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Showing drug card for Varenicline (DB01273)

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Version 2.5
Creation Date 2007-05-16 20:24:49
Update Date 2009-06-23 18:06:22
Primary Accession Number DB01273
Secondary Accession Number Not Available
Name Varenicline
Drug Type
  • Approved
  • Investigational
  • Small Molecule
Description Varenicline is a prescription medication used to treat smoking addiction. This medication is the first approved nicotinic receptor partial agonist. Specifically, varenicline is a partial agonist of the alpha4/beta2 subtype of the nicotinic acetylcholine receptor. In addition it acts on alpha3/beta4 and weakly on alpha3beta2 and alpha6-containing receptors. A full agonism was displayed on alpha7-receptors.
Synonyms
  1. CP-526,555
  2. Varenicline tartrate
  3. varenicline
Brand Names
  1. Champix
  2. Chantix
Brand Mixtures Not Available
Chemical IUPAC Name Not Available
Chemical Formula C13H13N3
Chemical Structure Structure
CAS Registry Number 249296-44-4
InChI Identifier InChI=1/C13H13N3/c1-2-16-13-5-11-9-3-8(6-14-7-9)10(11)4-12(13)15-1/h1-2,4-5,8-9,14H,3,6-7H2/t8-,9+
InChI Key JQSHBVHOMNKWFT-DTORHVGOBF
KEGG Drug Not Available
KEGG Compound Not Available
PubChem Compound 5310966 Link Image
PubChem Substance 16411442 Link Image
ChEBI ID Not Available
PharmGKB ID Not Available
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] Not Available
RxList Link http://www.rxlist.com/cgi/generic/chantix.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Varenicline Link Image
FDA Label
Material Safety Data Sheet (MSDS) Not Available
Synthesis Reference Not Available
Average Molecular Weight 211.2624
Monoisotopic Molecular Weight 211.1109
State Solid
Melting Point Not Available
Experimental Water Solubility Not Available Source: PhysProp
Predicted Water Solubility 8.77e-02 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 0.9 Source: PhysProp
Predicted LogP 1.39 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -3.38 Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point Not Available
Mass Spectrum Not Available
MOL File Show Link Image | Download Link Image
SDF File Show Link Image | Download Link Image
PDB File Show Link Image | Download Link Image
2D Structure
3D Structure
Experimental PDB ID Not Available
Isomeric SMILES C1NC[C@@H]2C[C@H]1C1=CC3=NC=CN=C3C=C21
Canonical SMILES C1NCC2CC1C1=CC3=NC=CN=C3C=C21
Drug Category
  • Nicotinic Agonists
ATC Codes
AHFS Codes Not Available
Indication For use as an aid in smoking cessation.
Pharmacology Varenicline is a partial nicotinic acetylcholine receptor agonist, designed to partially activate this system while displacing nicotine at its sites of action in the brain.
Mechanism of Action Varenicline is an alpha-4 beta-2 neuronal nicotinic acetylcholine receptor agonist. The drug shows high selectiviyty for this receptor subclass, relative to other nicotinic receptors (>500-fold alpha-3 beta-4, >3500-fold alpha-7, >20,000-fold alpha-1 beta gamma delta) or non-nicotinic receptors and transporters (>2000-fold). The drug competitively inhibits the ability of nicotine to bind to and activate the alpha-4 beta-2 receptor. The drug exerts mild agonistic activity at this site, though at a level much lower than nicotine; it is presumed that this activation eases withdrawal symptoms.
Absorption Not Available
Toxicity Not Available
Protein Binding Less than 20%.
Biotransformation Metabolism is limited (<10%). Most of the active compound is excreted renally (81%). A small proportion is glucuronidated, oxidated, N-formylated or conjugated to a hexose.
