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
Drug Categories	ganglionic stimulants
Drug Categories	drugs used in nicotine dependence
Drug Categories	drugs used in addictive disorders
Drug Categories	cytochrome p-450 cyp2e1 inhibitors (moderate)
Drug Categories	cytochrome p-450 cyp1a2 inducers
Drug Categories	agents producing tachycardia
Drug Categories	cholinergic nicotinic agonist
Drug Categories	cytochrome p-450 cyp1a2 inducers (strength unknown)
Drug Categories	cytochrome p-450 cyp2a6 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp2e1 inducers
Drug Categories	cytochrome p-450 cyp2e1 inducers (strength unknown)
Drug Categories	cytochrome p-450 cyp2e1 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 enzyme inducers
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	ganglion blockers
Drug Categories	miscellaneous autonomic drugs
Drug Categories	monoamine oxidase a inhibitors for interaction with monoamine oxidase a substrates
Drug Categories	nicotine, antagonists & inhibitors
Drug Categories	nicotine, metabolism
Drug Categories	oct1 inhibitors
Drug Categories	oct2 inhibitors
Drug Categories	smoking cessation agents

(6 More Sources)

Publications:

Olincy et al., 2006, Proof-of-concept trial of an alpha7 nicotinic agonist in schizophrenia., Arch. Gen. Psychiatry
Mansvelder et al., 2009, Nicotinic modulation of synaptic transmission and plasticity in cortico-limbic circuits., Semin. Cell Dev. Biol.
Narahashi et al., 2000, Symposium overview: mechanism of action of nicotine on neuronal acetylcholine receptors, from molecule to behavior., Toxicol. Sci.
Rigbi A et al., 2011, Why do young women smoke? VI. A controlled study of nicotine effects on attention: pharmacogenetic interactions., Pharmacogenomics J
Mexal et al., 2007, alpha7 nicotinic receptor gene promoter polymorphisms in inbred mice affect expression in a cell type-specific fashion., J. Biol. Chem.
Jackson et al., 2010, Role of alpha5 nicotinic acetylcholine receptors in pharmacological and behavioral effects of nicotine in mice., J. Pharmacol. Exp. Ther.
Zaniewska et al., Nicotine dependence - human and animal studies, current pharmacotherapies and future perspectives., Pharmacol Rep
Kuehl et al., 2003, N-glucuronidation of nicotine and cotinine by human liver microsomes and heterologously expressed UDP-glucuronosyltransferases., Drug Metab. Dispos.
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
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.
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
Espeseth et al., 2007, Nicotine receptor gene CHRNA4 modulates early event-related potentials in auditory and visual oddball target detection tasks., Neuroscience
Breitling LP et al., 2009, Association of nicotinic acetylcholine receptor subunit alpha 4 polymorphisms with nicotine dependence in 5500 Germans., Pharmacogenomics J
Winterer et al., 2007, Association of attentional network function with exon 5 variations of the CHRNA4 gene., Hum. Mol. Genet.
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
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.
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)
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
FAHMY et al., 1954, The inhibition of choline acetylase by nicotine., J. Pharm. Pharmacol.
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
Bloom AJ et al., 2013, The contribution of common UGT2B10 and CYP2A6 alleles to variation in nicotine glucuronidation among European Americans., Pharmacogenet Genomics
Munafò MR et al., 2008, Association of COMT Val108/158Met genotype with smoking cessation., Pharmacogenet Genomics
Sun H et al., 2012, Association of functional COMT Val108/Met polymorphism with smoking cessation in a nicotine replacement therapy., J Neural Transm (Vienna)
Choi HD et al., 2015, Association between catechol-O-methyltransferase (COMT) Val/Met genotype and smoking cessation treatment with nicotine: a meta-analysis., Pharmacogenomics
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
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
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.
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
Kaur-Knudsen D et al., 2014, CHRNA3 and CYP3A5*3 genotype, lung function and chronic obstructive pulmonary disease in the general population., Pharmacogenet Genomics
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.
Johnstone E et al., 2006, Determinants of the rate of nicotine metabolism and effects on smoking behavior., Clin Pharmacol Ther
Zanger UM et al., 2007, Polymorphic CYP2B6: molecular mechanisms and emerging clinical significance., Pharmacogenomics
Lang T et al., 2001, Extensive genetic polymorphism in the human CYP2B6 gene with impact on expression and function in human liver., Pharmacogenetics
Ring HZ et al., 2007, Gene-gene interactions between CYP2B6 and CYP2A6 in nicotine metabolism., Pharmacogenet Genomics
Garcia KL et al., 2015, Effect of Brain CYP2B Inhibition on Brain Nicotine Levels and Nicotine Self-Administration., Neuropsychopharmacology
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.
Barbieri et al., 1986, Nicotine, cotinine, and anabasine inhibit aromatase in human trophoblast in vitro., J. Clin. Invest.
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
Lori A et al., 2011, The galanin receptor 1 gene associates with tobacco craving in smokers seeking cessation treatment., Neuropsychopharmacology
Gold AB et al., 2012, Pharmacogenetic association of the galanin receptor (GALR1) SNP rs2717162 with smoking cessation., 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
Johnstone EC et al., 2004, Genetic variation in dopaminergic pathways and short-term effectiveness of the nicotine patch., Pharmacogenetics
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
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
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
Munafò MR et al., 2007, Association of the mu-opioid receptor gene with smoking cessation., Pharmacogenomics J
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
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
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
Türkan H et al., 2019, The association between the OPRM1 A118G polymorphism and addiction in a Turkish population., Arh Hig Rada Toksikol
Ray R et al., 2006, Association of OPRM1 A118G variant with the relative reinforcing value of nicotine., Psychopharmacology (Berl)
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 CHRNB3

