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nicotinic acetylcholine receptor α7 subunit

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 468

Nomenclature: nicotinic acetylcholine receptor α7 subunit

Family: Nicotinic acetylcholine receptors (nACh)

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 4 502 15q13.3 CHRNA7 cholinergic receptor nicotinic alpha 7 subunit 11
Mouse 4 502 7 34.47 cM Chrna7 cholinergic receptor, nicotinic, alpha polypeptide 7 43
Rat 4 502 1q22 Chrna7 cholinergic receptor nicotinic alpha 7 subunit 49
Previous and Unofficial Names Click here for help
nAChRa7 | NARAD | neuronal acetylcholine receptor subunit alpha-7 | Acra7 | cholinergic receptor, nicotinic, alpha 7 (neuronal) | cholinergic receptor, nicotinic alpha 7 | cholinergic receptor
Database Links Click here for help
Alphafold P36544 (Hs), P49582 (Mm), Q05941 (Rn)
CATH/Gene3D 2.70.170.10
ChEMBL Target CHEMBL2492 (Hs), CHEMBL3365 (Mm), CHEMBL4980 (Rn)
DrugBank Target P36544 (Hs)
Ensembl Gene ENSG00000175344 (Hs), ENSMUSG00000030525 (Mm), ENSRNOG00000010853 (Rn)
Entrez Gene 1139 (Hs), 11441 (Mm), 25302 (Rn)
Human Protein Atlas ENSG00000175344 (Hs)
KEGG Gene hsa:1139 (Hs), mmu:11441 (Mm), rno:25302 (Rn)
OMIM 118511 (Hs)
Orphanet ORPHA264663 (Hs)
Pharos P36544 (Hs)
RefSeq Nucleotide NM_000746 (Hs), NM_007390 (Mm), NM_012832 (Rn)
RefSeq Protein NP_000737 (Hs), NP_031416 (Mm), NP_036964 (Rn)
UniProtKB P36544 (Hs), P49582 (Mm), Q05941 (Rn)
Wikipedia CHRNA7 (Hs)
Functional Characteristics Click here for help
PCa/PNa = 6.6-20, Pf = 8.8 - 11.4%
Natural/Endogenous Ligands Click here for help
acetylcholine
Commonly used antagonists (Human)
(α7)5: DHβE (IC50 = 8 - 20 μM); (α7)5: tubocurarine (IC50 = 3.1 μM)