Half Life The elimination half-life of varenicline is approximately 24 hours
Dosage Forms
Form Route
Tablet, film coated Oral
Patient Information Show Link Image
Contraindications Not Available
Interactions Show Link Image
Drug Interactions Not Available
Food Interactions Not Available
Pathways Not Available
General References
  1. Coe JW, Brooks PR, Vetelino MG, Wirtz MC, Arnold EP, Huang J, Sands SB, Davis TI, Lebel LA, Fox CB, Shrikhande A, Heym JH, Schaeffer E, Rollema H, Lu Y, Mansbach RS, Chambers LK, Rovetti CC, Schulz DW, Tingley FD 3rd, O'Neill BT: Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation. J Med Chem. 2005 May 19;48(10):3474-7. [PubMed Link Image]
  2. Obach RS, Reed-Hagen AE, Krueger SS, Obach BJ, O'Connell TN, Zandi KS, Miller S, Coe JW: Metabolism and disposition of varenicline, a selective alpha4beta2 acetylcholine receptor partial agonist, in vivo and in vitro. Drug Metab Dispos. 2006 Jan;34(1):121-30. Epub 2005 Oct 12. [PubMed Link Image]
  3. Kuehn BM: FDA speeds smoking cessation drug review. JAMA. 2006 Feb 8;295(6):614. [PubMed Link Image]
  4. Mihalak KB, Carroll FI, Luetje CW: Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. Mol Pharmacol. 2006 Sep;70(3):801-5. Epub 2006 Jun 9. [PubMed Link Image]
  5. Jorenby DE, Hays JT, Rigotti NA, Azoulay S, Watsky EJ, Williams KE, Billing CB, Gong J, Reeves KR: Efficacy of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation: a randomized controlled trial. JAMA. 2006 Jul 5;296(1):56-63. [PubMed Link Image]
  6. Wikipedia Link Image
  7. RxList Link Image
Organisms Affected
  • Humans and other mammals
Targets
  1. Neuronal acetylcholine receptor subunit alpha-4
  2. Neuronal acetylcholine receptor subunit alpha-7
Drug Target 1 [top]
Target 1 ID 947
Target 1 Name Neuronal acetylcholine receptor subunit alpha-4
Target 1 Synonyms
  1. Neuronal acetylcholine receptor subunit alpha-4 precursor
Target 1 Gene Name CHRNA4
Target 1 Protein Sequence >Neuronal acetylcholine receptor subunit alpha-4 precursor 
MELGGPGAPRLLPPLLLLLGTGLLRASSHVETRAHAEERLLKKLFSGYNKWSRPVANISD
VVLVRFGLSIAQLIDVDEKNQMMTTNVWVKQEWHDYKLRWDPADYENVTSIRIPSELIWR
PDIVLYNNADGDFAVTHLTKAHLFHDGRVQWTPPAIYKSSCSIDVTFFPFDQQNCTMKFG
SWTYDKAKIDLVNMHSRVDQLDFWESGEWVIVDAVGTYNTRKYECCAEIYPDITYAFVIR
RLPLFYTINLIIPCLLISCLTVLVFYLPSECGEKITLCISVLLSLTVFLLLITEIIPSTS
LVIPLIGEYLLFTMIFVTLSIVITVFVLNVHHRSPRTHTMPTWVRRVFLDIVPRLLLMKR
PSVVKDNCRRLIESMHKMASAPRFWPEPEGEPPATSGTQSLHPPSPSFCVPLDVPAEPGP
SCKSPSDQLPPQQPLEAEKASPHPSPGPCRPPHGTQAPGLAKARSLSVQHMSSPGEAVEG
GVRCRSRSIQYCVPRDDAAPEADGQAAGALASRNTHSAELPPPDQPSPCKCTCKKEPSSV
SPSATVKTRSTKAPPPHLPLSPALTRAVEGVQYIADHLKAEDTDFSVKEDWKYVAMVIDR
IFLWMFIIVCLLGTVGLFLPPWLAGMI
Target 1 Number of Residues 637
Target 1 Molecular Weight 69958
Target 1 Theoretical pI 7.21
Target 1 GO Classification
Function
excitatory extracellular ligand-gated ion channel activity
nicotinic acetylcholine-activated cation-selective channel activity
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
signal transducer activity
receptor activity
neurotransmitter receptor activity
Process