Interaction Score: 2.63

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
19560048 11006350 20400469 20081230

Sources:
DrugBank
NICOTINE UGT2B10

Interaction Score: 2.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18300939 17909004 24192532

Sources:
PharmGKB
NICOTINE CHRNA9

Interaction Score: 1.2

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
19560048 11006350 20400469 20081230

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
NICOTINE CHRNA5

Interaction Score: 1.05

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
19560048 11006350 20400469 20081230

Sources:
DrugBank
NICOTINE CYP2A13

Interaction Score: 1.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29342418

Sources:
PharmGKB
NICOTINE CHRNA10

Interaction Score: 0.77

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Direct Interaction? False

PMIDs:
19560048 11006350 20400469 20081230

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
NICOTINE CHRNA6

Interaction Score: 0.75

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
19560048 11006350 20400469 20081230

Sources:
DrugBank
NICOTINE CHRNB2

Interaction Score: 0.55

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor; alpha4/beta2 agonist

Direct Interaction yes

Trial Name -

PMIDs:
16636791 20854418 19560048 17226798 11006350 26164842 20400469 20081230

Sources:
TEND DTC PharmGKB TdgClinicalTrial DrugBank ChemblInteractions
NICOTINE EPB41

Interaction Score: 0.53

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
NICOTINE ADGRL3

Interaction Score: 0.53

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
NICOTINE HINT1

Interaction Score: 0.53

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17978999

Sources:
PharmGKB
NICOTINE GALR1

Interaction Score: 0.45

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21430647 22373943

Sources:
PharmGKB

NICOTINE CHRNA4

Interaction Score: 0.42

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 CHRNB4

Interaction Score: 0.41

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
19560048 11006350 20886544 20400469 20081230

Sources:
PharmGKB DrugBank
NICOTINE CHRNA3

Interaction Score: 0.35

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Details of Interaction α3β4

Endogenous Drug? False

PMIDs:
19560048 11006350 20886544 24535486 31402126 20400469 20081230

Sources:
PharmGKB DrugBank GuideToPharmacology
NICOTINE FMO1

Interaction Score: 0.35

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
NICOTINE DDC

Interaction Score: 0.35

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16740595

Sources:
PharmGKB
NICOTINE CREB1

Interaction Score: 0.35

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11331423

Sources:
NCI
NICOTINE ANKK1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21540761 15077009 19273465

Sources:
PharmGKB
NICOTINE NR4A1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12111438 11979430

Sources:
NCI
NICOTINE CHRNA2

Interaction Score: 0.31

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
19560048 11006350 20400469 20081230 15048644

Sources:
TEND TdgClinicalTrial DrugBank
NICOTINE FMO3

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28290528

Sources:
PharmGKB
NICOTINE UGT1A7

Interaction Score: 0.23

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12167564

Sources:
NCI
NICOTINE ELANE

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8912774

Sources:
NCI
NICOTINE CHAT

Interaction Score: 0.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
13192619

Sources:
DrugBank
NICOTINE CHRNA7

Interaction Score: 0.18

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
16754836 19560048 11006350 20231857 17360707 20400469 20081230

Sources:
TEND PharmGKB TdgClinicalTrial DrugBank
NICOTINE AFP

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
1711749

Sources:
NCI
NICOTINE COMT

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18192898 22695756 26555332 11927842 16395295

Sources:
PharmGKB
NICOTINE UGT1A4

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
14570768

Sources:
NCI
NICOTINE E2F1

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16601104

Sources:
NCI
NICOTINE NTF3

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17268847

Sources:
NCI
NICOTINE VHL

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
14555188

Sources:
NCI
NICOTINE CYP2B6

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17015050 17638512 11470993 18004205 25652250

