:7, 2014
Isolation, structure elucidation, and biological evaluation of 15-amido-3-demethoxy-2alpha,3alpha-methylenedioxyerythroculine, a new alkaloid from Hyperbaena valida.Journal of natural products, , Volume: 69, Issue:10, 2006
Tying up Nicotine: New Selective Competitive Antagonist of the Neuronal Nicotinic Acetylcholine Receptors.ACS medicinal chemistry letters, , Apr-09, Volume: 6, Issue:4, 2015
Conformationally restrained carbamoylcholine homologues. Synthesis, pharmacology at neuronal nicotinic acetylcholine receptors and biostructural considerations.European journal of medicinal chemistry, , Sep-18, Volume: 102, 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
Synthesis, pharmacology, and biostructural characterization of novel α4β2 nicotinic acetylcholine receptor agonists.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 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
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
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
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
Novel α3β4 nicotinic acetylcholine receptor-selective ligands. Discovery, structure-activity studies, and pharmacological evaluation.Journal of medicinal chemistry, , Nov-25, Volume: 53, Issue:22, 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
Synthesis and biological evaluation of novel carbon-11 labeled pyridyl ethers: candidate ligands for in vivo imaging of alpha4beta2 nicotinic acetylcholine receptors (alpha4beta2-nAChRs) in the brain with positron emission tomography.Bioorganic & medicinal chemistry, , Jul-01, Volume: 17, Issue:13, 2009
Novel acetylcholine and carbamoylcholine analogues: development of a functionally selective alpha4beta2 nicotinic acetylcholine receptor agonist.Journal of medicinal chemistry, , Dec-11, Volume: 51, Issue:23, 2008
Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor.Journal of medicinal chemistry, , Sep-20, Volume: 50, Issue:19, 2007
Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity.Journal of medicinal chemistry, , May-04, Volume: 49, Issue:9, 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
Epibatidine analogues as selective ligands for the alpha(x)beta2-containing subtypes of nicotinic acetylcholine receptors.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 15, Issue:19, 2005
The characterization of a novel rigid nicotine analog with alpha7-selective nAChR agonist activity and modulation of agonist properties by boron inclusion.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 15, Issue:17, 2005
Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.Bioorganic & medicinal chemistry letters, , Apr-19, Volume: 14, Issue:8, 2004
Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors.Bioorganic & medicinal chemistry letters, , Apr-19, Volume: 14, Issue:8, 2004
Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues.Journal of medicinal chemistry, , Mar-13, Volume: 46, Issue:6, 2003
Neuronal nicotinic acetylcholine receptor binding affinities of boron-containing nicotine analogues.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
Synthesis and nicotinic acetylcholine receptor binding properties of exo-2-(2'-fluoro-5'-pyridinyl)-7-azabicyclo-[2.2.1]heptane: a new positron emission tomography ligand for nicotinic receptors.Journal of medicinal chemistry, , Jul-18, Volume: 40, Issue:15, 1997
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors.Journal of medicinal chemistry, , Feb-16, Volume: 39, Issue:4, 1996
(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
Synthesis and evaluation of nicotine analogs as neuronal nicotinic acetylcholine receptor ligands.Journal of medicinal chemistry, , Oct-14, Volume: 37, Issue:21, 1994
Synthesis and biological characterization of pyridohomotropanes. Structure-activity relationships of conformationally restricted nicotinoids.Journal of medicinal chemistry, , Volume: 31, Issue:3, 1988
Structure-activity relationships of some pyridine, piperidine, and pyrrolidine analogues for enhancing and inhibiting the binding of (+/-)-[3H]nicotine to the rat brain P2 preparation.Journal of medicinal chemistry, , Volume: 28, Issue:9, 1985
Ligand selectivity for the acetylcholine binding site of the rat alpha4beta2 and alpha3beta4 nicotinic subtypes investigated by molecular docking.Journal of medicinal chemistry, , Aug-11, Volume: 48, Issue:16, 2005
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted pyridinyl)-7-deschloroepibatidine analogues.Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
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
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 pharmacological characterization of novel analogues of the nicotinic acetylcholine receptor agonist (+/-)-UB-165.Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 2002
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Synthesis and biological characterization of pyridohomotropanes. Structure-activity relationships of conformationally restricted nicotinoids.Journal of medicinal chemistry, , Volume: 31, Issue:3, 1988
Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.Bioorganic & medicinal chemistry letters, , Apr-19, Volume: 14, Issue:8, 2004
Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors.Journal of medicinal chemistry, , Feb-16, Volume: 39, Issue:4, 1996
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
Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors.Journal of medicinal chemistry, , Feb-16, Volume: 39, Issue:4, 1996
Ligand selectivity for the acetylcholine binding site of the rat alpha4beta2 and alpha3beta4 nicotinic subtypes investigated by molecular docking.Journal of medicinal chemistry, , Aug-11, Volume: 48, Issue:16, 2005
Epibatidine structure-activity relationships.Bioorganic & medicinal chemistry letters, , Apr-19, Volume: 14, Issue:8, 2004
Dual Nicotinic Acetylcholine Receptor α4β2 Antagonists/α7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts.Journal of medicinal chemistry, , 02-22, Volume: 61, Issue:4, 2018
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
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 relationship studies of SEN12333 analogues: determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs.European journal of medicinal chemistry, , May-05, Volume: 95, 2015
Investigations of amide bond variation and biaryl modification in analogues of α7 nAChR agonist SEN12333.European journal of medicinal chemistry, , Sep-12, Volume: 84, 2014
Consequences of linker length alteration of the α7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 22, Issue:7, 2012