physiological process
cellular physiological process
transport
ion transport
Component
postsynaptic membrane
intrinsic to membrane
integral to membrane
cell
membrane
Target 1 General Function Involved in neurotransmitter receptor activity
Target 1 Specific 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
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • 1-28
Target 1 Transmembrane Regions
  • 243-267
  • 275-293
  • 309-330
  • 601-619
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 755648 Link Image
Target 1 UniProtKB/Swiss-Prot ID P43681 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name ACHA4_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 1 Gene Sequence >1884 bp 
ATGGAGCTAGGGGGCCCCGGAGCGCCGCGGCTGCTGCCGCCGCTGCTGCTGCTTCTGGGG
ACCGGCCTCCTGCGCGCCAGCAGCCATGTGGAGACCCGGGCCCACGCCGAGGAGCGGCTC
CTGAAGAAACTCTTCTCCGGTTACAACAAGTGGTCCCGACCCGTGGCCAACATCTCGGAC
GTGGTCCTCGTCCGCTTCGGCCTGTCCATCGCTCAGCTCATTGACGTGGATGAGAAGAAC
CAGATGATGACCACGAACGTATGGGTGAAGCAGGAGTGGCACGACTACAAGCTGCGCTGG
GACCCAGCTGACTATGAGAATGTCACCTCCATCCGCATCCCCTCCGAGCTCATCTGGCGG
CCGGACATCGTCCTCTACAACAATGCTGACGGGGACTTCGCGGTCACCCACCTGACCAAG
GCCCACCTGTTCCATGACGGGCGGGTGCAGTGGACTCCCCCGGCCATTTACAAGAGCTCC
TGCAGCATCGACGTCACCTTCTTCCCCTTCGACCAGCAGAACTGCACCATGAAATTCGGC
TCCTGGACCTACGACAAGGCCAAGATCGACCTGGTGAACATGCACAGCCGCGTGGACCAG
CTGGACTTCTGGGAGAGTGGCGAGTGGGTCATCGTGGATGCCGTGGGCACCTACAACACC
AGGAAGTACGAGTGCTGTGCCGAGATCTACCCGGACATCACCTATGCCTTCGTCATCCGG
CGGCTGCCGCTCTTCTACACCATCAACCTCATCATCCCCTGCCTGCTCATCTCCTGCCTC
ACCGTGCTGGTCTTCTACCTGCCCTCCGAGTGTGGCGAGAAGATCACGCTGTGCATCTCC
GTGCTGCTGTCGCTCACCGTCTTCCTGCTGCTCATCACCGAGATCATCCCGTCCACCTCA
CTGGTCATCCCACTCATCGGCGAGTACCTGCTGTTCACCATGATCTTCGTCACCCTGTCC
ATCGTCATCACGGTCTTCGTGCTCAACGTGCACCACCGCTCGCCACGCACGCACACCATG
CCCACCTGGGTACGCAGGGTCTTCCTGGACATCGTGCCACGCCTGCTCCTCATGAAGCGG
CCGTCCGTGGTCAAGGACAATTGCCGGCGGCTCATCGAGTCCATGCATAAGATGGCCAGT
GCCCCGCGCTTCTGGCCCGAGCCAGAAGGGGAGCCCCCTGCCACGAGCGGCACCCAGAGC
CTGCACCCGCCCTCACCGTCCTTCTGTGTCCCCCTGGATGTGCCGGCTGAGCCTGGGCCT
TCCTGCAAGTCACCCTCCGACCAGCTCCCTCCTCAGCAGCCCCTGGAAGCTGAGAAAGCC
AGCCCCCACCCCTCGCCTGGACCCTGCCGCCCGCCCCACGGCACCCAGGCACCAGGGCTG
GCCAAAGCCAGGTCCCTCAGCGTCCAGCACATGTCCAGCCCTGGCGAAGCGGTGGAAGGC
GGCGTCCGGTGCCGGTCTCGGAGCATCCAGTACTGTGTTCCCCGAGACGATGCCGCCCCC
GAGGCAGATGGCCAGGCTGCCGGCGCCCTGGCCTCTCGCAACACCCACTCGGCTGAGCTC
CCACCCCCAGACCAGCCCTCTCCGTGCAAATGCACATGCAAGAAGGAGCCCTCTTCGGTG
TCCCCGAGTGCCACGGTCAAGACCCGCAGCACCAAAGCACCGCCCCCGCACCTGCCCCTG
TCGCCGGCCCTGACCCGGGCGGTGGAGGGCGTCCAGTACATTGCAGACCACCTGAAGGCC
GAAGACACAGACTTCTCGGTGAAGGAGGACTGGAAGTACGTGGCCATGGTCATCGACCGC
ATCTTCCTCTGGATGTTCATCATCGTCTGCCTGCTGGGGACGGTGGGCCTCTTCCTGCCG
CCCTGGCTGGCTGGCATGATCTAG
Target 1 GenBank Gene ID
Target 1 GeneCard ID CHRNA4 Link Image
Target 1 GenAtlas ID CHRNA4 Link Image
Target 1 HGNC ID HGNC:1958 Link Image
Target 1 Chromosome Location 20
Target 1 Locus 20q13.2-q13.3