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]epibatidine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 12.2 pKd
⤷ pKd 12.2 (Kd 6x10-13 M) (α7)5
[3H]A-585539 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Full agonist 10.1 pKd 2
⤷ pKd 10.1 (Kd 7x10-11 M) native α7 [2]
[3H]AZ11637326 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Full agonist 9.6 pKd 21
⤷ pKd 9.6 (Kd 2.3x10-10 M) (α7)5 [21]
NS6740 Small molecule or natural product Immunopharmacology Ligand Rn - 9.0 pKi 6
⤷ pKi 9.0 (Ki 1.1x10-9 M) [6]
Description: Binding affinity to rat brain α7 nAChR, measured by displacement of the α7-selective agonist [3H]A-585539.
AZD0328 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Full agonist 8.5 pKi 39
⤷ pKi 8.5 (Ki 3x10-9 M) [39]
encenicline Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Partial agonist 8.4 pKi 39-40
⤷ pKi 8.4 (Ki 4.3x10-9 M) [39-40]
AQW051 Small molecule or natural product Hs Agonist 7.6 pKi 28
⤷ pKi 7.6 (Ki 2.7x10-8 M) [125I]α- bungarotoxin binding assay [28]
GTS-21 Small molecule or natural product Ligand has a PDB structure Rn Agonist 6.7 pKi 50
⤷ pKi 6.7 (Ki 2.2x10-7 M) [50]
Description: Inhibition of [125I]alpha-bungarotoxin binding to rat α nAChR
4OH-GTS-21 Small molecule or natural product Ligand has a PDB structure Rn Agonist 6.4 pKi 30
⤷ pKi 6.4 (Ki 4.2x10-7 M) [30]
Description: Displacement of [3H]-methyllycaconitine from rat α7 nAChR in hippocampal membranes by liquid scintillation counting
PSAB-OFP Small molecule or natural product Hs Full agonist 5.7 pEC50 7
⤷ pEC50 5.7 (EC50 2.2x10-6 M) [7]
4BP-TQS Small molecule or natural product Hs Full agonist - - 20
⤷ allosteric [20]
bradanicline Small molecule or natural product Hs Full agonist - - 25
⤷ (α7)5 [25]
PNU-282987 Small molecule or natural product Hs Full agonist - - 5
⤷ (α7)5 [5]
A-582941 Small molecule or natural product Hs Full agonist - - 4
⤷ (α7)5 [4]
PHA-709829 Small molecule or natural product Hs Full agonist - - 1
⤷ (α7)5 [1]
PHA-543613 Small molecule or natural product Hs Full agonist - - 54
⤷ (α7)5 [54]
View species-specific agonist tables
Agonist Comments
EVP-6124 shows selectivity for α7 nAChRs and does not activate or inhibit heteromeric α4β2 nAChRs [45].
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I]α-bungarotoxin Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 8.3 – 9.1 pKd
⤷ pKd 8.3 – 9.1 (Kd 5x10-9 – 7x10-10 M) (α7)5
[3H]α-bungarotoxin Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 8.3 – 9.1 pKd
⤷ pKd 8.3 – 9.1 (Kd 5x10-9 – 7x10-10 M) (α7)5
[3H]methyllycaconitine Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure Rn Antagonist 8.7 pKd
⤷ pKd 8.7 (Kd 1.9x10-9 M) native α7*
atracurium Small molecule or natural product Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 7.9 – 8.3 pIC50 29
⤷ pIC50 7.9 – 8.3 (IC50 1.3x10-8 – 5.6x10-9 M) [29]
Description: Antagonism of ACh activation of human α7 nACh receptors expressed in Xenopus oocytes, at different ACh concentrations.
α-bungarotoxin Peptide Click here for species-specific activity table Hs Antagonist - -
⤷ (α7)5
α-conotoxin ImI Peptide Hs Antagonist - -
⤷ (α7)5
methyllycaconitine Small molecule or natural product Ligand has a PDB structure Hs Antagonist - -
⤷ (α7)5
α-conotoxin ArIB Peptide Hs Antagonist - -
⤷ (α7)5
View species-specific antagonist tables
Channel Blockers
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Use-dependent Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
mecamylamine Small molecule or natural product Approved drug Click here for species-specific activity table Hs - no 4.8 pIC50 - no
⤷ pIC50 4.8 (IC50 1.56x10-5 M) (α7)5
Not voltage dependent
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
BNC375 Small molecule or natural product Rn Positive 5.7 pEC50 - no 24
⤷ pEC50 5.7 (EC50 1.9x10-6 M) [24]
Not voltage dependent
BNC375 Small molecule or natural product Hs Positive 5.6 pEC50 - no 53
⤷ pEC50 5.6 (EC50 2.64x10-6 M) [53]
Not voltage dependent
ivermectin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Positive 5.1 pEC50 - no 31
⤷ pEC50 5.1 (EC50 9x10-6 M) [31]
Not voltage dependent
JNJ1930942 Small molecule or natural product Hs Positive - - - no 13
⤷ (α7)5:Type 1/2 [13]
Not voltage dependent
A-867744 Small molecule or natural product Click here for species-specific activity table Hs Positive - - - no 36
⤷ (α7)5:Type 2; also blocks α3β4 and α4β2 [36]
Not voltage dependent
PNU-120596 Small molecule or natural product Ligand has a PDB structure Hs Positive - - - no 27
⤷ (α7)5:Type 2 [27]
Not voltage dependent
LY2087101 Small molecule or natural product Click here for species-specific activity table Hs Positive - - - no 8
⤷ (α7)5:Type 1 [8]
Not voltage dependent
NS1738 Small molecule or natural product Click here for species-specific activity table Hs Positive - - - no 51
⤷ (α7)5:Type 1; also blocks α3β4 and α4β2 [51]
Not voltage dependent
View species-specific allosteric modulator tables
Immunopharmacology Comments
Included in Guide to Immunopharmacology as CHRNA7 knockout aggravates rheumatoid arthritis in mice [52].
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
Immuno Process:  Immune regulation
Immuno Process:  Antigen presentation
