DGIdb - NICOTINE Drug Record

NICOTINE chembl:CHEMBL3 Approved

Alternate Names:

NIQUITIN MINIS ORANGE
NICABATE
NIQUITIN
STUBIT
NICOTROL
NICOTROL NS
NICOTINELL TTS 30
NICOPASS
NICOTINE
NICORETTE INVISI
NICOTINELL SUPPORT
NIQUITIN MINIS CHERRY
NIQUITIN PRE-QUIT
NICOPATCH
NICOTINELL TTS 20
NIQUITIN CLR
STOPPERS
NICOTINELL CLASSIC
NIQUITIN MINIS MINT
NICODERM CQ
NICOTINELL TTS 10
NICOTROL INHALER
NIQUITIN MINT
NIQUITIN STRIPS MINT
PROSTEP
HABITROL
NICODERM

Drug Info:

Year of Approval	1996
Drug Class	central nervous system stimulants
FDA Approval	1996
Drug Class	small molecule
Drug Indications	Central Nervous System Stimulants

(5 More Sources)

Publications:

Mansvelder et al., 2009, Nicotinic modulation of synaptic transmission and plasticity in cortico-limbic circuits., Semin. Cell Dev. Biol.
Zaniewska et al., Nicotine dependence - human and animal studies, current pharmacotherapies and future perspectives., Pharmacol Rep
Mexal et al., 2007, alpha7 nicotinic receptor gene promoter polymorphisms in inbred mice affect expression in a cell type-specific fashion., J. Biol. Chem.
Narahashi et al., 2000, Symposium overview: mechanism of action of nicotine on neuronal acetylcholine receptors, from molecule to behavior., Toxicol. Sci.
Olincy et al., 2006, Proof-of-concept trial of an alpha7 nicotinic agonist in schizophrenia., Arch. Gen. Psychiatry
Jackson et al., 2010, Role of alpha5 nicotinic acetylcholine receptors in pharmacological and behavioral effects of nicotine in mice., J. Pharmacol. Exp. Ther.
Rigbi A et al., 2011, Why do young women smoke? VI. A controlled study of nicotine effects on attention: pharmacogenetic interactions., Pharmacogenomics J
Kuehl et al., 2003, N-glucuronidation of nicotine and cotinine by human liver microsomes and heterologously expressed UDP-glucuronosyltransferases., Drug Metab. Dispos.
Ehringer et al., 2007, Association of the neuronal nicotinic receptor beta2 subunit gene (CHRNB2) with subjective responses to alcohol and nicotine., Am. J. Med. Genet. B Neuropsychiatr. Genet.
De Luca et al., 2006, Genetic interaction between alpha4 and beta2 subunits of high affinity nicotinic receptor: analysis in schizophrenia., Exp Brain Res
Hoft NR et al., 2011, CHRNB2 promoter region: association with subjective effects to nicotine and gene expression differences., Genes Brain Behav
Matera C et al., 2015, Bifunctional compounds targeting both D2 and non-α7 nACh receptors: design, synthesis and pharmacological characterization., Eur J Med Chem
Huang W et al., 2008, Significant association of DRD1 with nicotine dependence., Hum Genet
Klaassen et al., 2006, Seizures and enhanced cortical GABAergic inhibition in two mouse models of human autosomal dominant nocturnal frontal lobe epilepsy., Proc. Natl. Acad. Sci. U.S.A.
Espeseth et al., 2007, Nicotine receptor gene CHRNA4 modulates early event-related potentials in auditory and visual oddball target detection tasks., Neuroscience
Winterer et al., 2007, Association of attentional network function with exon 5 variations of the CHRNA4 gene., Hum. Mol. Genet.
Gu F et al., 2020, Association Between Nicotine-dependent Gene Polymorphism and Smoking Cessation in Patients With Lung Cancer., Clin Lung Cancer
Chu CJ et al., 2011, Association of nicotinic acetylcholine receptor subunit alpha-4 polymorphisms with smoking behaviors in Chinese male smokers., Chin Med J (Engl)
Breitling LP et al., 2009, Association of nicotinic acetylcholine receptor subunit alpha 4 polymorphisms with nicotine dependence in 5500 Germans., Pharmacogenomics J
Li MD et al., 2005, Ethnic- and gender-specific association of the nicotinic acetylcholine receptor alpha4 subunit gene (CHRNA4) with nicotine dependence., Hum Mol Genet
Teitelbaum AM et al., 2018, Nicotine dependence is associated with functional variation in FMO3, an enzyme that metabolizes nicotine in the brain., Pharmacogenomics J
Ghosheh et al., 2002, N-glucuronidation of nicotine and cotinine in human: formation of cotinine glucuronide in liver microsomes and lack of catalysis by 10 examined UDP-glucuronosyltransferases., Drug Metab. Dispos.
Mobascher A et al., 2010, Association of a variant in the muscarinic acetylcholine receptor 2 gene (CHRM2) with nicotine addiction., Am J Med Genet B Neuropsychiatr Genet
Ichino et al., 2002, Increase of transcriptional levels of egr-1 and nur77 genes due to both nicotine treatment and withdrawal in pheochromocytoma cells., J Neural Transm (Vienna)