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Deloukas P, Matthews LH, Ashurst J, Burton J, Gilbert JG, Jones M, Stavrides G, Almeida JP, Babbage AK, Bagguley CL, Bailey J, Barlow KF, Bates KN, Beard LM, Beare DM, Beasley OP, Bird CP, Blakey SE, Bridgeman AM, Brown AJ, Buck D, Burrill W, Butler AP, Carder C, Carter NP, Chapman JC, Clamp M, Clark G, Clark LN, Clark SY, Clee CM, Clegg S, Cobley VE, Collier RE, Connor R, Corby NR, Coulson A, Coville GJ, Deadman R, Dhami P, Dunn M, Ellington AG, Frankland JA, Fraser A, French L, Garner P, Grafham DV, Griffiths C, Griffiths MN, Gwilliam R, Hall RE, Hammond S, Harley JL, Heath PD, Ho S, Holden JL, Howden PJ, Huckle E, Hunt AR, Hunt SE, Jekosch K, Johnson CM, Johnson D, Kay MP, Kimberley AM, King A, Knights A, Laird GK, Lawlor S, Lehvaslaiho MH, Leversha M, Lloyd C, Lloyd DM, Lovell JD, Marsh VL, Martin SL, McConnachie LJ, McLay K, McMurray AA, Milne S, Mistry D, Moore MJ, Mullikin JC, Nickerson T, Oliver K, Parker A, Patel R, Pearce TA, Peck AI, Phillimore BJ, Prathalingam SR, Plumb RW, Ramsay H, Rice CM, Ross MT, Scott CE, Sehra HK, Shownkeen R, Sims S, Skuce CD, Smith ML, Soderlund C, Steward CA, Sulston JE, Swann M, Sycamore N, Taylor R, Tee L, Thomas DW, Thorpe A, Tracey A, Tromans AC, Vaudin M, Wall M, Wallis JM, Whitehead SL, Whittaker P, Willey DL, Williams L, Williams SA, Wilming L, Wray PW, Hubbard T, Durbin RM, Bentley DR, Beck S, Rogers J: The DNA sequence and comparative analysis of human chromosome 20. Nature. 2001 Dec 20-27;414(6866):865-71. [PubMed Link Image]
  2. Steinlein OK, Mulley JC, Propping P, Wallace RH, Phillips HA, Sutherland GR, Scheffer IE, Berkovic SF: A missense mutation in the neuronal nicotinic acetylcholine receptor alpha 4 subunit is associated with autosomal dominant nocturnal frontal lobe epilepsy. Nat Genet. 1995 Oct;11(2):201-3. [PubMed Link Image]
  3. Monteggia LM, Gopalakrishnan M, Touma E, Idler KB, Nash N, Arneric SP, Sullivan JP, Giordano T: Cloning and transient expression of genes encoding the human alpha 4 and beta 2 neuronal nicotinic acetylcholine receptor (nAChR) subunits. Gene. 1995 Apr 3;155(2):189-93. [PubMed Link Image]
  4. Steinlein O, Weiland S, Stoodt J, Propping P: Exon-intron structure of the human neuronal nicotinic acetylcholine receptor alpha 4 subunit (CHRNA4). Genomics. 1996 Mar 1;32(2):289-94. [PubMed Link Image]
  5. Elliott KJ, Ellis SB, Berckhan KJ, Urrutia A, Chavez-Noriega LE, Johnson EC, Velicelebi G, Harpold MM: Comparative structure of human neuronal alpha 2-alpha 7 and beta 2-beta 4 nicotinic acetylcholine receptor subunits and functional expression of the alpha 2, alpha 3, alpha 4, alpha 7, beta 2, and beta 4 subunits. J Mol Neurosci. 1996 Fall;7(3):217-28. [PubMed Link Image]
  6. Groot Kormelink PJ, Luyten WH: Cloning and sequence of full-length cDNAs encoding the human neuronal nicotinic acetylcholine receptor (nAChR) subunits beta3 and beta4 and expression of seven nAChR subunits in the human neuroblastoma cell line SH-SY5Y and/or IMR-32. FEBS Lett. 1997 Jan 6;400(3):309-14. [PubMed Link Image]
Target 1 Drug References
  1. Nakamura M, Oshima A, Fujimoto Y, Maruyama N, Ishibashi T, Reeves KR: Efficacy and tolerability of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, in a 12-week, randomized, placebo-controlled, dose-response study with 40-week follow-up for smoking cessation in Japanese smokers. Clin Ther. 2007 Jun;29(6):1040-56. [PubMed Link Image]