Immuno Process:  B cell (activation)
Immuno Process:  Cellular signalling
Immuno Process:  Inflammation
Immuno Process:  T cell (activation)
Tissue Distribution Click here for help
Brain:-
High levels of α7 mRNA are expressed in the dentate granular layer and CA2/CA3 region of the hippocampus, in the caudate nucleus, and in the pulvinar and ventroposterolateral nuclei of the thalamus. [125I]α-bungarotoxin binding is very high in the hippocampus and in the pyramidal cells of the CA1 region, but is relatively low in the subicular complex.
Expression level:  High
Species:  Human
Technique:  in situ hybridisation, Radioligand binding.
References:  47
Brain:-
Expression in mouse brain is similar to that reported in rat, with strong expression in the hippocampus, amygdala, several hypothalamic nuclei, cerebral cortex, lateral areas of the interpeduncular nucleus, medial habenula and inferior colliculus. In contrast to rat brain, significant labeling of caudate putamen was observed.
Expression level:  High
Species:  Mouse
Technique:  in situ hybridisation
References:  37
Brain:-
The regional distribution of [125I]α-bungarotoxin binding is similar to that in rat brain. However, unlike in rat brain there is a significant signal in the olfactory tubercle, the nucleus accumbens and the caudate putamen. The binding sites for [125I]α-bungarotoxin are eliminated from all brain areas in α7 knockout mice.
Species:  Mouse
Technique:  Radioligand binding.
References:  42,44
Brain:-
High levels of α7 subunit mRNA are expressed in hippocampal cell layers, superficial and deep layers of the cerebral cortex, several hypothalamic nuclei, olfactory cortex, inferior colliculus and medial septum. Expression also occurs in the inferior colliculus, medial habenula and interpeduncular nucleus.
Species:  Rat
Technique:  in situ hybridisation
References:  49
Brain:-
High levels of [125I]α-bungarotoxin binding are detected in the accessory olfactory bulb, deep cortical layers, thehippocampus (particularly the stratum oriens, and the dentate and CA3 regions), the amygdala, hypothalamic nuclei, the subthalamic nucleus, the ventrolateral geniculate nucleus, the superior and inferior colliculus, and several pontine nuclei. Very little specific labeling is observed in the nucleus accumbens, caudate putamen and most thalamic nuclei
Expression level:  High
Species:  Rat
Technique:  Radioligand binding.
References:  3,14,26,48
Tissue Distribution Comments
For expression profiles in other primates see:-
Cynomologous monkey [12], Rhesus monkey [22-23,33], Macaca cynomologous Monkey[32], and Squirrel monkey [46]
Physiological Consequences of Altering Gene Expression Click here for help
Knockout mice have been reported to have reduced cognitive deficits in a model of Alzheimer's disease.
Species:  Mouse
Tissue:  in vivo
Technique:  Knockout
References:  15
Knockout mice have been reported to have an increased incidence and severity of rheumatoid arthritis.
Species:  Mouse
Tissue:  in vivo
Technique:  Knockout
References:  52
Mice expressing α7 containing the L247T mutation in the second transmembrane domain die within a day of birth. Extensive apoptosis is observed in these mutant mice. Heterozygotes are viable but are more sensitive to nicotine-induced seizures.
Species:  Mouse
Tissue:  in vivo
Technique:  Transgensis
References:  9,41
Impaired passive avoidance learning is observed in mice lacking both the α7 and β2 subunits.
Species:  Mouse
Tissue:  in vivo
Technique:  Knockout
References:  38
Knockout mice are viable and anatomically normal but lack high-affinity α-bungarotoxin binding sites in the brain and lack rapidly desensitizing nicotinic currents in hippocampal neurons. Other effects that have been reported include: reduced neuroprotective effects of nicotine in hippocampal neurons and reduced maturation and integration of adult-born neurons in the hippocampus; cognitive deficits; impaired attention and spatial learning.
Species:  Mouse
Tissue:  in vivo
Technique:  Knockout
References:  10,16-17,35,41,55
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Chromosome 15q13.3 deletion syndrome
Synonyms: 15q13.3 microdeletion syndrome [Orphanet: ORPHA199318]
Chromosome 15q13.3 microdeletion syndrome
OMIM: 612001
Orphanet: ORPHA199318
Disease:  Schizophrenia 13; SCZD13
Synonyms: Schizophrenia [Orphanet: ORPHA3140] [OMIM: 181500] [Disease Ontology: DOID:5419]
Disease Ontology: DOID:5419
OMIM: 181500, 613025
Orphanet: ORPHA3140
Role:  There is linkage between the α7 gene locus on chromosome 15 and auditory gating deficits common in schizophrenic patients. Polymorphisms in the promoter region of the α7 gene that reduce its transcription appear to be associated with schizophrenia. Brains of schizophrenics have reduced levels of α-bungarotoxin binding sites.
References:  18,34
Click column headers to sort
Type Species Amino acid change Nucleotide change Description Reference
Partial gene duplication Human - Chromosome 15 19
Polymorphism Human - Promoter 34
Gene Expression and Pathophysiology Click here for help
Decrease
Tissue or cell type:  Brain
Pathophysiology:  Schizophrenia
Species:  Human
Technique:  Post-mortem radioligand binding
References:  18