Chen et al., 2002, Nicotine modulates the effects of retinoids on growth inhibition and RAR beta expression in lung cancer cells., Int. J. Cancer
Bloom AJ et al., 2013, The contribution of common UGT2B10 and CYP2A6 alleles to variation in nicotine glucuronidation among European Americans., Pharmacogenet Genomics
Chen G et al., 2008, Identification of a prevalent functional missense polymorphism in the UGT2B10 gene and its association with UGT2B10 inactivation against tobacco-specific nitrosamines., Pharmacogenet Genomics
Chen G et al., 2007, Glucuronidation of nicotine and cotinine by UGT2B10: loss of function by the UGT2B10 Codon 67 (Asp>Tyr) polymorphism., Cancer Res
Choi HD et al., 2015, Association between catechol-O-methyltransferase (COMT) Val/Met genotype and smoking cessation treatment with nicotine: a meta-analysis., Pharmacogenomics
Sun H et al., 2012, Association of functional COMT Val108/Met polymorphism with smoking cessation in a nicotine replacement therapy., J Neural Transm (Vienna)
Munafò MR et al., 2008, Association of COMT Val108/158Met genotype with smoking cessation., Pharmacogenet Genomics
Beuten J et al., 2006, Significant association of catechol-O-methyltransferase (COMT) haplotypes with nicotine dependence in male and female smokers of two ethnic populations., Neuropsychopharmacology
David SP et al., 2002, No association between functional catechol O-methyl transferase 1947A>G polymorphism and smoking initiation, persistent smoking or smoking cessation., Pharmacogenetics
Ray R et al., 2007, Genetic variation in mu-opioid-receptor-interacting proteins and smoking cessation in a nicotine replacement therapy trial., Nicotine Tob Res
Kumondai M et al., 2018, Functional characterization of 9 CYP2A13 allelic variants by assessment of nicotine C-oxidation and coumarin 7-hydroxylation., Drug Metab Pharmacokinet
Shin-young et al., 2007, Nicotine inhibits bFGF-induced neurite outgrowth through suppression of NO synthesis in H19-7 cells., Neurochem. Res.
Kaur-Knudsen D et al., 2014, CHRNA3 and CYP3A5*3 genotype, lung function and chronic obstructive pulmonary disease in the general population., Pharmacogenet Genomics
Winterer G et al., 2010, Risk gene variants for nicotine dependence in the CHRNA5-CHRNA3-CHRNB4 cluster are associated with cognitive performance., Am J Med Genet B Neuropsychiatr Genet
Audrain-McGovern et al., 2004, Interacting effects of genetic predisposition and depression on adolescent smoking progression., Am J Psychiatry
Wuenschell et al., 2004, Nicotine-responsive genes in cultured embryonic mouse lung buds: interaction of nicotine and superoxide dismutase., Pharmacol. Res.
Garcia KL et al., 2015, Effect of Brain CYP2B Inhibition on Brain Nicotine Levels and Nicotine Self-Administration., Neuropsychopharmacology
Ring HZ et al., 2007, Gene-gene interactions between CYP2B6 and CYP2A6 in nicotine metabolism., Pharmacogenet Genomics
Johnstone E et al., 2006, Determinants of the rate of nicotine metabolism and effects on smoking behavior., Clin Pharmacol Ther
Lang T et al., 2001, Extensive genetic polymorphism in the human CYP2B6 gene with impact on expression and function in human liver., Pharmacogenetics
Zanger UM et al., 2007, Polymorphic CYP2B6: molecular mechanisms and emerging clinical significance., Pharmacogenomics
Genbacev et al., Disruption of oxygen-regulated responses underlies pathological changes in the placentas of women who smoke or who are passively exposed to smoke during pregnancy., Reprod. Toxicol.
Pandey et al., 2001, Effects of protracted nicotine exposure and withdrawal on the expression and phosphorylation of the CREB gene transcription factor in rat brain., J. Neurochem.
Lee et al., 2005, Effects of nicotine on proliferation, cell cycle, and differentiation in immortalized and malignant oral keratinocytes., J. Oral Pathol. Med.
Onoda et al., 2001, Nicotine affects the signaling of the death pathway, reducing the response of head and neck cancer cell lines to DNA damaging agents., Head Neck
Gold AB et al., 2012, Pharmacogenetic association of the galanin receptor (GALR1) SNP rs2717162 with smoking cessation., Neuropsychopharmacology
Lori A et al., 2011, The galanin receptor 1 gene associates with tobacco craving in smokers seeking cessation treatment., Neuropsychopharmacology
Sullivan et al., 2004, Candidate genes for nicotine dependence via linkage, epistasis, and bioinformatics., Am. J. Med. Genet. B Neuropsychiatr. Genet.
