DGIdb - CHRNA7 Gene Record

CHRNA7 1139 Druggable Genome

Alternate Names:

1139
CHOLINERGIC RECEPTOR NICOTINIC ALPHA 7 SUBUNIT
CHRNA7
CHRNA7-2
NACHRA7
118511
1960
ENSG00000175344
OTTHUMG00000129285
Neuronal acetylcholine receptor subunit alpha-7
BE0003438
Q693P7
P36544
ACHA7_HUMAN
BE0002341
1139; 89832
468
nicotinic acetylcholine receptor α7 subunit
NEURONAL ACETYLCHOLINE RECEPTOR PROTEIN, ALPHA-7 SUBUNIT PRECURSOR. [SOURCE:UNIPROT/SWISSPROT;ACC:P36544]
PA114
Neuronal acetylcholine receptor alpha-7
T34429
NM_000746
NP_000737

Gene Info:

Interpro Acc	IPR006202
Human Readable Name	ION CHANNEL
Human Readable Name	DRUGGABLE GENOME
Interpro Acc	IPR006201
Uniprot Status	Swiss-Prot
Interpro Name	Neurotransmitter-gated ion-channel
Interpro Type	Domain
Interpro Type	Family
Interpro Short Name	Neur_chan_lig-bd
Interpro Name	Neurotransmitter-gated ion-channel ligand-binding
Interpro Short Name	Neur_channel
Uniprot Evidence	1: Evidence at protein level
Target Class	Receptors
Target Subclass	TC:1.A.9.1.1
Target Subclass	Channels
Target Subclass	cys-loop
Target Subclass	Ligand_gated_ion_channels
Target Main Class	Receptors
Transmembrane Helix Count	4
Gene Biotype	PROTEIN_CODING
GuideToPharmacology Gene Category Name	Nicotinic acetylcholine receptors
GuideToPharmacology Gene Category ID	76

(11 More Sources)

Gene Categories: Category Details

ION CHANNEL
DRUGGABLE GENOME

Publications:

