DGIdb - SLC6A2 Gene Record

SLC6A2 6530 Druggable GenomeDrug Resistance

Alternate Names:

6530
SOLUTE CARRIER FAMILY 6 MEMBER 2
SLC6A2
NAT1
NET
NET1
SLC6A5
163970
11048
ENSG00000103546
OTTHUMG00000133208
P23975
SC6A2_HUMAN
926
BE0000486
PA310
SODIUM-DEPENDENT NORADRENALINE TRANSPORTER (NOREPINEPHRINE TRANSPORTER) (NET). [SOURCE:UNIPROT/SWISSPROT;ACC:P23975]
SODIUM-DEPENDENT NORADRENALINE TRANSPORTER
Norepinephrine transporter
SLCA2

Gene Info:

Human Readable Name	DRUGGABLE GENOME
Target Subclass	Other
Target Subclass	SLC
Target Subclass	SLC6
Target Main Class	Transporters
Transmembrane Helix Count	12
Interpro Short Name	Na/ntran_symport
Interpro Acc	IPR000175
Uniprot Status	Swiss-Prot
Interpro Name	Sodium:neurotransmitter symporter
Human Readable Name	TRANSPORTER
Interpro Type	Family
Uniprot Evidence	1: Evidence at protein level
GuideToPharmacology Gene Category Name	Monoamine transporter subfamily
GuideToPharmacology Gene Category ID	176
Target Class	Transporters
Target Subclass	TC:2.A.22.1.2
Gene Biotype	PROTEIN_CODING

(9 More Sources)

Gene Categories: Category Details

TRANSPORTER
CELL SURFACE
DRUG RESISTANCE
DRUGGABLE GENOME

Publications:

Gillman, 2007, Tricyclic antidepressant pharmacology and therapeutic drug interactions updated., Br. J. Pharmacol.
Wille SM et al., 2008, Relevant issues in the monitoring and the toxicology of antidepressants., Crit Rev Clin Lab Sci
Arias et al., 2009, Pharmacological and neurotoxicological actions mediated by bupropion and diethylpropion., Int. Rev. Neurobiol.
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Cloonan et al., 2010, The antidepressants maprotiline and fluoxetine have potent selective antiproliferative effects against Burkitt lymphoma independently of the norepinephrine and serotonin transporters., Leuk. Lymphoma
Dronjak et al., 2007, Effects of noradrenaline and serotonin reuptake inhibitors on pituitary-adrenocortical and sympatho-adrenomedullar system of adult rats., Neuro Endocrinol. Lett.
Mochizucki, 2004, Serotonin and noradrenaline reuptake inhibitors in animal models of pain., Hum Psychopharmacol
Arai et al., 2003, Chronic inhibition of the norepinephrine transporter in the brain participates in seizure sensitization to cocaine and local anesthetics., Brain Res.
Saba et al., 2007, [11C]LBT-999: a suitable radioligand for investigation of extra-striatal dopamine transporter with PET., Synapse
Berrocoso et al., 2009, Cooperative opioid and serotonergic mechanisms generate superior antidepressant-like effects in a mice model of depression., Int. J. Neuropsychopharmacol.
Sagata et al., 2002, Tramadol inhibits norepinephrine transporter function at desipramine-binding sites in cultured bovine adrenal medullary cells., Anesth. Analg.
Frink et al., 1996, Influence of tramadol on neurotransmitter systems of the rat brain., Arzneimittelforschung
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Barakat A, 2019, Revisiting Tramadol: A Multi-Modal Agent for Pain Management., CNS Drugs
Wernicke et al., 2004, Changes in symptoms and adverse events after discontinuation of atomoxetine in children and adults with attention deficit/hyperactivity disorder: a prospective, placebo-controlled assessment., J Clin Psychopharmacol
Purper-Ouakil et al., [Atomoxetine: a new treatment for Attention Deficit/Hyperactivity Disorder (ADHD) in children and adolescents]., Encephale
Ramoz N et al., 2009, A haplotype of the norepinephrine transporter (Net) gene Slc6a2 is associated with clinical response to atomoxetine in attention-deficit hyperactivity disorder (ADHD)., Neuropsychopharmacology
Yang L et al., 2013, Adrenergic neurotransmitter system transporter and receptor genes associated with atomoxetine response in attention-deficit hyperactivity disorder children., J Neural Transm (Vienna)
Michelson et al., 2003, Atomoxetine in adults with ADHD: two randomized, placebo-controlled studies., Biol. Psychiatry
Spencer et al., 2002, Results from 2 proof-of-concept, placebo-controlled studies of atomoxetine in children with attention-deficit/hyperactivity disorder., J Clin Psychiatry
Gaillez et al., 2007, [Atomoxetine (Strattera), an alternative in the treatment of attention-deficit/hyperactivity disorder (ADHD) in children]., Encephale
Garnock-Jones et al., 2009, Atomoxetine: a review of its use in attention-deficit hyperactivity disorder in children and adolescents., Paediatr Drugs
Tatsumi et al., 1997, Pharmacological profile of antidepressants and related compounds at human monoamine transporters., Eur. J. Pharmacol.
Wernicke et al., 2003, Cardiovascular effects of atomoxetine in children, adolescents, and adults., Drug Saf
Biederman et al., 2002, Efficacy of atomoxetine versus placebo in school-age girls with attention-deficit/hyperactivity disorder., Pediatrics
Yu G et al., 2016, Atomoxetine: A Review of Its Pharmacokinetics and Pharmacogenomics Relative to Drug Disposition., J Child Adolesc Psychopharmacol
Kaplan et al., 2004, Efficacy and safety of atomoxetine in childhood attention-deficit/hyperactivity disorder with comorbid oppositional defiant disorder., J Atten Disord
Galli et al., 1995, Sodium-dependent norepinephrine-induced currents in norepinephrine-transporter-transfected HEK-293 cells blocked by cocaine and antidepressants., J. Exp. Biol.
Carrera et al., 2004, Cocaine pharmacology and current pharmacotherapies for its abuse., Bioorg. Med. Chem.
Burchett et al., 1997, Serotonin, dopamine and norepinephrine transporter mRNAs: heterogeneity of distribution and response to 'binge' cocaine administration., Brain Res. Mol. Brain Res.
Zhao et al., Perinatal cocaine exposure reduces myocardial norepinephrine transporter function in the neonatal rat., Neurotoxicol Teratol
Mitchell et al., 2006, The effects of norepinephrine transporter inactivation on locomotor activity in mice., Biol. Psychiatry
Tatsumi et al., 1999, Pharmacological profile of neuroleptics at human monoamine transporters., Eur. J. Pharmacol.