Stapleton JA et al., 2011, Association between DRD2/ANKK1 Taq1A genotypes, depression and smoking cessation with nicotine replacement therapy., Pharmacogenet Genomics
Munafò MR et al., 2009, Lack of association of DRD2 rs1800497 (Taq1A) polymorphism with smoking cessation in a nicotine replacement therapy randomized trial., Nicotine Tob Res
Johnstone EC et al., 2004, Genetic variation in dopaminergic pathways and short-term effectiveness of the nicotine patch., Pharmacogenetics
Türkan H et al., 2019, The association between the OPRM1 A118G polymorphism and addiction in a Turkish population., Arh Hig Rada Toksikol
Chen YT et al., 2013, OPRM1 genetic polymorphisms are associated with the plasma nicotine metabolite cotinine concentration in methadone maintenance patients: a cross sectional study., J Hum Genet
Kleinjan M et al., 2013, Dual growth of adolescent smoking and drinking: evidence for an interaction between the mu-opioid receptor (OPRM1) A118G polymorphism and sex., Addict Biol
Munafò MR et al., 2007, Association of the mu-opioid receptor gene with smoking cessation., Pharmacogenomics J
Ray R et al., 2006, Association of OPRM1 A118G variant with the relative reinforcing value of nicotine., Psychopharmacology (Berl)
Arias A et al., 2006, Association of an Asn40Asp (A118G) polymorphism in the mu-opioid receptor gene with substance dependence: a meta-analysis., Drug Alcohol Depend
Lerman C et al., 2004, The functional mu opioid receptor (OPRM1) Asn40Asp variant predicts short-term response to nicotine replacement therapy in a clinical trial., Pharmacogenomics J
Schinka JA et al., 2002, A functional polymorphism within the mu-opioid receptor gene and risk for abuse of alcohol and other substances., Mol Psychiatry
Serres et al., 2006, Nicotine regulates SH-SY5Y neuroblastoma cell proliferation through the release of brain-derived neurotrophic factor., Brain Res.
Bui et al., 1995, Comparative effects of 6-week nicotine treatment on blood pressure and components of the antioxidant system in male spontaneously hypertensive (SHR) and normotensive Wistar Kyoto (WKY) rats., Toxicology
Lerman C et al., 2006, Role of functional genetic variation in the dopamine D2 receptor (DRD2) in response to bupropion and nicotine replacement therapy for tobacco dependence: results of two randomized clinical trials., Neuropsychopharmacology
Cinciripini P et al., 2004, The effects of the DRD2 polymorphism on smoking cessation and negative affect: evidence for a pharmacogenetic effect on mood., Nicotine Tob Res
Wang et al., 2005, P-glycoprotein does not actively transport nicotine and cotinine., Addict Biol
Tiili EM et al., 2015, Effect of genotype and methylation of CYP2D6 on smoking behaviour., Pharmacogenet Genomics
Miller RT et al., 2014, Ethanol self-administration and nicotine treatment increase brain levels of CYP2D in African green monkeys., Br J Pharmacol
Yu Y et al., 2006, Intronic variants in the dopa decarboxylase (DDC) gene are associated with smoking behavior in European-Americans and African-Americans., Hum Mol Genet
Lee et al., An in vitro bioassay for xenobiotics using the SXR-driven human CYP3A4/lacZ reporter gene., Int. J. Toxicol.
Armstrong et al., 1996, Nicotine enhances expression of the neutrophil elastase gene and protein in a human myeloblast/promyelocyte cell line., Am. J. Respir. Crit. Care Med.
Cucina et al., 1999, Nicotine regulates basic fibroblastic growth factor and transforming growth factor beta1 production in endothelial cells., Biochem. Biophys. Res. Commun.
Zhong et al., 2008, Presynaptic type III neuregulin 1 is required for sustained enhancement of hippocampal transmission by nicotine and for axonal targeting of alpha7 nicotinic acetylcholine receptors., J. Neurosci.
Dasgupta et al., 2006, Nicotine inhibits apoptosis induced by chemotherapeutic drugs by up-regulating XIAP and survivin., Proc. Natl. Acad. Sci. U.S.A.
Ma JZ et al., 2010, Significant association of glutamate receptor, ionotropic N-methyl-D-aspartate 3A (GRIN3A), with nicotine dependence in European- and African-American smokers., Hum Genet
Greiff et al., 1991, [Significant effects on alpha-fetoprotein (AFP) concentration in maternal serum in pregnancy]., Zentralbl Gynakol
Frazer-Abel et al., 2004, Nicotine activates nuclear factor of activated T cells c2 (NFATc2) and prevents cell cycle entry in T cells., J. Pharmacol. Exp. Ther.