Sources:
PharmGKB
NICOTINE CDKN1A

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16011614

Sources:
NCI
NICOTINE CP

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
7740554

Sources:
NCI
NICOTINE POR

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
NICOTINE NRG1

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18784291

Sources:
NCI
NICOTINE DDIT3

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11592233

Sources:
NCI
NICOTINE HTR3B

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
NICOTINE OPRM1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22260295 15007373 17224915 23223006 11840318 16387451 31246565 16960700

Sources:
PharmGKB
NICOTINE CDK4

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15231866

Sources:
NCI
NICOTINE GRIN3A

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20084518

Sources:
PharmGKB
NICOTINE TGFB1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10198208

Sources:
NCI
NICOTINE CYP19A1

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
3711333

Sources:
DrugBank
NICOTINE BAX

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15225679

Sources:
NCI
NICOTINE BDNF

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16790237

Sources:
NCI
NICOTINE TRPA1

Interaction Score: 0.03

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: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15229055

Sources:
NCI
NICOTINE CHRM2

Interaction Score: 0.02

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: 0.01

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

DrugBank: DB00184

Version: 5.1.7

Alternate Names:

54-11-5 CAS Number

American Fare Nicotine Transdermal System Drug Brand

Basic Care Nicotine Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories agents producing tachycardia

Publications:

Olincy et al., 2006, Proof-of-concept trial of an alpha7 nicotinic agonist in schizophrenia., Arch. Gen. Psychiatry

Mansvelder et al., 2009, Nicotinic modulation of synaptic transmission and plasticity in cortico-limbic circuits., Semin. Cell Dev. Biol.

Narahashi et al., 2000, Symposium overview: mechanism of action of nicotine on neuronal acetylcholine receptors, from molecule to behavior., Toxicol. Sci.

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

54-11-5	CAS Number
American Fare Nicotine Transdermal System	Drug Brand
Basic Care Nicotine	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Categories	agents producing tachycardia

agonist (activating)
antagonist (inhibitory)

agonist (activating)
antagonist (inhibitory)

NICOTINE Drug Record

NICOTINE chembl:CHEMBL3 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 19560048 11006350 20400469 20081230

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18300939 17909004 24192532

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: 19560048 11006350 20400469 20081230

Sources: TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 19560048 11006350 20400469 20081230

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 29342418

Sources: PharmGKB

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

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

PMIDs: 19560048 11006350 20400469 20081230

Sources: TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 19560048 11006350 20400469 20081230

Sources: DrugBank

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 16636791 20854418 19560048 17226798 11006350 26164842 20400469 20081230

Sources: TEND DTC PharmGKB TdgClinicalTrial DrugBank ChemblInteractions

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: 17978999

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21430647 22373943

Sources: PharmGKB

Interaction Types & Directionality: agonist (activating)

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

Sources: TEND DTC PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 19560048 11006350 20886544 20400469 20081230

Sources: PharmGKB DrugBank

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 19560048 11006350 20886544 24535486 31402126 20400469 20081230

Sources: PharmGKB DrugBank GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16740595

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 11331423

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21540761 15077009 19273465

Sources: PharmGKB

Interaction Types & Directionality:

agonist (activating)

PMIDs:
19560048 11006350 20400469 20081230

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
18300939 17909004 24192532

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:
19560048 11006350 20400469 20081230

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

PMIDs:
19560048 11006350 20400469 20081230

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
29342418

Sources:
PharmGKB

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Direct Interaction? False

PMIDs:
19560048 11006350 20400469 20081230

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

PMIDs:
19560048 11006350 20400469 20081230

Sources:
DrugBank

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Neuronal acetylcholine receptor; alpha4/beta2 agonist

Direct Interaction yes

Trial Name -

PMIDs:
16636791 20854418 19560048 17226798 11006350 26164842 20400469 20081230

Sources:
TEND DTC PharmGKB TdgClinicalTrial DrugBank ChemblInteractions

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:
17978999

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
21430647 22373943

Sources:
PharmGKB

Interaction Types & Directionality:

agonist (activating)

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

Sources:
TEND DTC PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

PMIDs:
19560048 11006350 20886544 20400469 20081230

Sources:
PharmGKB DrugBank

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Details of Interaction α3β4

Endogenous Drug? False

PMIDs:
19560048 11006350 20886544 24535486 31402126 20400469 20081230

Sources:
PharmGKB DrugBank GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
16740595

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
11331423

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
21540761 15077009 19273465

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
12111438 11979430

Sources:
NCI

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
19560048 11006350 20400469 20081230 15048644

Sources:
TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
28290528

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
12167564

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
8912774

Sources:
NCI

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
13192619

Sources:
DrugBank