Anton et al., 2004, Use of the norepinephrine transporter as a reporter gene for non-invasive imaging of genetically modified cells., J Gene Med
Kantor et al., 2001, Protein kinase C and intracellular calcium are required for amphetamine-mediated dopamine release via the norepinephrine transporter in undifferentiated PC12 cells., J. Pharmacol. Exp. Ther.
Dziedzicka-Wasylewska et al., 2006, Effect of antidepressant drugs in mice lacking the norepinephrine transporter., Neuropsychopharmacology
Haenisch B et al., 2011, Inhibitory potencies of trimipramine and its main metabolites at human monoamine and organic cation transporters., Psychopharmacology (Berl)
Shalabi AR et al., 2017, Deconstructed Analogues of Bupropion Reveal Structural Requirements for Transporter Inhibition versus Substrate-Induced Neurotransmitter Release., ACS Chem Neurosci
Bondarev et al., 2003, Behavioral and biochemical investigations of bupropion metabolites., Eur. J. Pharmacol.
Mortensen OV et al., 2006, Gain of function mutants reveal sites important for the interaction of the atypical inhibitors benztropine and bupropion with monoamine transporters., J Neurochem
Stahl et al., 2004, A Review of the Neuropharmacology of Bupropion, a Dual Norepinephrine and Dopamine Reuptake Inhibitor., Prim Care Companion J Clin Psychiatry
Jungkun et al., 2001, Long-term effects of tricyclic antidepressants on norepinephrine kinetics in humans., J Neural Transm (Vienna)
Yi et al., 2005, Alpha-adrenergic modulation of synaptic transmission in rabbit pancreatic ganglia., Auton Neurosci
Galli et al., 1996, Norepinephrine transporters have channel modes of conduction., Proc. Natl. Acad. Sci. U.S.A.
Joyce et al., 2001, Interaction of local anaesthetic agents with the endogenous norepinephrine transporter in SH-SY5Y human neuroblastoma cells., Neurosci. Lett.
Roubert et al., 2001, A Na(+)/Cl(-)-dependent transporter for catecholamines, identified as a norepinephrine transporter, is expressed in the brain of the teleost fish medaka (Oryzias latipes)., Mol. Pharmacol.
Roubert et al., 2001, Determination of residues in the norepinephrine transporter that are critical for tricyclic antidepressant affinity., J. Biol. Chem.
Vaishnavi et al., 2004, Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity., Biol. Psychiatry
Barker et al., 1996, Identification of a single amino acid, phenylalanine 586, that is responsible for high affinity interactions of tricyclic antidepressants with the human serotonin transporter., Mol. Pharmacol.
Kim et al., 2006, Monoamine transporter gene polymorphisms and antidepressant response in koreans with late-life depression., JAMA
Mason et al., 2007, Desvenlafaxine succinate identifies novel antagonist binding determinants in the human norepinephrine transporter., J. Pharmacol. Exp. Ther.
Deecher et al., 2006, Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor., J. Pharmacol. Exp. Ther.
Perry et al., 2009, Desvenlafaxine: a new serotonin-norepinephrine reuptake inhibitor for the treatment of adults with major depressive disorder., Clin Ther
Reddy et al., 2010, Clinical utility of desvenlafaxine 50 mg/d for treating MDD: a review of two randomized placebo-controlled trials for the practicing physician., Curr Med Res Opin
Kamath et al., 2008, Desvenlafaxine succinate for major depressive disorder: a critical review of the evidence., Expert Rev Neurother
Liebowitz et al., 2010, Efficacy, safety, and tolerability of Desvenlafaxine 50 mg/d for the treatment of major depressive disorder:a systematic review of clinical trials., Prim Care Companion J Clin Psychiatry
Angyal N et al., 2018, Association analysis of norepinephrine transporter polymorphisms and methylphenidate response in ADHD patients., Prog Neuropsychopharmacol Biol Psychiatry
Kim BN et al., 2013, Norepinephrine genes predict response time variability and methylphenidate-induced changes in neuropsychological function in attention deficit hyperactivity disorder., J Clin Psychopharmacol
Myer NM et al., 2018, Pharmacogenetics predictors of methylphenidate efficacy in childhood ADHD., Mol Psychiatry
Sandoval et al., 2001, Methamphetamine-induced rapid and reversible changes in dopamine transporter function: an in vitro model., J. Neurosci.
Yang et al., 2004, Association of norepinephrine transporter gene with methylphenidate response., J Am Acad Child Adolesc Psychiatry
Williard et al., 2007, Methylphenidate and its ethanol transesterification metabolite ethylphenidate: brain disposition, monoamine transporters and motor activity., Behav Pharmacol
Chuhan et al., 2006, Impairment of single-trial memory formation by oral methylphenidate in the rat., Neurobiol Learn Mem