NICOTINE HINT1

Interaction Score: 2.6

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17978999

Sources:
PharmGKB
NICOTINE UGT2B10

Interaction Score: 2.6

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24192532 18300939 17909004

Sources:
PharmGKB
NICOTINE CHRNA9

Interaction Score: 2.28

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
11006350 19560048 20400469 20081230

Sources:
TdgClinicalTrial TEND GuideToPharmacology
NICOTINE CHRNA10

Interaction Score: 1.52

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Direct Interaction? False

PMIDs:
11006350 19560048 20400469 20081230

Sources:
TdgClinicalTrial TEND GuideToPharmacology
NICOTINE CYP2A13

Interaction Score: 1.3

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29342418

Sources:
PharmGKB
NICOTINE CHRNB2

Interaction Score: 1.06

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor; alpha4/beta2 agonist

Direct Interaction yes

Trial Name -

PMIDs:
17226798 19560048 20081230 11006350 16636791 20400469 20854418 26164842

Sources:
DTC TdgClinicalTrial ChemblInteractions TEND PharmGKB

NICOTINE CHRNA4

Interaction Score: 0.7

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Details of the Assay for Interaction <i>In vitro</i> affinity for recombinant human α4β2 receptors in membranes from transfected CHO-K1 cells, determined by displacement of [<sup>3</sup>H]-(−)-cytisine.

Specific Action of the Ligand Agonist

Details of Interaction α4β2

NICOTINE DDC

Interaction Score: 0.65

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16740595

Sources:
PharmGKB
NICOTINE EPB41

Interaction Score: 0.65

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
NICOTINE ADGRL3

Interaction Score: 0.65

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
NICOTINE CREB1

Interaction Score: 0.65

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11331423

Sources:
NCI
NICOTINE CHRNB4

Interaction Score: 0.6

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
20886544 11006350 19560048 20400469 20081230

Sources:
PharmGKB
NICOTINE CHRNA3

Interaction Score: 0.59

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Details of Interaction α3β4

Endogenous Drug? False

PMIDs:
11006350 19560048 20400469 20081230 31402126 24535486 20886544

Sources:
GuideToPharmacology PharmGKB
NICOTINE GALR1

Interaction Score: 0.56

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22373943 21430647

Sources:
PharmGKB
NICOTINE CHRNA2

Interaction Score: 0.46

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
15048644 11006350 19560048 20400469 20081230

Sources:
TdgClinicalTrial TEND
NICOTINE FMO1

Interaction Score: 0.43

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
NICOTINE ANKK1

Interaction Score: 0.43

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21540761 19273465 15077009

Sources:
PharmGKB
NICOTINE NR4A1

Interaction Score: 0.39

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12111438 11979430

Sources:
NCI
NICOTINE FMO3

Interaction Score: 0.33

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28290528

Sources:
PharmGKB
NICOTINE CHRNA7

Interaction Score: 0.3

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
19560048 20081230 17360707 11006350 16754836 20400469 20231857