  2. McColl S, Burstein A, Reeves K, Billing Jr C, Stolar M, Sellers E: Human Abuse Liability of the Smoking Cessation Drug Varenicline in Smokers and Nonsmokers. Clin Pharmacol Ther. 2008 Feb 20;. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 4095
Target 2 Name Neuronal acetylcholine receptor subunit alpha-7
Target 2 Synonyms
  1. Neuronal acetylcholine receptor subunit alpha-7 precursor
Target 2 Gene Name CHRNA7
Target 2 Protein Sequence >Neuronal acetylcholine receptor subunit alpha-7 
MRCSPGGVWLALAASLLHVSLQGEFQRKLYKELVKNYNPLERPVANDSQPLTVYFSLSLL
QIMDVDEKNQVLTTNIWLQMSWTDHYLQWNVSEYPGVKTVRFPDGQIWKPDILLYNSADE
RFDATFHTNVLVNSSGHCQYLPPGIFKSSCYIDVRWFPFDVQHCKLKFGSWSYGGWSLDL
QMQEADISGYIPNGEWDLVGIPGKRSERFYECCKEPYPDVTFTVTMRRRTLYYGLNLLIP
CVLISALALLVFLLPADSGEKISLGITVLLSLTVFMLLVAEIMPATSDSVPLIAQYFAST
MIIVGLSVVVTVIVLQYHHHDPDGGKMPKWTRVILLNWCAWFLRMKRPGEDKVRPACQHK
QRRCSLASVEMSAVAPPPASNGNLLYIGFRGLDGVHCVPTPDSGVVCGRMACSPTHDEHL
LHGGQPPEGDPDLAKILEEVRYIANRFRCQDESEAVCSEWKFAACVVDRLCLMAFSVFTI
ICTIGILMSAPNFVEAVSKDFA
Target 2 Number of Residues 510
Target 2 Molecular Weight 56450
Target 2 Theoretical pI 6.44
Target 2 GO Classification
Function
excitatory extracellular ligand-gated ion channel activity
nicotinic acetylcholine-activated cation-selective channel activity
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
signal transducer activity
receptor activity
neurotransmitter receptor activity
Process
physiological process
cellular physiological process
transport
ion transport
Component
postsynaptic membrane
intrinsic to membrane
integral to membrane
cell
membrane
Target 2 General Function Not Available
Target 2 Specific 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
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • 1-22
Target 2 Transmembrane Regions
  • 231-255
  • 262-280
  • 296-317
  • 470-490
Target 2 Essentiality Non Essential
Target 2 GenBank ID Protein 496607 Link Image
Target 2 UniProtKB/Swiss-Prot ID P36544 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name ACHA7_HUMAN Link Image
Target 2 PDB ID Not Available
Target 2 Cellular Location
  • Membrane
Target 2 Gene Sequence >1509 bp 
ATGCGCTGCTCGCCGGGAGGCGTCTGGCTGGGCCTGGCCGCGTCGCTCCTGCACGTGTCC
CTGCAAGGCGAGTTCCAGAGGAAGCTTTACAAGGAGCTGGTCAAGAACTACAATCCCTTG
GAGAGGCCCGTGGCCAATGACTCGCAACCACTCACCGTCTACTTCTCCCTGAGCCTCCTG
CAGATCATGGACGTGGATGAGAAGAACCAAGTTTTAACCACCAACATTTGGCTGCAAATG
TCTTGGACAGATCACTATTTACAGTGGAATGTGTCAGAATATCCAGGGGTGAAGACTGTT
CGTTTCCCAGATGGCCAGATTTGGAAACCAGACATTCTTCTCTATAACAGTGCTGATGAG
CGCTTTGACGCCACATTCCACACTAACGTGTTGGTGAATTCTTCTGGGCATTGCCAGTAC
CTGCCTCCAGGCATATTCAAGAGTTCCTGCTACATCGATGTACGCTGGTTTCCCTTTGAT
GTGCAGCACTGCAAACTGAAGTTTGGGTCCTGGTCTTACGGAGGCTGGTCCTTGGATCTG
CAGATGCAGGAGGCAGATATCAGTGGCTATATCCCCAATGGAGAATGGGACCTAGTGGGA
ATCCCCGGCAAGAGGAGTGAAAGGTTCTATGAGTGCTGCAAAGAGCCCTACCCCGATGTC
ACCTTCACAGTGACCATGCGCCGCAGGACACTCTACTATGGCCTCAACCTGCTGATCCCC
TGTGTGCTCATCTCCGCCCTCGCCCTGCTGGTGTTCCTGCTTCCTGCAGATTCCGGGGAG