Arias et al., 2005, Anesthetics as chemical tools to study the structure and function of nicotinic acetylcholine receptors., Curr. Protein Pept. Sci.
Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.
Krasowski et al., 1999, General anaesthetic actions on ligand-gated ion channels., Cell. Mol. Life Sci.
Mansvelder et al., 2009, Nicotinic modulation of synaptic transmission and plasticity in cortico-limbic circuits., Semin. Cell Dev. Biol.
Zaniewska et al., Nicotine dependence - human and animal studies, current pharmacotherapies and future perspectives., Pharmacol Rep
Mexal et al., 2007, alpha7 nicotinic receptor gene promoter polymorphisms in inbred mice affect expression in a cell type-specific fashion., J. Biol. Chem.
Narahashi et al., 2000, Symposium overview: mechanism of action of nicotine on neuronal acetylcholine receptors, from molecule to behavior., Toxicol. Sci.
Olincy et al., 2006, Proof-of-concept trial of an alpha7 nicotinic agonist in schizophrenia., Arch. Gen. Psychiatry
Jackson et al., 2010, Role of alpha5 nicotinic acetylcholine receptors in pharmacological and behavioral effects of nicotine in mice., J. Pharmacol. Exp. Ther.
Rigbi A et al., 2011, Why do young women smoke? VI. A controlled study of nicotine effects on attention: pharmacogenetic interactions., Pharmacogenomics J
Pavlov et al., 2007, Selective alpha7-nicotinic acetylcholine receptor agonist GTS-21 improves survival in murine endotoxemia and severe sepsis., Crit. Care Med.
Stokes et al., 2004, The structural basis for GTS-21 selectivity between human and rat nicotinic alpha7 receptors., Mol. Pharmacol.
Kim et al., 2007, Synthesis and positron emission tomography studies of C-11-labeled isotopomers and metabolites of GTS-21, a partial alpha7 nicotinic cholinergic agonist drug., Nucl. Med. Biol.
Barbier AJ et al., 2015, Pharmacodynamics, pharmacokinetics, safety, and tolerability of encenicline, a selective α7 nicotinic receptor partial agonist, in single ascending-dose and bioavailability studies., Clin Ther
Braga IL et al., 2015, Effect of APOE and CHRNA7 genotypes on the cognitive response to cholinesterase inhibitor treatment at different stages of Alzheimer's disease., Am J Alzheimers Dis Other Demen
Ng HJ et al., 2007, Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators., Proc Natl Acad Sci U S A
Olin et al., 2002, Galantamine for Alzheimer's disease., Cochrane Database Syst Rev
Woodruff-Pak et al., 2002, Nicotinic cholinergic modulation: galantamine as a prototype., CNS Drug Rev
Lilienfeld, 2002, Galantamine--a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer's disease., CNS Drug Rev
Scott et al., 2000, Galantamine: a review of its use in Alzheimer's disease., Drugs
Lilienfeld et al., 2000, Galantamine: additional benefits to patients with Alzheimer's disease., Dement Geriatr Cogn Disord
Hansen et al.
Ludwig J et al., 2010, Localization by site-directed mutagenesis of a galantamine binding site on α7 nicotinic acetylcholine receptor extracellular domain., J Recept Signal Transduct Res
Woodruff-Pak DS et al., 2001, Galantamine: effect on nicotinic receptor binding, acetylcholinesterase inhibition, and learning., Proc Natl Acad Sci U S A
Walker et al., 2014, Cytisine versus nicotine for smoking cessation., N. Engl. J. Med.
Houlihan et al., 2001, Activity of cytisine and its brominated isosteres on recombinant human alpha7, alpha4beta2 and alpha4beta4 nicotinic acetylcholine receptors., J. Neurochem.
Mihalak et al., 2006, Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors., Mol. Pharmacol.
Pagán et al., 2001, Cembranoid and long-chain alkanol sites on the nicotinic acetylcholine receptor and their allosteric interaction., Biochemistry
Damaj et al., 2005, Effect of dextrometorphan and dextrorphan on nicotine and neuronal nicotinic receptors: in vitro and in vivo selectivity., J. Pharmacol. Exp. Ther.
Briggs CA et al., 1999, Gain of function mutation of the alpha7 nicotinic receptor: distinct pharmacology of the human alpha7V274T variant., Eur J Pharmacol
Bréthous L et al., 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)., J Med Chem
Dopico et al., 2009, Acute alcohol action and desensitization of ligand-gated ion channels., Pharmacol. Rev.
Hendrickson et al., 2013, Neuronal nicotinic acetylcholine receptors: common molecular substrates of nicotine and alcohol dependence., Front Psychiatry
Shiraishi et al., 2002, Inhibitory effects of tramadol on nicotinic acetylcholine receptors in adrenal chromaffin cells and in Xenopus oocytes expressing alpha 7 receptors., Br. J. Pharmacol.
Barakat A, 2019, Revisiting Tramadol: A Multi-Modal Agent for Pain Management., CNS Drugs
Rogers et al., 1992, Detection of nicotinic receptor ligands with a light addressable potentiometric sensor., Anal. Biochem.
Fiacchino et al., 1990, Abnormal responses to succinylcholine and pancuronium in a patient with hemiparesis., Ital J Neurol Sci
Marshall et al., 1990, The actions of suxamethonium (succinyldicholine) as an agonist and channel blocker at the nicotinic receptor of frog muscle., J. Physiol. (Lond.)
Aracava et al., 2005, Memantine blocks alpha7* nicotinic acetylcholine receptors more potently than n-methyl-D-aspartate receptors in rat hippocampal neurons., J. Pharmacol. Exp. Ther.
Pohanka M, 2012, Alpha7 nicotinic acetylcholine receptor is a target in pharmacology and toxicology., Int J Mol Sci
Maskell PD et al., 2003, Inhibition of human alpha 7 nicotinic acetylcholine receptors by open channel blockers of N-methyl-D-aspartate receptors., Br J Pharmacol
Niessen KV et al., 2011, Interaction of bispyridinium compounds with the orthosteric binding site of human α7 and Torpedo californica nicotinic acetylcholine receptors (nAChRs)., Toxicol Lett
Talka R et al., 2015, Methadone's effect on nAChRs--a link between methadone use and smoking?, Biochem Pharmacol
Talka R et al., 2015, Methadone is a non-competitive antagonist at the α4β2 and α3* nicotinic acetylcholine receptors and an agonist at the α7 nicotinic acetylcholine receptor., Basic Clin Pharmacol Toxicol
Ibeas Bih C et al., 2015, Molecular Targets of Cannabidiol in Neurological Disorders., Neurotherapeutics
Zhao L et al., 2003, Functional properties of homomeric, human alpha 7-nicotinic acetylcholine receptors heterologously expressed in the SH-EP1 human epithelial cell line., J Pharmacol Exp Ther
Matsubayashi H et al., 1997, Amantadine inhibits nicotinic acetylcholine receptor function in hippocampal neurons., J Pharmacol Exp Ther
Kohrs R et al., 1998, Ketamine: teaching an old drug new tricks., Anesth Analg
Briggs CA et al., 1998, Activation and inhibition of the human alpha7 nicotinic acetylcholine receptor by agonists., Neuropharmacology