Hong SB et al., 2012, Dopaminergic and noradrenergic gene polymorphisms and response to methylphenidate in korean children with attention-deficit/hyperactivity disorder: is there an interaction?, J Child Adolesc Psychopharmacol
Berridge CW et al., 2006, Methylphenidate preferentially increases catecholamine neurotransmission within the prefrontal cortex at low doses that enhance cognitive function., Biol Psychiatry
Gray et al., 2007, Methylphenidate administration to juvenile rats alters brain areas involved in cognition, motivated behaviors, appetite, and stress., J. Neurosci.
Tilley et al., 2008, The effects of methylphenidate on knockin mice with a methylphenidate-resistant dopamine transporter., J. Pharmacol. Exp. Ther.
Markowitz JS et al., 2006, A comprehensive in vitro screening of d-, l-, and dl-threo-methylphenidate: an exploratory study., J Child Adolesc Psychopharmacol
Rauhut et al., 2002, Reboxetine: attenuation of intravenous nicotine self-administration in rats., J. Pharmacol. Exp. Ther.
Wilson et al., 2003, Synthesis and in vivo evaluation of novel radiotracers for the in vivo imaging of the norepinephrine transporter., Nucl. Med. Biol.
Lin et al., 2005, Synthesis, enantiomeric resolution, F-18 labeling and biodistribution of reboxetine analogs: promising radioligands for imaging the norepinephrine transporter with positron emission tomography., Nucl. Med. Biol.
Spivak et al., 2006, Reboxetine versus fluvoxamine in the treatment of motor vehicle accident-related posttraumatic stress disorder: a double-blind, fixed-dosage, controlled trial., J Clin Psychopharmacol
Kasper et al., 2000, Reboxetine: the first selective noradrenaline re-uptake inhibitor., Expert Opin Pharmacother
Dlugos et al., 2007, Norepinephrine transporter gene variation modulates acute response to D-amphetamine., Biol. Psychiatry
Dlugos et al., 2009, Further evidence of association between amphetamine response and SLC6A2 gene variants., Psychopharmacology (Berl.)
Burnette et al., 1996, Human norepinephrine transporter kinetics using rotating disk electrode voltammetry., Anal. Chem.
Larsen MH et al., 2007, Expression of brain derived neurotrophic factor, activity-regulated cytoskeleton protein mRNA, and enhancement of adult hippocampal neurogenesis in rats after sub-chronic and chronic treatment with the triple monoamine re-uptake inhibitor tesofensine., Eur J Pharmacol
Basile et al., 2007, Characterization of the antinociceptive actions of bicifadine in models of acute, persistent, and chronic pain., J. Pharmacol. Exp. Ther.
Bryson HM et al., 1996, Amitriptyline. A review of its pharmacological properties and therapeutic use in chronic pain states., Drugs Aging
Van Ameringen et al., 2009, Pharmacotherapy for social anxiety disorder: an update., Isr J Psychiatry Relat Sci
Béïque et al., 1998, Affinities of venlafaxine and various reuptake inhibitors for the serotonin and norepinephrine transporters., Eur. J. Pharmacol.
Westenberg, 2009, Recent advances in understanding and treating social anxiety disorder., CNS Spectr
Sindrup et al., 2005, Antidepressants in the treatment of neuropathic pain., Basic Clin. Pharmacol. Toxicol.
Béïque et al., 2000, Effects of sustained administration of the serotonin and norepinephrine reuptake inhibitor venlafaxine: I. in vivo electrophysiological studies in the rat., Neuropharmacology
Bymaster et al., 2001, Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors., Neuropsychopharmacology
Marshe VS et al., 2017, Norepinephrine Transporter Gene Variants and Remission From Depression With Venlafaxine Treatment in Older Adults., Am J Psychiatry
Rothman et al., 2002, Interaction of the anorectic medication, phendimetrazine, and its metabolites with monoamine transporters in rat brain., Eur. J. Pharmacol.
Rothman et al., 2006, Therapeutic potential of monoamine transporter substrates., Curr Top Med Chem
Heusser et al., 2006, Influence of sibutramine treatment on sympathetic vasomotor tone in obese subjects., Clin. Pharmacol. Ther.
Tziomalos et al., 2009, The use of sibutramine in the management of obesity and related disorders: an update., Vasc Health Risk Manag
Krahn et al., 2001, Narcolepsy and obesity: remission of severe cataplexy with sibutramine., Sleep Med.
Jordan et al., 2005, Influence of Sibutramine on blood pressure: evidence from placebo-controlled trials., Int J Obes (Lond)
Gomis Barbará, [Pharmacological treatment of obesity]., Rev Med Univ Navarra
Birkenfeld et al., 2002, Paradoxical effect of sibutramine on autonomic cardiovascular regulation., Circulation
Berke et al., 2000, Medical management of obesity., Am Fam Physician
Sharma et al., 2008, Sibutramine: current status as an anti-obesity drug and its future perspectives., Expert Opin Pharmacother
Heusser et al., 2007, Sympathetic vasomotor tone determines blood pressure response to long-term sibutramine treatment., J. Clin. Endocrinol. Metab.