Sources:
TdgClinicalTrial TEND PharmGKB
NICOTINE ELANE

Interaction Score: 0.29

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8912774

Sources:
NCI
NICOTINE UGT1A7

Interaction Score: 0.29

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12167564

Sources:
NCI
NICOTINE COMT

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26555332 22695756 18192898 16395295 11927842

Sources:
PharmGKB
NICOTINE AFP

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
1711749

Sources:
NCI
NICOTINE CP

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
7740554

Sources:
NCI
NICOTINE UGT1A4

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
14570768

Sources:
NCI
NICOTINE POR

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
NICOTINE E2F1

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16601104

Sources:
NCI
NICOTINE NTF3

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17268847

Sources:
NCI
NICOTINE CYP2B6

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25652250 18004205 17015050 11470993 17638512

Sources:
PharmGKB
NICOTINE VHL

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
14555188

Sources:
NCI
NICOTINE CDKN1A

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16011614

Sources:
NCI
NICOTINE NRG1

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18784291

Sources:
NCI
NICOTINE HTR3B

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
NICOTINE DDIT3

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11592233

Sources:
NCI
NICOTINE OPRM1

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31246565 23223006 22260295 17224915 16960700 16387451 15007373 11840318

Sources:
PharmGKB
NICOTINE GRIN3A

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20084518

Sources:
PharmGKB
NICOTINE CDK4

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15231866

Sources:
NCI
NICOTINE TGFB1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10198208

Sources:
NCI
NICOTINE BAX

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15225679

Sources:
NCI
NICOTINE TRPA1

Interaction Score: 0.05

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Details of the Assay for Interaction Patch clamp

Specific Action of the Ligand Activation

Details of Interaction non-covalent

PMIDs:
None found

Sources:
GuideToPharmacology
NICOTINE SLC6A3

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15229055

Sources:
NCI
NICOTINE BDNF

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16790237

Sources:
NCI
NICOTINE CHRM2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19644963

Sources:
PharmGKB
NICOTINE DRD2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16123753 15203796

Sources:
PharmGKB
NICOTINE DRD1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18092181

Sources:
PharmGKB
NICOTINE ABCB1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16191663

Sources:
NCI
NICOTINE CYP2D6

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26287939 24611668

Sources:
PharmGKB
NICOTINE CYP3A4

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12851153

Sources:
NCI

TEND: NICOTINE
- Version: 01-August-2011
Alternate Names:

Drug Info:

Drug Class central nervous system stimulants

Year of Approval 1996

Publications:
TdgClinicalTrial: NICOTINE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications Central Nervous System Stimulants

Drug Class small molecule

FDA Approval 1996

Publications:

NCI: NICOTINE

Version: 14-September-2017

Alternate Names:

C691 NCI drug code

Drug Info:

Publications:

Ghosheh et al., 2002, N-glucuronidation of nicotine and cotinine in human: formation of cotinine glucuronide in liver microsomes and lack of catalysis by 10 examined UDP-glucuronosyltransferases., Drug Metab. Dispos.

Ichino et al., 2002, Increase of transcriptional levels of egr-1 and nur77 genes due to both nicotine treatment and withdrawal in pheochromocytoma cells., J Neural Transm (Vienna)

Chen et al., 2002, Nicotine modulates the effects of retinoids on growth inhibition and RAR beta expression in lung cancer cells., Int. J. Cancer

DTC: NICOTINE
- Version: 02-September-2020
Alternate Names:

CHEMBL3 ChEMBL Drug ID

Drug Info:

Publications:

Matera C et al., 2015, Bifunctional compounds targeting both D2 and non-α7 nACh receptors: design, synthesis and pharmacological characterization., Eur J Med Chem

PharmGKB: nicotine

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Huang W et al., 2008, Significant association of DRD1 with nicotine dependence., Hum Genet

Teitelbaum AM et al., 2018, Nicotine dependence is associated with functional variation in FMO3, an enzyme that metabolizes nicotine in the brain., Pharmacogenomics J

Mobascher A et al., 2010, Association of a variant in the muscarinic acetylcholine receptor 2 gene (CHRM2) with nicotine addiction., Am J Med Genet B Neuropsychiatr Genet