References

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1. Acker BA, Jacobsen EJ, Rogers BN, Wishka DG, Reitz SC, Piotrowski DW, Myers JK, Wolfe ML, Groppi VE, Thornburgh BA et al.. (2008) Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the alpha7 nicotinic acetylcholine receptor: in vitro and in vivo activity. Bioorg Med Chem Lett, 18 (12): 3611-5. [PMID:18490160]

2. Anderson DJ, Bunnelle W, Surber B, Du J, Surowy C, Tribollet E, Marguerat A, Bertrand D, Gopalakrishnan M. (2008) [3H]A-585539 [(1S,4S)-2,2-dimethyl-5-(6-phenylpyridazin-3-yl)-5-aza-2-azoniabicyclo[2.2.1]heptane], a novel high-affinity alpha7 neuronal nicotinic receptor agonist: radioligand binding characterization to rat and human brain. J Pharmacol Exp Ther, 324 (1): 179-87. [PMID:17959745]

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6. Briggs CA, Grønlien JH, Curzon P, Timmermann DB, Ween H, Thorin-Hagene K, Kerr P, Anderson DJ, Malysz J, Dyhring T et al.. (2009) Role of channel activation in cognitive enhancement mediated by alpha7 nicotinic acetylcholine receptors. Br J Pharmacol, 158 (6): 1486-94. [PMID:19845675]

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9. Broide RS, Salas R, Ji D, Paylor R, Patrick JW, Dani JA, De Biasi M. (2002) Increased sensitivity to nicotine-induced seizures in mice expressing the L250T alpha 7 nicotinic acetylcholine receptor mutation. Mol Pharmacol, 61 (3): 695-705. [PMID:11854451]

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12. Cimino M, Marini P, Fornasari D, Cattabeni F, Clementi F. (1992) Distribution of nicotinic receptors in cynomolgus monkey brain and ganglia: localization of alpha 3 subunit mRNA, alpha-bungarotoxin and nicotine binding sites. Neuroscience, 51 (1): 77-86. [PMID:1465189]

13. Dinklo T, Shaban H, Thuring JW, Lavreysen H, Stevens KE, Zheng L, Mackie C, Grantham C, Vandenberk I, Meulders G et al.. (2011) Characterization of 2-[[4-fluoro-3-(trifluoromethyl)phenyl]amino]-4-(4-pyridinyl)-5-thiazolemethanol (JNJ-1930942), a novel positive allosteric modulator of the {alpha}7 nicotinic acetylcholine receptor. J Pharmacol Exp Ther, 336 (2): 560-74. [PMID:21084390]

