Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00520

Target Information
NameNeuronal acetylcholine receptor protein, alpha-7 chain    
Type of targetSuccessful target    
SynonymsAlpha(7) nicotinic receptor    
Alpha-7 nAChR    
Alpha7 nAChR    
Alpha7 nicotinic receptor    
Nicotinic acetylcholine receptor alpha7    
Nicotinic acetylcholine receptor subunit alpha 7    
DiseaseAlzheimer's disease
[ICD9: 331.0   ICD10: G30]
[1][2]
Analgesics
[ICD9: 338   ICD10: R52]
[3]
Drug dependence
[ICD9: 303-304   ICD10: F10.2-F19.2]
[4]
Neuropsychiatric disorders[4]
Pain
[ICD9: 338,780   ICD10: R52, G89]
[3]
Schizophrenia
[ICD9: 295   ICD10: F20]
[4]
Drug(s)TC-5280LaunchedSchizophrenia[5]
EVP-6124Phase IIMild to moderate Alzheimer's disease
EVP-6124Phase IISchizophrenia
MEM-3454Phase IISchizophrenia[5]
R3487Phase IIAlzheimer's disease, schizophrenia[6]
PNU-282987DiscontinuedSchizophrenia[5]
R4996Suspended in Phase IAlzheimer's disease[6]
RMG-40083PreclinicalSchizophrenia[5]
TC-1698PreclinicalSchizophrenia[5]
BioChemical ClassIon transport    
PathwayCalcium signaling pathway
UniProt IDP36544
FunctionAfter binding acetylcholine, the achr responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.    
SequenceMRCSPGGVWLALAASLLHVSLQGEFQRKLYKELVKNYNPLERPVANDSQPLTVYFSLSLL QIMDVDEKNQVLTTNIWLQMSWTDHYLQWNVSEYPGVKTVRFPDGQIWKPDILLYNSADE RFDATFHTNVLVNSSGHCQYLPPGIFKSSCYIDVRWFPFDVQHCKLKFGSWSYGGWSLDL QMQEADISGYIPNGEWDLVGIPGKRSERFYECCKEPYPDVTFTVTMRRRTLYYGLNLLIP CVLISALALLVFLLPADSGEKISLGITVLLSLTVFMLLVAEIMPATSDSVPLIAQYFAST MIIVGLSVVVTVIVLQYHHHDPDGGKMPKWTRVILLNWCAWFLRMKRPGEDKVRPACQHK QRRCSLASVEMSAVAPPPASNGNLLYIGFRGLDGVHCVPTPDSGVVCGRMACSPTHDEHL LHGGQPPEGDPDLAKILEEVRYIANRFRCQDESEAVCSEWKFAACVVDRLCLMAFSVFTI ICTIGILMSAPNFVEAVSKDFA
Target ValidationClick to Find Target Validation Information.    
Inhibitor3,8-dibromoboldine[7]
3-bromoboldine[7]
ALCURONIUM[8]
CP-810123[9]
CYTISINE[10]
GCCSHPACAGNNQHIC*[11]
GCCSNPVCHLEHSNLC*[11]
N-methyllaurotetanine methiodide[7]
PH-709829[12]
PHA-543613[12]
TOXIFERINE[8]
boldine methiodide[7]
glaucine methiodide[7]
AgonistGTS-21[2][13]
R3487[6]
R4996[6]
AntagonistBarbital[14]
Barbituric acid derivative[14]
Laudanosine[15]
MEM-3454[5]
Methyllycaconitine[1][16]
PNU-282987[5]
RMG-40083[5]
BinderTC-1698[5]
TC-5280[5]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Nicotine increases the expression of high affinity nerve growth factor receptors in both in vitro and in vivo. Life Sci. 2002 Feb 15;70(13):1543-54. To Reference
Ref 2The brain alpha7 nicotinic receptor may be an important therapeutic target for the treatment of Alzheimer's disease: studies with DMXBA (GTS-21). Behav Brain Res. 2000 Aug;113(1-2):169-81. To Reference
Ref 3Challenges in Analgesic Drug Development. Clin Pharmacol Ther. 2009 Aug 12. To Reference
Ref 4Rats exhibiting acute behavioural tolerance to nicotine have more [125I]alpha-bungarotoxin binding sites in brain than rats not exhibiting tolerance. Behav Brain Res. 2000 Aug;113(1-2):105-15. To Reference
Ref 5The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31. To Reference
Ref 6Roche. Product Development Pipeline. July 29 2009. To Reference
Ref 7Bioorg Med Chem. 2007 May 15;15(10):3368-72. Epub 2007 Mar 13.Aporphine metho salts as neuronal nicotinic acetylcholine receptor blockers. To Reference
Ref 8J Med Chem. 2007 Sep 20;50(19):4616-29. Epub 2007 Aug 28.Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor. To Reference
Ref 9J Med Chem. 2010 Feb 11;53(3):1222-37.Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models. To Reference
Ref 10Bioorg Med Chem Lett. 2005 Nov 15;15(22):4889-97.3,5-Bicyclic aryl piperidines: a novel class of alpha4beta2 neuronal nicotinic receptor partial agonists for smoking cessation. To Reference
Ref 11J Med Chem. 2005 Jul 28;48(15):4705-45.Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations. To Reference
Ref 12Bioorg Med Chem Lett. 2008 Jun 15;18(12):3611-5. Epub 2008 May 1.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. To Reference
Ref 13Selective alpha7-nicotinic agonists normalize inhibition of auditory response in DBA mice. Psychopharmacology (Berl). 1998 Apr;136(4):320-7. To Reference
Ref 14Whiting PJ: The GABAA receptor gene family: new opportunities for drug development. Curr Opin Drug Discov Devel. 2003 Sep;6(5):648-57. To Reference
Ref 15Blockade and activation of the human neuronal nicotinic acetylcholine receptors by atracurium and laudanosine. Anesthesiology. 2001 Apr;94(4):643-51. To Reference
Ref 16Experience of Black participants in the Lung Health Study smoking cessation intervention program. Nicotine Tob Res. 2001 Nov;3(4):375-82. To Reference



 

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