ENCENICLINE CHRNA7

Interaction Score: 5.24

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name EVP-6124

Direct Interaction yes

PMIDs:
25438724

Sources:
DrugBank TdgClinicalTrial ChemblInteractions GuideToPharmacology TTD
GTS-21 CHRNA7

Interaction Score: 5.24

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name GTS-21

Novel drug target Established target

PMIDs:
17334244 15213292 17591554

Sources:
DrugBank TdgClinicalTrial TTD
SSR180711 CHRNA7

Interaction Score: 2.62

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit partial agonist

Direct Interaction yes

PMIDs:
22591063

Sources:
DTC ChemblInteractions
CHEMBL257591 CHRNA7

Interaction Score: 2.62

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Specific Action of the Ligand Positive

Details of Interaction (α7)5:Type 2

Endogenous Drug? False

PMIDs:
17470817

Sources:
DTC GuideToPharmacology

TC-6987 CHRNA7

Interaction Score: 2.62

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name TC-6987Êby Targacept forÊasthmaÊandÊtype II diabetes

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TTD

GALANTAMINE CHRNA7

Interaction Score: 1.92

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

PMIDs:
12137632 12481195 12177686 11129124 10971048 20480924 24951635 21062106 11172080

Sources:
DrugBank PharmGKB
ABT-126 CHRNA7

Interaction Score: 1.75

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
AQW051 CHRNA7

Interaction Score: 1.75

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit partial agonist

Specific Action of the Ligand Agonist

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology
JNJ-39393406 CHRNA7

Interaction Score: 1.75

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
AZD0328 CHRNA7

Interaction Score: 1.75

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist

Direct Interaction yes

Specific Action of the Ligand Full agonist

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology
AVL-3288 CHRNA7

Interaction Score: 1.75

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
PHA-543613 CHRNA7

Interaction Score: 1.75

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist

Direct Interaction yes

Specific Action of the Ligand Full agonist

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology
ABT-107 CHRNA7

Interaction Score: 0.87

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ND0801 CHRNA7

Interaction Score: 0.87

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
METHYLLYCACONITINE CHRNA7

Interaction Score: 0.87

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Details of Interaction (α7)5

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
CHEMBL526281 CHRNA7

Interaction Score: 0.87

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Details of Interaction (α7)5

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
APN1125 CHRNA7

Interaction Score: 0.87

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit partial agonist

PMIDs:
None found

Sources:
ChemblInteractions
BRADANICLINE CHRNA7

Interaction Score: 0.87

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist

Trial Name TC-5619

PMIDs:
None found

Sources:
DrugBank TdgClinicalTrial ChemblInteractions GuideToPharmacology
PNU-282987 CHRNA7

Interaction Score: 0.87

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Details of Interaction (α7)5