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15. Dziewczapolski G, Glogowski CM, Masliah E, Heinemann SF. (2009) Deletion of the alpha 7 nicotinic acetylcholine receptor gene improves cognitive deficits and synaptic pathology in a mouse model of Alzheimer's disease. J Neurosci, 29 (27): 8805-15. [PMID:19587288]

16. Egea J, Rosa AO, Sobrado M, Gandía L, López MG, García AG. (2007) Neuroprotection afforded by nicotine against oxygen and glucose deprivation in hippocampal slices is lost in alpha7 nicotinic receptor knockout mice. Neuroscience, 145 (3): 866-72. [PMID:17291692]

17. Fernandes C, Hoyle E, Dempster E, Schalkwyk LC, Collier DA. (2006) Performance deficit of alpha7 nicotinic receptor knockout mice in a delayed matching-to-place task suggests a mild impairment of working/episodic-like memory. Genes Brain Behav, 5 (6): 433-40. [PMID:16923147]

18. Freedman R, Hall M, Adler LE, Leonard S. (1995) Evidence in postmortem brain tissue for decreased numbers of hippocampal nicotinic receptors in schizophrenia. Biol Psychiatry, 38 (1): 22-33. [PMID:7548469]

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24. Harvey AJ, Avery TD, Schaeffer L, Joseph C, Huff BC, Singh R, Morice C, Giethlen B, Grishin AA, Coles CJ et al.. (2019) Discovery of BNC375, a Potent, Selective, and Orally Available Type I Positive Allosteric Modulator of α7 nAChRs. ACS Med Chem Lett, 10 (5): 754-760. [PMID:31097995]

25. Hauser TA, Kucinski A, Jordan KG, Gatto GJ, Wersinger SR, Hesse RA, Stachowiak EK, Stachowiak MK, Papke RL, Lippiello PM et al.. (2009) TC-5619: an alpha7 neuronal nicotinic receptor-selective agonist that demonstrates efficacy in animal models of the positive and negative symptoms and cognitive dysfunction of schizophrenia. Biochem Pharmacol, 78 (7): 803-12. [PMID:19482012]

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29. Jonsson M, Gurley D, Dabrowski M, Larsson O, Johnson EC, Eriksson LI. (2006) Distinct pharmacologic properties of neuromuscular blocking agents on human neuronal nicotinic acetylcholine receptors: a possible explanation for the train-of-four fade. Anesthesiology, 105 (3): 521-33. [PMID:16931985]

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31. Krause RM, Buisson B, Bertrand S, Corringer PJ, Galzi JL, Changeux JP, Bertrand D. (1998) Ivermectin: a positive allosteric effector of the alpha7 neuronal nicotinic acetylcholine receptor. Mol Pharmacol, 53 (2): 283-94. [PMID:9463487]

32. Kulak JM, Carroll FI, Schneider JS. (2006) [125I]Iodomethyllycaconitine binds to alpha7 nicotinic acetylcholine receptors in monkey brain. Eur J Neurosci, 23 (10): 2604-10. [PMID:16817863]

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35. Levin ED, Petro A, Rezvani AH, Pollard N, Christopher NC, Strauss M, Avery J, Nicholson J, Rose JE. (2009) Nicotinic alpha7- or beta2-containing receptor knockout: effects on radial-arm maze learning and long-term nicotine consumption in mice. Behav Brain Res, 196 (2): 207-13. [PMID:18831991]

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38. Marubio LM, Paylor R. (2004) Impaired passive avoidance learning in mice lacking central neuronal nicotinic acetylcholine receptors. Neuroscience, 129 (3): 575-82. [PMID:15541879]

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40. No authors listed. (2004) Natalizumab: AN 100226, anti-4alpha integrin monoclonal antibody. Drugs R D, 5 (2): 102-7. [PMID:15293871]

41. Orr-Urtreger A, Broide RS, Kasten MR, Dang H, Dani JA, Beaudet AL, Patrick JW. (2000) Mice homozygous for the L250T mutation in the alpha7 nicotinic acetylcholine receptor show increased neuronal apoptosis and die within 1 day of birth. J Neurochem, 74 (5): 2154-66. [PMID:10800961]

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