AAGATTTCCCTGGGGATAACAGTCTTACTCTCTCTTACCGTCTTCATGCTGCTCGTGGCT
GAGATCATGCCCGCAACATCCGATTCGGTACCATTGATAGCCCAGTACTTCGCCAGCACC
ATGATCATCGTGGGCCTCTCGGTGGTGGTGACAGTGATCGTGCTGCAGTACCACCACCAC
GACCCCGACGGGGGCAAGATGCCCAAGTGGACCAGAGTCATCCTTCTGAACTGGTGCGCG
TGGTTCCTGCGAATGAAGAGGCCCGGGGAGGACAAGGTGCGCCCGGCCTGCCAGCACAAG
CAGCGGCGCTGCAGCCTGGCCAGTGTGGAGATGAGCGCCGTGGGCCCGCCGCCCGCCAGC
AACGGGAACCTGCTGTACATCGGCTTCCGCGGCCTGGACGGCGTGCACTGTGTCCCGACC
CCCGACTCTGGGGTAGTGTGTGGCCGCATGGCCTGCTCCCCCACGCACGATGAGCACCTC
CTGCACGGCGGGCAACCCCCCGAGGGGGACCCGGACTTGGCCAAGATCCTGGAGGAGGTC
CGCTACATTGCCAACCGCTTCCGCTGCCAGGACGAAAGCGAGGCGGTCTGCAGCGAGTGG
AAGTTCGCCGCCTGTGTGGTGGACCGCCTGTGCCTCATGGCCTTCTCGGTCTTCACCATC
ATCTGCACCATCGGCATCCTGATGTCGGCTCCCAACTTCGTGGAGGCCGTGTCCAAAGAC
TTTGCGTAA
Target 2 GenBank Gene ID
Target 2 GeneCard ID CHRNA7 Link Image
Target 2 GenAtlas ID CHRNA7 Link Image
Target 2 HGNC ID HGNC:1960 Link Image
Target 2 Chromosome Location 15
Target 2 Locus 15q14
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Riley B, Williamson M, Collier D, Wilkie H, Makoff A: A 3-Mb map of a large Segmental duplication overlapping the alpha7-nicotinic acetylcholine receptor gene (CHRNA7) at human 15q13-q14. Genomics. 2002 Feb;79(2):197-209. [PubMed Link Image]
  2. Harris RA, Yang A, Stein RC, Lucy K, Brusten L, Herath A, Parekh R, Waterfield MD, O'Hare MJ, Neville MA, Page MJ, Zvelebil MJ: Cluster analysis of an extensive human breast cancer cell line protein expression map database. Proteomics. 2002 Feb;2(2):212-23. [PubMed Link Image]
  3. Peng X, Katz M, Gerzanich V, Anand R, Lindstrom J: Human alpha 7 acetylcholine receptor: cloning of the alpha 7 subunit from the SH-SY5Y cell line and determination of pharmacological properties of native receptors and functional alpha 7 homomers expressed in Xenopus oocytes. Mol Pharmacol. 1994 Mar;45(3):546-54. [PubMed Link Image]
  4. Chini B, Raimond E, Elgoyhen AB, Moralli D, Balzaretti M, Heinemann S: Molecular cloning and chromosomal localization of the human alpha 7-nicotinic receptor subunit gene (CHRNA7). Genomics. 1994 Jan 15;19(2):379-81. [PubMed Link Image]
  5. Elliott KJ, Ellis SB, Berckhan KJ, Urrutia A, Chavez-Noriega LE, Johnson EC, Velicelebi G, Harpold MM: Comparative structure of human neuronal alpha 2-alpha 7 and beta 2-beta 4 nicotinic acetylcholine receptor subunits and functional expression of the alpha 2, alpha 3, alpha 4, alpha 7, beta 2, and beta 4 subunits. J Mol Neurosci. 1996 Fall;7(3):217-28. [PubMed Link Image]
  6. Groot Kormelink PJ, Luyten WH: Cloning and sequence of full-length cDNAs encoding the human neuronal nicotinic acetylcholine receptor (nAChR) subunits beta3 and beta4 and expression of seven nAChR subunits in the human neuroblastoma cell line SH-SY5Y and/or IMR-32. FEBS Lett. 1997 Jan 6;400(3):309-14. [PubMed Link Image]
Target 2 Drug References
  1. Mihalak KB, Carroll FI, Luetje CW: Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. Mol Pharmacol. 2006 Sep;70(3):801-5. Epub 2006 Jun 9. [PubMed Link Image]

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.