Birkenfeld et al., 2005, Paradoxical effect of sibutramine on autonomic cardiovascular regulation in obese hypertensive patients--sibutramine and blood pressure., Clin. Auton. Res.
Markowitz et al., 2008, Differential pharmacokinetics and pharmacodynamics of methylphenidate enantiomers: does chirality matter?, J Clin Psychopharmacol
Ding et al., 1997, Chiral drugs: comparison of the pharmacokinetics of [11C]d-threo and L-threo-methylphenidate in the human and baboon brain., Psychopharmacology (Berl.)
Davids et al., 2002, Stereoselective effects of methylphenidate on motor hyperactivity in juvenile rats induced by neonatal 6-hydroxydopamine lesioning., Psychopharmacology (Berl.)
Foley et al., 2002, Stereospecific inhibition of monoamine uptake transporters by meta-hydroxyephedrine isomers., J Neural Transm (Vienna)
Wee et al., 2004, Reinforcing effect of pseudoephedrine isomers and the mechanism of action., Eur. J. Pharmacol.
Weinshenker et al., 2002, Regulation of norepinephrine transporter abundance by catecholamines and desipramine in vivo., Brain Res.
Paczkowski FA et al., 2007, chi-Conotoxin and tricyclic antidepressant interactions at the norepinephrine transporter define a new transporter model., J Biol Chem
Zhu et al., 2004, The persistent membrane retention of desipramine causes lasting inhibition of norepinephrine transporter function., Neurochem. Res.
Zavosh et al., 1999, Desipramine treatment decreases 3H-nisoxetine binding and norepinephrine transporter mRNA in SK-N-SHSY5Y cells., Brain Res. Bull.
Bryan-Lluka et al., 2003, chi-Conopeptide MrIA partially overlaps desipramine and cocaine binding sites on the human norepinephrine transporter., J. Biol. Chem.
Ordway et al., 2005, Norepinephrine transporter function and desipramine: residual drug effects versus short-term regulation., J. Neurosci. Methods
Fleckenstein et al., 2007, New insights into the mechanism of action of amphetamines., Annu. Rev. Pharmacol. Toxicol.
Haughey et al., 2000, Differential effects of methamphetamine on Na(+)/Cl(-)-dependent transporters., Brain Res.
Sulzer et al., 2005, Mechanisms of neurotransmitter release by amphetamines: a review., Prog. Neurobiol.
Sanchez C et al., 2014, A comparative review of escitalopram, paroxetine, and sertraline: Are they all alike?, Int Clin Psychopharmacol
Bareggi et al., 2007, The use of escitalopram beyond major depression: pharmacological aspects, efficacy and tolerability in anxiety disorders., Expert Opin Drug Metab Toxicol
Raffel et al., 2006, Dependence of cardiac 11C-meta-hydroxyephedrine retention on norepinephrine transporter density., J. Nucl. Med.
Zhao et al., 2000, Chemical synthesis and pharmacology of 6- and 7-hydroxylated 2-carbomethoxy-3-(p-tolyl)tropanes: antagonism of cocaine's locomotor stimulant effects., J. Med. Chem.
Sharpe et al., 2003, Inhibition of the norepinephrine transporter by the venom peptide chi-MrIA. Site of action, Na+ dependence, and structure-activity relationship., J. Biol. Chem.
Raffel et al., 2004, Binding of [3H]mazindol to cardiac norepinephrine transporters: kinetic and equilibrium studies., Naunyn Schmiedebergs Arch. Pharmacol.
Ritz et al., 1990, [3H]WIN 35,065-2: a ligand for cocaine receptors in striatum., J. Neurochem.
Proietto et al., 2000, Novel anti-obesity drugs., Expert Opin Investig Drugs
Stephens et al., 2005, Phentermine and anaesthesia., Anaesth Intensive Care
Samanin et al., 1993, Neurochemical mechanism of action of anorectic drugs., Pharmacol. Toxicol.
Codd et al., 1995, Serotonin and norepinephrine uptake inhibiting activity of centrally acting analgesics: structural determinants and role in antinociception., J. Pharmacol. Exp. Ther.
Rothman et al., 2001, Amphetamine-type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin., Synapse
Tzschentke et al., 2007, (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol hydrochloride (tapentadol HCl): a novel mu-opioid receptor agonist/norepinephrine reuptake inhibitor with broad-spectrum analgesic properties., J. Pharmacol. Exp. Ther.
Nemeroff et al., 2003, Neuropharmacology of paroxetine., Psychopharmacol Bull
Gilmor et al., 2002, Inhibition of norepinephrine uptake in patients with major depression treated with paroxetine., Am J Psychiatry
Rubin, 2000, Paroxetine binding to the rat norepinephrine transporter in vivo., Biol. Psychiatry
Schou et al., 2005, Post-mortem human brain autoradiography of the norepinephrine transporter using (S,S)-[18F]FMeNER-D2., Eur Neuropsychopharmacol
Carter et al., 2009, Duloxetine: a review of its use in the treatment of generalized anxiety disorder., CNS Drugs
Jost et al., 2004, Duloxetine: mechanism of action at the lower urinary tract and Onuf's nucleus., Clin. Auton. Res.
Gould et al., 2007, Effect of chronic administration of duloxetine on serotonin and norepinephrine transporter binding sites in rat brain., Biol. Psychiatry
