Target Information

Target General Infomation
Target ID
T73724
Former ID
TTDR00164
Target Name
Neuronal acetylcholine receptor protein, beta-4 chain
Gene Name
CHRNB4
Synonyms
Beta-4 nAChR; CHRNB4
Target Type
Discontinued
Disease Alzheimer disease [ICD9: 331; ICD10: G30]
Function
After 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.
BioChemical Class
Ion transport
Target Validation
T73724
UniProt ID
P30926
Sequence
MRRAPSLVLFFLVALCGRGNCRVANAEEKLMDDLLNKTRYNNLIRPATSSSQLISIKLQL
SLAQLISVNEREQIMTTNVWLKQEWTDYRLTWNSSRYEGVNILRIPAKRIWLPDIVLYNN
ADGTYEVSVYTNLIVRSNGSVLWLPPAIYKSACKIEVKYFPFDQQNCTLKFRSWTYDHTE
IDMVLMTPTASMDDFTPSGEWDIVALPGRRTVNPQDPSYVDVTYDFIIKRKPLFYTINLI
IPCVLTTLLAILVFYLPSDCGEKMTLCISVLLALTFFLLLISKIVPPTSLDVPLIGKYLM
FTMVLVTFSIVTSVCVLNVHHRSPSTHTMAPWVKRCFLHKLPTFLFMKRPGPDSSPARAF
PPSKSCVTKPEATATSTSPSNFYGNSMYFVNPASAASKSPAGSTPVAIPRDFWLRSSGRF
RQDVQEALEGVSFIAQHMKNDDEDQSVVEDWKYVAMVVDRLFLWVFMFVCVLGTVGLFLP
PLFQTHAASEGPYAAQRD
Drugs and Mode of Action
Drug(s) SIB-1553A Drug Info Discontinued in Phase 2 Alzheimer disease [546683]
HOMOEPIBATIDINE Drug Info Terminated Discovery agent [546333]
Inhibitor (2S,3S)-2-(m-Tolyl)-3,5,5-trimethylmorpholin-2-ol Drug Info [530946]
(2S,3S)-2-Phenyl-3,5,5-trimethylmorpholin-2-ol Drug Info [530946]
15-nor-18-Methoxycornaridine Drug Info [526639]
18-Dimethylaminocoronaridine Drug Info [526639]
18-methoxycoronaridinate 2-Hydroxyethylamide Drug Info [526639]
18-methoxycoronaridinate 2-methoxyethylamide Drug Info [526639]
18-Methylaminocoronaridine Drug Info [526639]
2-Acetylaminoethyl 18-methoxycoronaridinate Drug Info [526639]
2-Hydroxyethyl 18-methoxycoronaridinate Drug Info [526639]
2-Methoxyethyl 18-methoxycoronaridinate Drug Info [526639]
CYTISINE Drug Info [529383]
GCCSNPVCHLEHSNLC* Drug Info [527644]
HOMOEPIBATIDINE Drug Info [528394]
N,N-Dimethylaminoethyl 18-methoxycoronaridinate Drug Info [526639]
Agonist SIB-1553A Drug Info [535261]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Cholinergic synapse
PANTHER Pathway Nicotinic acetylcholine receptor signaling pathway
Nicotine pharmacodynamics pathway
Reactome Highly sodium permeable acetylcholine nicotinic receptors
Highly calcium permeable postsynaptic nicotinic acetylcholine receptors
Highly calcium permeable nicotinic acetylcholine receptors
WikiPathways SIDS Susceptibility Pathways
Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell
Nicotine Activity on Chromaffin Cells
References
Ref 546333Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007531)
Ref 546683Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009631)
Ref 526639J Med Chem. 2003 Jun 19;46(13):2716-30.Synthesis and biological evaluation of 18-methoxycoronaridine congeners. Potential antiaddiction agents.
Ref 527644J Med Chem. 2005 Jul 28;48(15):4705-45.Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.
Ref 528394Bioorg Med Chem Lett. 2006 Nov 1;16(21):5493-7. Epub 2006 Aug 28.Epibatidine isomers and analogues: structure-activity relationships.
Ref 529383Bioorg Med Chem Lett. 2008 Apr 1;18(7):2316-9. Epub 2008 Mar 6.Deconstructing cytisine: The syntheses of (+/-)-cyfusine and (+/-)-cyclopropylcyfusine, fused ring analogs of cytisine.
Ref 530946J Med Chem. 2010 Jun 24;53(12):4731-48.Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation.
Ref 535261SIB-1553A, (+/-)-4-[[2-(1-methyl-2-pyrrolidinyl)ethyl]thio]phenol hydrochloride, a subtype-selective ligand for nicotinic acetylcholine receptors with putative cognitive-enhancing properties: effectson working and reference memory performances in aged rodents and nonhuman primates. J Pharmacol Exp Ther. 2001 Oct;299(1):297-306.

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