Target Information
Target General Infomation | |||||
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Target ID |
T73724
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Former ID |
TTDR00164
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Target Name |
Neuronal acetylcholine receptor protein, beta-4 chain
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Gene Name |
CHRNB4
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Synonyms |
Beta-4 nAChR; CHRNB4
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Target Type |
Discontinued
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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.
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BioChemical Class |
Ion transport
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Target Validation |
T73724
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UniProt ID | |||||
Sequence |
MRRAPSLVLFFLVALCGRGNCRVANAEEKLMDDLLNKTRYNNLIRPATSSSQLISIKLQL
SLAQLISVNEREQIMTTNVWLKQEWTDYRLTWNSSRYEGVNILRIPAKRIWLPDIVLYNN ADGTYEVSVYTNLIVRSNGSVLWLPPAIYKSACKIEVKYFPFDQQNCTLKFRSWTYDHTE IDMVLMTPTASMDDFTPSGEWDIVALPGRRTVNPQDPSYVDVTYDFIIKRKPLFYTINLI IPCVLTTLLAILVFYLPSDCGEKMTLCISVLLALTFFLLLISKIVPPTSLDVPLIGKYLM FTMVLVTFSIVTSVCVLNVHHRSPSTHTMAPWVKRCFLHKLPTFLFMKRPGPDSSPARAF PPSKSCVTKPEATATSTSPSNFYGNSMYFVNPASAASKSPAGSTPVAIPRDFWLRSSGRF RQDVQEALEGVSFIAQHMKNDDEDQSVVEDWKYVAMVVDRLFLWVFMFVCVLGTVGLFLP PLFQTHAASEGPYAAQRD |
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Drugs and Mode of Action | |||||
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 526639 | J Med Chem. 2003 Jun 19;46(13):2716-30.Synthesis and biological evaluation of 18-methoxycoronaridine congeners. Potential antiaddiction agents. | ||||
Ref 527644 | J Med Chem. 2005 Jul 28;48(15):4705-45.Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations. | ||||
Ref 528394 | Bioorg Med Chem Lett. 2006 Nov 1;16(21):5493-7. Epub 2006 Aug 28.Epibatidine isomers and analogues: structure-activity relationships. | ||||
Ref 529383 | Bioorg 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 530946 | J 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 535261 | SIB-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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