Bymaster et al., 2005, The dual transporter inhibitor duloxetine: a review of its preclinical pharmacology, pharmacokinetic profile, and clinical results in depression., Curr. Pharm. Des.
Hunziker et al., 2005, Duloxetine hydrochloride: a new dual-acting medication for the treatment of major depressive disorder., Clin Ther
van Groeningen et al., 1989, Lack of effectiveness of combined 5-fluorouracil and leucovorin in patients with 5-fluorouracil-resistant advanced colorectal cancer., Eur J Cancer Clin Oncol
Karpa et al., 2002, Duloxetine pharmacology: profile of a dual monoamine modulator., CNS Drug Rev
Trivedi et al., 2008, Clinical evidence for serotonin and norepinephrine reuptake inhibition of duloxetine., Int Clin Psychopharmacol
Vincent et al., 2004, Clinical assessment of norepinephrine transporter blockade through biochemical and pharmacological profiles., Circulation
Khullar et al., 2010, Mixed incontinence: current evidence and future perspectives., Neurourol. Urodyn.
Mirza et al., 2007, Serotonin transporter density and anxiolytic-like effects of antidepressants in mice., Prog. Neuropsychopharmacol. Biol. Psychiatry
Cheetham et al., 1996, [3H]nisoxetine--a radioligand for noradrenaline reuptake sites: correlation with inhibition of [3H]noradrenaline uptake and effect of DSP-4 lesioning and antidepressant treatments., Neuropharmacology
Rothman et al., 2003, In vitro characterization of ephedrine-related stereoisomers at biogenic amine transporters and the receptorome reveals selective actions as norepinephrine transporter substrates., J. Pharmacol. Exp. Ther.
Pubill et al., 1999, Assessment of the adrenergic effects of orphenadrine in rat vas deferens., J. Pharm. Pharmacol.
Taylor et al., 1995, Pharmacology and neurochemistry of nefazodone, a novel antidepressant drug., J Clin Psychiatry
Owens et al., 1995, The serotonergic antidepressant nefazodone inhibits the serotonin transporter: in vivo and ex vivo studies., Life Sci.
Owen et al., 1999, Norepinephrine transporter gene polymorphism is not associated with susceptibility to major depression., Psychiatry Res
Davis et al., 1997, Nefazodone. A review of its pharmacology and clinical efficacy in the management of major depression., Drugs
Baladi MG et al., 2018, Characterization of the Neurochemical and Behavioral Effects of Solriamfetol (JZP-110), a Selective Dopamine and Norepinephrine Reuptake Inhibitor., J Pharmacol Exp Ther
Stahl, 2008, Selective histamine H1 antagonism: novel hypnotic and pharmacologic actions challenge classical notions of antihistamines., CNS Spectr
Leo et al., 2006, Clinical potential of milnacipran, a serotonin and norepinephrine reuptake inhibitor, in pain., Curr Opin Investig Drugs
Moret et al., 1985, Biochemical profile of midalcipran (F 2207), 1-phenyl-1-diethyl-aminocarbonyl-2-aminomethyl-cyclopropane (Z) hydrochloride, a potential fourth generation antidepressant drug., Neuropharmacology
McMahon et al., 2003, Discriminative stimulus effects of (-)-ephedrine in rats: analysis with catecholamine transporter and receptor ligands., Drug Alcohol Depend
Kobayashi et al., 2003, The sympathomimetic actions of l-ephedrine and d-pseudoephedrine: direct receptor activation or norepinephrine release?, Anesth. Analg.
Gu et al., 2010, Synthesis and structure-activity studies of benzyl ester meperidine and normeperidine derivatives as selective serotonin transporter ligands., Bioorg. Med. Chem.
Lomenzo et al., 2005, Synthesis and biological evaluation of meperidine analogues at monoamine transporters., J. Med. Chem.
Wall et al., 1995, Biogenic amine flux mediated by cloned transporters stably expressed in cultured cell lines: amphetamine specificity for inhibition and efflux., Mol. Pharmacol.
Salt et al., 1979, Inhibition of neuronal and extraneuronal uptake of noradrenaline by ketamine in the isolated perfused rat heart., Br J Anaesth
Timple JM et al., 2013, The lignan (-)-hinokinin displays modulatory effects on human monoamine and GABA transporter activities., J Nat Prod
Finnerty et al., 1985, Guanadrel. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in hypertension., Drugs
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Mitchell et al., 1970, Guanethidine and related agents. 3. Antagonism by drugs which inhibit the norepinephrine pump in man., J. Clin. Invest.
Joyce et al., 2002, The effect of guanethidine and local anesthetics on the electrically stimulated mouse vas deferens., Anesth. Analg.
Bryan-Lluka et al., 1996, Amezinium and debrisoquine are substrates of uptake1 and potent inhibitors of monoamine oxidase in perfused lungs of rats., Naunyn Schmiedebergs Arch. Pharmacol.
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REBOXETINE SLC6A2