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
HEXOBARBITAL CHRNA7

Interaction Score: 0.52

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
16248797 11264449 10487207

Sources:
DrugBank TdgClinicalTrial TEND
BUTETHAL CHRNA7

Interaction Score: 0.52

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
16248797 11264449 10487207

Sources:
DrugBank TdgClinicalTrial TEND
CYTISINICLINE CHRNA7

Interaction Score: 0.5

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
25517706 11553677

Sources:
DrugBank TTD
SECOBARBITAL CHRNA7

Interaction Score: 0.48

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
16248797 11264449 10487207

Sources:
DrugBank TdgClinicalTrial TEND
LOBELINE CHRNA7

Interaction Score: 0.44

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9833639

Sources:
DrugBank
RIVASTIGMINE CHRNA7

Interaction Score: 0.44

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24951635

Sources:
PharmGKB
VARENICLINE CHRNA7

Interaction Score: 0.44

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name varenicline, CP-526

Novel drug target Established target

PMIDs:
16766716

Sources:
DrugBank TdgClinicalTrial TEND
THIOPENTAL CHRNA7

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
16248797 11264449 10487207

Sources:
DrugBank TdgClinicalTrial TEND
MEPHOBARBITAL CHRNA7

Interaction Score: 0.4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11264449 16248797 10487207

Sources:
DrugBank TdgClinicalTrial TEND
SUXAMETHONIUM CHRNA7

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
1621972 2272786 2133043

Sources:
DrugBank
APROBARBITAL CHRNA7

Interaction Score: 0.35

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
16248797 11264449 10487207

Sources:
DrugBank
MEMANTINE CHRNA7

Interaction Score: 0.35

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
15522999 22408449 14645141

Sources:
DrugBank
HEPTABARBITAL CHRNA7

Interaction Score: 0.35

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
16248797 11264449 10487207

Sources:
DrugBank
BARBITAL CHRNA7

Interaction Score: 0.35

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
16248797 11264449 10487207

Sources:
DrugBank
AMOBARBITAL CHRNA7

Interaction Score: 0.35

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
16248797 11264449 10487207

Sources:
DrugBank
RG3487 CHRNA7

Interaction Score: 0.29

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit partial agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
CHEMBL490153 CHRNA7

Interaction Score: 0.29

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Details of Interaction (α7)5:Type 2; also blocks α3β4 and α4β2

PMIDs:
None found

Sources:
GuideToPharmacology
METHARBITAL CHRNA7

Interaction Score: 0.26

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
16248797 11264449 10487207

Sources:
DrugBank TdgClinicalTrial TEND
BUTALBITAL CHRNA7

Interaction Score: 0.26

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
16248797 11264449 10487207

Sources:
DrugBank TdgClinicalTrial TEND
TALBUTAL CHRNA7

Interaction Score: 0.26

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
16248797 11264449 10487207

Sources:
DrugBank TdgClinicalTrial TEND
CHOLINE SALICYLATE CHRNA7

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12626641

Sources:
DrugBank
EPIBATIDINE CHRNA7

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21703337

Sources:
DrugBank
TENOCYCLIDINE CHRNA7

Interaction Score: 0.25

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
11551210

Sources:
DrugBank
BUTABARBITAL CHRNA7

Interaction Score: 0.24

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11264449 16248797 10487207

Sources:
TdgClinicalTrial TEND
MECAMYLAMINE CHRNA7

Interaction Score: 0.24

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Details of Interaction (α7)5

PMIDs:
10082212

Sources:
DrugBank GuideToPharmacology
PENTOBARBITAL CHRNA7

Interaction Score: 0.24

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
16248797 11264449 10487207

Sources:
DrugBank TdgClinicalTrial TEND
TUBOCURARINE CHRNA7

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10082212

Sources:
DrugBank
CHOLINE CHRNA7

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12626641

Sources:
DrugBank
ACETYLCHOLINE CHRNA7

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12626641

Sources:
DrugBank
NICOTINE CHRNA7

Interaction Score: 0.18

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
19560048 20081230 17360707 11006350 16754836 20400469 20231857

Sources:
DrugBank TdgClinicalTrial TEND PharmGKB
AMANTADINE CHRNA7

Interaction Score: 0.17

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
9152392

Sources:
DrugBank
IVERMECTIN CHRNA7

Interaction Score: 0.17

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Positive

PMIDs:
None found

Sources:
GuideToPharmacology

ATRACURIUM CHRNA7

Interaction Score: 0.17

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Details of the Assay for Interaction Antagonism of ACh activation of human α7 nACh receptors expressed in Xenopus oocytes, at different ACh concentrations.

