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nicotinic acetylcholine receptor α9 subunit

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Target not currently curated in GtoImmuPdb

Target id: 469

Nomenclature: nicotinic acetylcholine receptor α9 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 4 479 4p14 CHRNA9 cholinergic receptor nicotinic alpha 9 subunit 5
Mouse 4 479 5 C3.1 Chrna9 cholinergic receptor, nicotinic, alpha polypeptide 9
Rat 4 479 14p11 Chrna9 cholinergic receptor nicotinic alpha 9 subunit 1
Previous and Unofficial Names Click here for help
NACHRA9 | NACHR alpha 9 | nicotinic acetylcholine receptor subunit alpha-9 | Acra9 | cholinergic receptor, nicotinic, alpha 9 (neuronal) | cholinergic receptor, nicotinic alpha 9 | cholinergic receptor
Database Links Click here for help
Alphafold Q9UGM1 (Hs), P43144 (Rn)
CATH/Gene3D 2.70.170.10
ChEMBL Target CHEMBL2184 (Hs), CHEMBL2585 (Rn)
Ensembl Gene ENSG00000174343 (Hs), ENSMUSG00000029205 (Mm), ENSRNOG00000002484 (Rn)
Entrez Gene 55584 (Hs), 231252 (Mm), 65024 (Rn)
Human Protein Atlas ENSG00000174343 (Hs)
KEGG Gene hsa:55584 (Hs), mmu:231252 (Mm), rno:65024 (Rn)
OMIM 605116 (Hs)
Pharos Q9UGM1 (Hs)
RefSeq Nucleotide NM_017581 (Hs), NM_001081104 (Mm), NM_022930 (Rn)
RefSeq Protein NP_060051 (Hs), NP_001074573 (Mm), NP_075219 (Rn)
SynPHARM 9251 (in complex with [3H]methyllycaconitine)
UniProtKB Q9UGM1 (Hs), P43144 (Rn)
Wikipedia CHRNA9 (Hs)
Functional Characteristics Click here for help
(α9)5: PCa/PNa = 9; α9α10: PCa/PNa = 9, Pf = 22%
Natural/Endogenous Ligands Click here for help
acetylcholine
Commonly used antagonists (Human)
(α9)5: α-bungarotoxin > methyllycaconitine > strychnine ~ tropisetron > tubocurarine; α9α10: α-bungarotoxin > tropisetron = strychnine > tubocurarine

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

Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]methyllycaconitine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Antagonist 8.1 pKd
⤷ pKd 8.1 (Kd 7.5x10-9 M) α9α10
RgIA4 Peptide Click here for species-specific activity table Rn Antagonist 9.1 pIC50 6
⤷ pIC50 9.1 (IC50 9x10-10 M) α9α10 [6]
RgIA4 Peptide Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.8 pIC50 6
⤷ pIC50 8.8 (IC50 1.5x10-9 M) α9α10 [6]
strychnine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist - -
⤷ α9α10
(α9)5
nicotine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist - -
⤷ α9α10
(α9)5
α-bungarotoxin Peptide Click here for species-specific activity table Hs Antagonist - -
⤷ (α9)5
α9α10
[125I]α-bungarotoxin Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist - -
⤷
[3H]α-bungarotoxin Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist - -
⤷
muscarine Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
⤷ α9α10
(α9)5
α-conotoxin RgIA Peptide Click here for species-specific activity table Hs Antagonist - -
⤷ α9α10
View species-specific antagonist tables
Tissue Distribution Click here for help
Pituitary gland, keratinocytes
Species:  Human
Technique:  RT-PCR
References:  7
Olfactory epithelia
Species:  Mouse
Technique:  RT-PCR
References:  8
Pituitary gland, nasal epithelium, tongue, cochlea:-
mRNA has been detected by in situ hybridization in the pars tiberalis region of the pituitary gland, the nasal epithelium and tongue. In contrast, no evidence for expression in the central nervous system was detected. By means of of RT-PCR and, subsequently, by in situ hybridization, expression has been confirmed in the cochlea.
Species:  Rat
Technique:  In situ hybridisation, RT-PCR
References:  1,3
Dorsal root ganglion neurons
Species:  Rat
Technique:  In situ hybridisation, RT-PCR
References:  2
Physiological Consequences of Altering Gene Expression Click here for help
Knockout mice have altered development and function of efferent innervation in the outer hair cells of the cochlear.
Species:  Mouse
Tissue:  Cochlear
Technique:  Knockout
References:  4,8

References

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1. Elgoyhen AB, Johnson DS, Boulter J, Vetter DE, Heinemann S. (1994) Alpha 9: an acetylcholine receptor with novel pharmacological properties expressed in rat cochlear hair cells. Cell, 79 (4): 705-15. [PMID:7954834]

2. Lips KS, Pfeil U, Kummer W. (2002) Coexpression of alpha 9 and alpha 10 nicotinic acetylcholine receptors in rat dorsal root ganglion neurons. Neuroscience, 115 (1): 1-5. [PMID:12401316]

3. Morley BJ, Li HS, Hiel H, Drescher DG, Elgoyhen AB. (1998) Identification of the subunits of the nicotinic cholinergic receptors in the rat cochlea using RT-PCR and in situ hybridization. Brain Res Mol Brain Res, 53 (1-2): 78-87. [PMID:9473597]

4. Murthy V, Taranda J, Elgoyhen AB, Vetter DE. (2009) Activity of nAChRs containing alpha9 subunits modulates synapse stabilization via bidirectional signaling programs. Dev Neurobiol, 69 (14): 931-49. [PMID:19790106]

5. Nguyen VT, Ndoye A, Grando SA. (2000) Novel human alpha9 acetylcholine receptor regulating keratinocyte adhesion is targeted by Pemphigus vulgaris autoimmunity. Am J Pathol, 157 (4): 1377-91. [PMID:11021840]

6. Romero HK, Christensen SB, Di Cesare Mannelli L, Gajewiak J, Ramachandra R, Elmslie KS, Vetter DE, Ghelardini C, Iadonato SP, Mercado JL et al.. (2017) Inhibition of α9α10 nicotinic acetylcholine receptors prevents chemotherapy-induced neuropathic pain. Proc Natl Acad Sci USA, 114 (10): E1825-E1832. [PMID:28223528]

7. Sgard F, Charpantier E, Bertrand S, Walker N, Caput D, Graham D, Bertrand D, Besnard F. (2002) A novel human nicotinic receptor subunit, alpha10, that confers functionality to the alpha9-subunit. Mol Pharmacol, 61 (1): 150-9. [PMID:11752216]

8. Vetter DE, Liberman MC, Mann J, Barhanin J, Boulter J, Brown MC, Saffiote-Kolman J, Heinemann SF, Elgoyhen AB. (1999) Role of alpha9 nicotinic ACh receptor subunits in the development and function of cochlear efferent innervation. Neuron, 23 (1): 93-103. [PMID:10402196]

Contributors

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