TTD: Nicotine
- Version: 2020.06.01
Alternate Names:

D0T8GD TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL3
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL3
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
GuideToPharmacology: 53801040
- Version: 29-September-2020
Alternate Names:

Drug Info:

Publications:

Trial Name	-
Novel drug target	Established target
Specific Action of the Ligand	Antagonist

Mechanism of Interaction	Neuronal acetylcholine receptor; alpha4/beta2 agonist
Direct Interaction	yes
Trial Name	-

Details of the Assay for Interaction	<i>In vitro</i> affinity for recombinant human α4β2 receptors in membranes from transfected CHO-K1 cells, determined by displacement of [<sup>3</sup>H]-(−)-cytisine.
Specific Action of the Ligand	Agonist
Details of Interaction	α4β2

Details of the Assay for Interaction	Patch clamp
Specific Action of the Ligand	Activation
Details of Interaction	non-covalent

agonist (activating)
antagonist (inhibitory)

agonist (activating)
antagonist (inhibitory)

NICOTINE Drug Record

NICOTINE chembl:CHEMBL3 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17978999

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24192532 18300939 17909004

Sources: PharmGKB

Interaction Types & Directionality: agonist (activating) antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target Specific Action of the Ligand Antagonist

PMIDs: 11006350 19560048 20400469 20081230

Sources: TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality: agonist (activating) antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target Direct Interaction? False

PMIDs: 11006350 19560048 20400469 20081230

Sources: TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 29342418

Sources: PharmGKB

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Neuronal acetylcholine receptor; alpha4/beta2 agonist Direct Interaction yes Trial Name -

PMIDs: 17226798 19560048 20081230 11006350 16636791 20400469 20854418 26164842

Sources: DTC TdgClinicalTrial ChemblInteractions TEND PharmGKB

Interaction Types & Directionality: agonist (activating)

PMIDs: 17146052 17226798 19560048 20081230 17590520 17613539 11006350 16636791 20400469 31402126 21740768 20854418 19290018 15790597 26164842

Sources: DTC TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16740595

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 11331423

Sources: NCI

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 20886544 11006350 19560048 20400469 20081230

Sources: PharmGKB

Interaction Types & Directionality: agonist (activating)

Interaction Info: Specific Action of the Ligand Agonist Details of Interaction &alpha;3&beta;4 Endogenous Drug? False

PMIDs: 11006350 19560048 20400469 20081230 31402126 24535486 20886544

Sources: GuideToPharmacology PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22373943 21430647

Sources: PharmGKB

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 15048644 11006350 19560048 20400469 20081230

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21540761 19273465 15077009

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12111438 11979430

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28290528

Sources: PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
17978999

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
24192532 18300939 17909004

Sources:
PharmGKB

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
11006350 19560048 20400469 20081230

Sources:
TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Direct Interaction? False

PMIDs:
11006350 19560048 20400469 20081230

Sources:
TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
29342418

Sources:
PharmGKB

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor; alpha4/beta2 agonist

Direct Interaction yes

Trial Name -

PMIDs:
17226798 19560048 20081230 11006350 16636791 20400469 20854418 26164842

Sources:
DTC TdgClinicalTrial ChemblInteractions TEND PharmGKB

Interaction Types & Directionality:

agonist (activating)

PMIDs:
17146052 17226798 19560048 20081230 17590520 17613539 11006350 16636791 20400469 31402126 21740768 20854418 19290018 15790597 26164842

Sources:
DTC TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD

Interaction Types & Directionality:

n/a

PMIDs:
16740595

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
11331423

Sources:
NCI

Interaction Types & Directionality:

agonist (activating)

PMIDs:
20886544 11006350 19560048 20400469 20081230

Sources:
PharmGKB

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Details of Interaction α3β4

Endogenous Drug? False

PMIDs:
11006350 19560048 20400469 20081230 31402126 24535486 20886544

Sources:
GuideToPharmacology PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
22373943 21430647

Sources:
PharmGKB

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
15048644 11006350 19560048 20400469 20081230

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
21540761 19273465 15077009

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
12111438 11979430

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
28290528

Sources:
PharmGKB

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
19560048 20081230 17360707 11006350 16754836 20400469 20231857

Sources:
TdgClinicalTrial TEND PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
8912774

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
12167564

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
26555332 22695756 18192898 16395295 11927842

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
1711749

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
7740554