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

ALCURONIUM CHRNA7

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PRIMIDONE CHRNA7

Interaction Score: 0.16

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
16248797 11264449 10487207

Sources:
DrugBank TdgClinicalTrial TEND
PHENOBARBITAL CHRNA7

Interaction Score: 0.14

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
16248797 11264449 10487207

Sources:
DrugBank TdgClinicalTrial TEND
DONEPEZIL CHRNA7

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24951635

Sources:
PharmGKB
ASM-024 CHRNA7

Interaction Score: 0.12

Interaction Types & Directionality:

modulator

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TRAMADOL CHRNA7

Interaction Score: 0.1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
12010769 31004280

Sources:
DrugBank
KETAMINE CHRNA7

Interaction Score: 0.09

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
9806706

Sources:
DrugBank
DEXTROMETHORPHAN CHRNA7

Interaction Score: 0.09

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
15356218

Sources:
DrugBank
METHADONE CHRNA7

Interaction Score: 0.08

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
26231941 25196810

Sources:
DrugBank
CANNABIDIOL CHRNA7

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26264914

Sources:
DrugBank
NABIXIMOLS CHRNA7

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26264914

Sources:
DrugBank
ZIPRASIDONE CHRNA7

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ALCOHOL CHRNA7

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19270242 23641218

Sources:
DrugBank

Ensembl: ENSG00000175344
- Version: 101_38
Alternate Names:

CHRNA7 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: P36544
- Version: 11-September-2012
Alternate Names:

ENSG00000175344 Ensembl Gene Id

P36544 Uniprot Accession

1139 Entrez Gene Id

Gene Info:

Interpro Acc IPR006202

Human Readable Name ION CHANNEL

Human Readable Name DRUGGABLE GENOME

Gene Categories:

ION CHANNEL, DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P36544
- Version: January-2014
Alternate Names:

CHRNA7 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass TC:1.A.9.1.1

Publications:
RussLampel: ENSG00000175344
- Version: 26-July-2011
Alternate Names:

NEURONAL ACETYLCHOLINE RECEPTOR PROTEIN, ALPHA-7 SUBUNIT PRECURSOR. [SOURCE:UNIPROT/SWISSPROT;ACC:P36544] Description

CHRNA7 Display Id

ENSG00000175344 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TEND: P36544
- Version: 01-August-2011
Alternate Names:

1139; 89832 Entrez Gene Id

ACHA7_HUMAN Uniprot Id

P36544 Uniprot Accession

Gene Info:

Target Subclass Channels

Target Subclass cys-loop

Target Subclass Ligand_gated_ion_channels

Publications:
GuideToPharmacology: 1139
- Version: 29-September-2020
Alternate Names:

1960 HUGO Gene ID

1960 HUGO Gene Symbol

cholinergic receptor nicotinic alpha 7 subunit HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Nicotinic acetylcholine receptors

GuideToPharmacology Gene Category ID 76

Gene Categories:

ION CHANNEL

Publications:

PharmGKB: CHRNA7

Version: 18-August-2020

Alternate Names:

PA114 PharmGKB ID

Gene Info:

Publications:

Braga IL et al., 2015, Effect of APOE and CHRNA7 genotypes on the cognitive response to cholinesterase inhibitor treatment at different stages of Alzheimer's disease., Am J Alzheimers Dis Other Demen

Rigbi A et al., 2011, Why do young women smoke? VI. A controlled study of nicotine effects on attention: pharmacogenetic interactions., Pharmacogenomics J

DrugBank: BE0003438

Version: 5.1.7

Alternate Names:

CHRNA7 DrugBank Gene Name

Q693P7 UniProt Accession

1139 Entrez Gene Id

Gene Info:

Publications:

Shiraishi et al., 2002, Inhibitory effects of tramadol on nicotinic acetylcholine receptors in adrenal chromaffin cells and in Xenopus oocytes expressing alpha 7 receptors., Br. J. Pharmacol.