Interaction Score: 5.83

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
12388649 16893531 12623106 15878511 16633143 11249515

Sources:
DrugBank GuideToPharmacology
GUANADREL SLC6A2

Interaction Score: 4.37

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

PMIDs:
3896742 6351026 17139284 17016423 6850722

Sources:
DrugBank
GUANETHIDINE SLC6A2

Interaction Score: 4.37

Interaction Types & Directionality:

inducer (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
16126010 8710929 11403930

Sources:
TEND TdgClinicalTrial DrugBank
DEXMETHYLPHENIDATE SLC6A2

Interaction Score: 2.91

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Focalin

Novel drug target Established target

PMIDs:
11160413 18480678 15322419 17218796 9537821 9181638 16246598 17611273 18698001 11862378

Sources:
TdgClinicalTrial DrugBank
PHENMETRAZINE SLC6A2

Interaction Score: 2.55

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12106802 17139284 17016423 17017961

Sources:
TEND TdgClinicalTrial DrugBank
DIETHYLPROPION SLC6A2

Interaction Score: 2.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
19897080 17139284 17016423

Sources:
TEND TdgClinicalTrial DrugBank
SIBUTRAMINE SLC6A2

Interaction Score: 1.82

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name sibutramine HCl monohydrate,Meridia, Reductil, Reduxade, Zelium

Specific Action of the Ligand Inhibition

PMIDs:
16678551 19475780 11152984 15685250 15382615 12417543 10929704 18671470 11752352 17284621 15944869

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
ATOMOXETINE SLC6A2

Interaction Score: 1.64

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
14709944 16142049 19387424 23266789 12547466 12523874 18033153 19445548 9537821 12862507 12456942 26859445 15801334

Sources:
TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology
VILOXAZINE SLC6A2

Interaction Score: 1.46

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
27230580

Sources:
DrugBank
DESVENLAFAXINE SLC6A2

Interaction Score: 1.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Pristiq

Direct Interaction? True

PMIDs:
17673606 16675639 19698900 19919295 19086875 20944767

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
SOLRIAMFETOL SLC6A2

Interaction Score: 0.97

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a NE reuptake assay in HEK293 cells expressing hNET.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
29891587

Sources:
TdgClinicalTrial DrugBank GuideToPharmacology
MAZINDOL SLC6A2

Interaction Score: 0.97

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
16954558 10966747 9537821 12885787 15300361 2120386

Sources:
DrugBank GuideToPharmacology
PROTRIPTYLINE SLC6A2

Interaction Score: 0.83

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of [3H]nisoxetine binding to CHO cells expressing hNET.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
9537821 17139284 17016423 8684598

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
PHENTERMINE SLC6A2

Interaction Score: 0.83

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
11060745 16119498 7902561 17139284 17016423

Sources:
TEND TdgClinicalTrial DrugBank
AMINEPTINE SLC6A2

Interaction Score: 0.73

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17139284 17016423

Sources:
DrugBank
EPHEDRINE SLC6A2

Interaction Score: 0.73

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

PMIDs:
17209801 12757963 14570629 15955613

Sources:
DrugBank
MILNACIPRAN SLC6A2

Interaction Score: 0.73

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
16869117 3005901

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
LEVOMILNACIPRAN SLC6A2

Interaction Score: 0.73

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
TdgClinicalTrial DrugBank GuideToPharmacology
DULOXETINE SLC6A2

Interaction Score: 0.66

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Cymbalta

Novel drug target Established target

Specific Action of the Ligand Inhibition

PMIDs:
16139169 9669506 14744476 19480470 15316838 16650830 15892657 16199241 11752352 2784100 12481192 18408530 15184278 20432324 17335951

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
VENLAFAXINE SLC6A2

Interaction Score: 0.64

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Effexor

Novel drug target Established target

Specific Action of the Ligand Inhibition

PMIDs:
19728573 9669506 16893531 14744476 19238127 15910402 10884561 11750180 28068779

Sources:
TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology
DEBRISOQUIN SLC6A2

Interaction Score: 0.62

Interaction Types & Directionality:

inducer (activating)

Interaction Info:

PMIDs:
16126010 5431666 8710929 12401623 8740147

Sources:
DrugBank
TESOFENSINE SLC6A2

Interaction Score: 0.55

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name tesofensine, NS-2330

PMIDs:
17112503

Sources:
TdgClinicalTrial DrugBank
DEXTROAMPHETAMINE SLC6A2

Interaction Score: 0.55

Interaction Types & Directionality:

negative modulator (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name SLI 381, SPD 465,Adderall, Adderall XR, Adderall IR

Specific Action of the Ligand Inhibition

PMIDs:
17239355 19727679 8794928

Sources:
TdgClinicalTrial DrugBank GuideToPharmacology
NETARSUDIL SLC6A2

Interaction Score: 0.49

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
28609185

Sources:
DrugBank
HINOKININ SLC6A2

Interaction Score: 0.49

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24112084

Sources:
DTC
PHENDIMETRAZINE SLC6A2

Interaction Score: 0.49

Interaction Types & Directionality:

negative modulator (inhibitory)

