Target Information

Target General Infomation
Target ID
T55815
Former ID
TTDS00400
Target Name
Neuronal acetylcholinereceptor subunit alpha-2
Gene Name
CHRNA2
Synonyms
CHRNA2
Target Type
Successful
Disease General anesthesia [ICD9: 338; ICD10: R20.0]
Glaucoma [ICD9: 365; ICD10: H40-H42]
Muscle relaxant [ICD10: N39.3, N39.4, R32]
Narcotic depression [ICD9: 304.9, 311; ICD10: F19.20, F32]
Smoking withdrawl syndrom; Anesthesia [ICD9:292, 338; ICD10: F17.2, R20.0]
Spasms; Pain [ICD9: 338,780; ICD10: R52, G89]
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
T55815
UniProt ID
Q15822
Sequence
MGPSCPVFLSFTKLSLWWLLLTPAGGEEAKRPPPRAPGDPLSSPSPTALPQGGSHTETED
RLFKHLFRGYNRWARPVPNTSDVVIVRFGLSIAQLIDVDEKNQMMTTNVWLKQEWSDYKL
RWNPTDFGNITSLRVPSEMIWIPDIVLYNNADGEFAVTHMTKAHLFSTGTVHWVPPAIYK
SSCSIDVTFFPFDQQNCKMKFGSWTYDKAKIDLEQMEQTVDLKDYWESGEWAIVNATGTY
NSKKYDCCAEIYPDVTYAFVIRRLPLFYTINLIIPCLLISCLTVLVFYLPSDCGEKITLC
ISVLLSLTVFLLLITEIIPSTSLVIPLIGEYLLFTMIFVTLSIVITVFVLNVHHRSPSTH
TMPHWVRGALLGCVPRWLLMNRPPPPVELCHPLRLKLSPSYHWLESNVDAEEREVVVEEE
DRWACAGHVAPSVGTLCSHGHLHSGASGPKAEALLQEGELLLSPHMQKALEGVHYIADHL
RSEDADSSVKEDWKYVAMVIDRIFLWLFIIVCFLGTIGLFLPPFLAGMI
Drugs and Mode of Action
Drug(s) Carbachol Drug Info Approved Glaucoma [538221], [539992]
Cisatracurium Drug Info Approved Muscle relaxant [551871]
Levallorphan Drug Info Approved Narcotic depression [538429], [542223]
Mivacurium Drug Info Approved General anesthesia [536361], [542260], [551871]
Pipecuronium Drug Info Approved Spasms; Pain [538529], [551871]
Rocuronium Drug Info Approved Muscle relaxant [551871]
Tubocurarine Drug Info Approved Smoking withdrawl syndrom; Anesthesia [538386], [539445], [551871]
Vecuronium Drug Info Approved Spasms; Pain [536361], [540619]
Cisatracurium Drug Info Phase 4 Discovery agent [525283]
Inhibitor (S)-3-(azetidin-2-ylmethoxy)-2-fluoropyridine Drug Info [530178]
1,1-Dimethyl-4-phenyl-piperazin-1-ium iodide Drug Info [527014]
1-(piperidin-3-ylmethyl)pyridin-2(1H)-one Drug Info [528157]
1-(piperidin-4-ylmethyl)pyridin-2(1H)-one Drug Info [528157]
2-Pyridin-3-yl-7-aza-bicyclo[2.2.1]heptane Drug Info [527015]
3-((S)-Azetidin-2-yloxy)-5-iodo-pyridine Drug Info [527014]
5-(1-Methyl-pyrrolidin-2-yl)-2-phenethyl-pyridine Drug Info [527574]
CHOLINE Drug Info [527014]
CYTISINE Drug Info [528157]
Antagonist Carbachol Drug Info [536781]
Cisatracurium Drug Info [536781], [537286]
Levallorphan Drug Info [536781]
Mivacurium Drug Info [537286]
Pipecuronium Drug Info [536781]
Rocuronium Drug Info [536781], [537286]
Tubocurarine Drug Info [536781], [537286]
Vecuronium Drug Info [536781], [537286]
Modulator (allosteric modulator) LY2087101 Drug Info [528221]
Agonist [125I]epibatidine Drug Info [543841]
[3H]cytisine Drug Info [543841]
[3H]epibatidine Drug Info [543841]
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
PANTHER Pathway Nicotinic acetylcholine receptor signaling pathway
Reactome Highly calcium permeable postsynaptic nicotinic acetylcholine receptors
Highly calcium permeable nicotinic acetylcholine receptors
WikiPathways Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell
References
Ref 525283ClinicalTrials.gov (NCT02518789) Effects and Mechanism of Pretreatment With Dexmedetomidine to Etomidate Induce Myoclonus.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 538221FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070292.
Ref 538386FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 005657.
Ref 538429FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 010423.
Ref 538529FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 019638.
Ref 539445(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2294).
Ref 539992(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 298).
Ref 540619(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4002).
Ref 542223(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7209).
Ref 542260(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7243).
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 527014Bioorg Med Chem Lett. 2004 Apr 19;14(8):1845-8.Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
Ref 527015Bioorg Med Chem Lett. 2004 Apr 19;14(8):1889-96.Epibatidine structure-activity relationships.
Ref 527574Bioorg Med Chem Lett. 2005 Jul 1;15(13):3237-40.6-(2-Phenylethyl)nicotine: a novel nicotinic cholinergic receptor ligand.
Ref 528157J Med Chem. 2006 May 4;49(9):2673-6.Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity.
Ref 528221Identification and pharmacological profile of a new class of selective nicotinic acetylcholine receptor potentiators. J Pharmacol Exp Ther. 2006 Sep;318(3):1108-17. Epub 2006 May 31.
Ref 530178Bioorg Med Chem. 2009 Jul 1;17(13):4367-77. Epub 2009 May 15.Synthesis and biological evaluation of novel carbon-11 labeled pyridyl ethers: candidate ligands for in vivo imaging of alpha4beta2 nicotinic acetylcholine receptors (alpha4beta2-nAChRs) in the brain with positron emission tomography.
Ref 536781Synergy between pairs of competitive antagonists at adult human muscle acetylcholine receptors. Anesth Analg. 2008 Aug;107(2):525-33.
Ref 537286Pharmacological characteristics of the inhibition of nondepolarizing neuromuscular blocking agents at human adult muscle nicotinic acetylcholine receptor. Anesthesiology. 2009 Jun;110(6):1244-52.
Ref 543841(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 463).

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