Barakat A, 2019, Revisiting Tramadol: A Multi-Modal Agent for Pain Management., CNS Drugs

Marshall et al., 1990, The actions of suxamethonium (succinyldicholine) as an agonist and channel blocker at the nicotinic receptor of frog muscle., J. Physiol. (Lond.)

DrugBank: BE0002341

Version: 5.1.7

Alternate Names:

CHRNA7 DrugBank Gene Name

P36544 UniProt Accession

1139 Entrez Gene Id

Gene Info:

Publications:

Mexal et al., 2007, alpha7 nicotinic receptor gene promoter polymorphisms in inbred mice affect expression in a cell type-specific fashion., J. Biol. Chem.

Narahashi et al., 2000, Symposium overview: mechanism of action of nicotine on neuronal acetylcholine receptors, from molecule to behavior., Toxicol. Sci.

Mansvelder et al., 2009, Nicotinic modulation of synaptic transmission and plasticity in cortico-limbic circuits., Semin. Cell Dev. Biol.

DTC: CHRNA7

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Ng HJ et al., 2007, Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators., Proc Natl Acad Sci U S A

Bréthous L et al., 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)., J Med Chem

ChemblInteractions: NACHRA7
- Version: chembl_23
Alternate Names:

NACHRA7 GENE_SYMBOL

CHRNA7 GENE_SYMBOL

Neuronal acetylcholine receptor subunit alpha-7 UNIPROT

Gene Info:

Publications:
HingoraniCasas: ENSG00000175344
- Version: 31-May-2017
Alternate Names:

ENSG00000175344 Gene Symbol

CHRNA7 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
Pharos: CHRNA7
- Version: 03-September-2020
Alternate Names:

Neuronal acetylcholine receptor subunit alpha-7 Gene Name

P36544 UniProt ID

Gene Info:

Gene Categories:

ION CHANNEL

Publications:
GO: CHRNA7
- Version: 05-September-2020
Alternate Names:

NACHRA7 GO Gene Synonym

Gene Info:

Gene Categories:

ION CHANNEL

Publications:
TTD: Neuronal acetylcholine receptor alpha-7
- Version: 2020.06.01
Alternate Names:

CHRNA7 TTD Gene Abbreviation

T34429 TTD Target ID

Gene Info:

Publications:

Novel drug target	Established target
Trial Name	EVP-6124
Direct Interaction	yes

Mechanism of Interaction	Neuronal acetylcholine receptor protein alpha-7 subunit partial agonist
Direct Interaction	yes

Specific Action of the Ligand	Positive
Details of Interaction	(α7)<sub>5</sub>:Type 2
Endogenous Drug?	False

Specific Action of the Ligand	Antagonist
Details of Interaction	(α7)<sub>5</sub>
Endogenous Drug?	False

Specific Action of the Ligand	Full agonist
Details of Interaction	(α7)<sub>5</sub>
Endogenous Drug?	False

Trial Name	varenicline, CP-526
Novel drug target	Established target

Direct Interaction?	False
Endogenous Drug?	False
Details of Interaction	(α7)<sub>5</sub>:Type 2; also blocks α3β4 and α4β2

Details of the Assay for Interaction	Antagonism of ACh activation of human α7 nACh receptors expressed in <i>Xenopus</i> oocytes, at different ACh concentrations.
Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

ENSG00000175344	Ensembl Gene Id
P36544	Uniprot Accession
1139	Entrez Gene Id

NEURONAL ACETYLCHOLINE RECEPTOR PROTEIN, ALPHA-7 SUBUNIT PRECURSOR. [SOURCE:UNIPROT/SWISSPROT;ACC:P36544]	Description
CHRNA7	Display Id
ENSG00000175344	Ensembl Gene Id

1960	HUGO Gene ID
1960	HUGO Gene Symbol
cholinergic receptor nicotinic alpha 7 subunit	HUGO Gene Name

CHRNA7	DrugBank Gene Name
Q693P7	UniProt Accession
1139	Entrez Gene Id

NACHRA7	GENE_SYMBOL
CHRNA7	GENE_SYMBOL
Neuronal acetylcholine receptor subunit alpha-7	UNIPROT

Neuronal acetylcholine receptor subunit alpha-7	Gene Name
P36544	UniProt ID

CHRNA7 Gene Record

CHRNA7 1139 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: partial agonist (activating) agonist (activating)

Interaction Info: Novel drug target Established target Trial Name EVP-6124 Direct Interaction yes

PMIDs: 25438724

Sources: DrugBank TdgClinicalTrial ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality: n/a

Interaction Info: Trial Name GTS-21 Novel drug target Established target

PMIDs: 17334244 15213292 17591554

Sources: DrugBank TdgClinicalTrial TTD

Interaction Types & Directionality: partial agonist (activating)

Interaction Info: Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit partial agonist Direct Interaction yes

PMIDs: 22591063

Sources: DTC ChemblInteractions

Interaction Types & Directionality: allosteric modulator

Interaction Info: Specific Action of the Ligand Positive Details of Interaction (&alpha;7)<sub>5</sub>:Type 2 Endogenous Drug? False

PMIDs: 17470817

Sources: DTC GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info: Novel drug target Established target Trial Name TC-6987Êby Targacept forÊasthmaÊandÊtype II diabetes Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist

PMIDs: None found

Sources: TdgClinicalTrial ChemblInteractions TTD

Interaction Types & Directionality: allosteric modulator

Interaction Info:

PMIDs: 12137632 12481195 12177686 11129124 10971048 20480924 24951635 21062106 11172080

Sources: DrugBank PharmGKB

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: partial agonist (activating) agonist (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit partial agonist Specific Action of the Ligand Agonist

PMIDs: None found

Sources: ChemblInteractions GuideToPharmacology

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit positive allosteric modulator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist Direct Interaction yes Specific Action of the Ligand Full agonist

PMIDs: None found

Sources: ChemblInteractions GuideToPharmacology

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit positive allosteric modulator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist Direct Interaction yes Specific Action of the Ligand Full agonist

PMIDs: None found

Sources: ChemblInteractions GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Details of Interaction (&alpha;7)<sub>5</sub> Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info: Specific Action of the Ligand Full agonist Details of Interaction (&alpha;7)<sub>5</sub> Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: partial agonist (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit partial agonist

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: agonist (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist Trial Name TC-5619

PMIDs: None found

Sources: DrugBank TdgClinicalTrial ChemblInteractions GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info: Specific Action of the Ligand Full agonist Details of Interaction (&alpha;7)<sub>5</sub> Endogenous Drug? False

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name EVP-6124

Direct Interaction yes

PMIDs:
25438724

Sources:
DrugBank TdgClinicalTrial ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name GTS-21

Novel drug target Established target

PMIDs:
17334244 15213292 17591554

Sources:
DrugBank TdgClinicalTrial TTD

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit partial agonist

Direct Interaction yes

PMIDs:
22591063

Sources:
DTC ChemblInteractions

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Specific Action of the Ligand Positive

Details of Interaction (α7)<sub>5</sub>:Type 2

Endogenous Drug? False

PMIDs:
17470817

Sources:
DTC GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name TC-6987Êby Targacept forÊasthmaÊandÊtype II diabetes

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TTD

Interaction Types & Directionality:

allosteric modulator

PMIDs:
12137632 12481195 12177686 11129124 10971048 20480924 24951635 21062106 11172080

Sources:
DrugBank PharmGKB

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit partial agonist

Specific Action of the Ligand Agonist

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist

Direct Interaction yes

Specific Action of the Ligand Full agonist

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist

Direct Interaction yes

Specific Action of the Ligand Full agonist

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Details of Interaction (α7)<sub>5</sub>

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Details of Interaction (α7)<sub>5</sub>

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit partial agonist

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Neuronal acetylcholine receptor protein alpha-7 subunit agonist

Trial Name TC-5619

PMIDs:
None found

Sources:
DrugBank TdgClinicalTrial ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Details of Interaction (α7)<sub>5</sub>

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
16248797 11264449 10487207

Sources:
DrugBank TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)