Interaction Info:

PMIDs:
17017961

Sources:
DrugBank
BICIFADINE SLC6A2

Interaction Score: 0.49

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17325229

Sources:
DrugBank
NEFAZODONE SLC6A2

Interaction Score: 0.44

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Dissociation constant of [3H]- nisoxatine vs. nefazodone.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
7649970 7475971 10512149 9537821 9098663

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
MIDOMAFETAMINE SLC6A2

Interaction Score: 0.42

Interaction Types & Directionality:

negative modulator (inhibitory)

Interaction Info:

PMIDs:
17209801 10773193 15955613

Sources:
DrugBank
DESIPRAMINE SLC6A2

Interaction Score: 0.39

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Inhibition

PMIDs:
12137927 17428804 9537821 15002740 10424850 11752352 12837768 15814154

Sources:
TEND DTC PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology
BUPROPION SLC6A2

Interaction Score: 0.38

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name BVF-033,Aplenzin

Novel drug target Established target

Trial Name Contrave

PMIDs:
28220701 16893531 12909199 16923164 11752352 15361919

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
IOBENGUANE SLC6A2

Interaction Score: 0.36

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24814532

Sources:
DTC
NISOXETINE SLC6A2

Interaction Score: 0.36

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
EDIVOXETINE SLC6A2

Interaction Score: 0.36

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name LY-2216684

PMIDs:
None found

Sources:
TdgClinicalTrial
EPHEDRA SLC6A2

Interaction Score: 0.34

Interaction Types & Directionality:

negative modulator (inhibitory)

Interaction Info:

PMIDs:
15189772 17209801 10773193 12954796 15955613

Sources:
DrugBank
TAPENTADOL SLC6A2

Interaction Score: 0.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
17656655

Sources:
TdgClinicalTrial DrugBank GuideToPharmacology
NORTRIPTYLINE SLC6A2

Interaction Score: 0.3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
11502876 11092898 14744476 9537821 8863842 17018806

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
METHYLPHENIDATE SLC6A2

Interaction Score: 0.28

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name methylphenidate HCl,Ritalin LA

Trial Name methylphenidate HCl,Metadate CD, Equasym

Novel drug target Established target

PMIDs:
29374517 23609393 29230023 11160413 15322419 17218796 9537821 16246598 23083021 16806100 17611273 18698001 17201613

Sources:
TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology
TRIMIPRAMINE SLC6A2

Interaction Score: 0.28

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
21484238 9537821 17139284 17016423

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
NOMIFENSINE SLC6A2

Interaction Score: 0.27

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
9537821

Sources:
DrugBank GuideToPharmacology
MAPROTILINE SLC6A2

Interaction Score: 0.27

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Endogenous Drug? False

PMIDs:
20141432 17984940 15378668 12573515 17068778

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
CLOMIPRAMINE SLC6A2

Interaction Score: 0.26

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Inhibition

PMIDs:
9537821 11341486

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
BENZATROPINE SLC6A2

Interaction Score: 0.24

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
17897630

Sources:
DrugBank
CHLORPHENIRAMINE SLC6A2

Interaction Score: 0.24

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
9537821

Sources:
DrugBank
DOTHIEPIN SLC6A2

Interaction Score: 0.24

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
17471183 18293180

Sources:
DrugBank GuideToPharmacology
TRAMADOL SLC6A2

Interaction Score: 0.22

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name PTI-601

Novel drug target Established target

Trial Name tramadol extended-release,Raliva ER

PMIDs:
19341511 11916794 8955860 11752352 31004280

Sources:
TEND TdgClinicalTrial DrugBank
ORPHENADRINE SLC6A2

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
10344632

Sources:
DrugBank
IMIPRAMINE SLC6A2

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
16893531 10193665 14716684 11356924 16554743

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
COCAINE SLC6A2

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
7500004 15351386 9387868 15113605

Sources:
TEND TdgClinicalTrial DrugBank
CHEMBL126506 SLC6A2

Interaction Score: 0.18

Interaction Types & Directionality:

negative modulator (inhibitory)

Interaction Info:

PMIDs:
17209801

Sources:
DrugBank
TRODUSQUEMINE SLC6A2

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
AMITIFADINE SLC6A2

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
DOXEPIN SLC6A2

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
19179941 9537821

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
LOFEPRAMINE SLC6A2

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
GuideToPharmacology
AMOXAPINE SLC6A2

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
9537821 17139284 17016423

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
BETHANIDINE SLC6A2

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TEND TdgClinicalTrial
DASOTRALINE SLC6A2

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
MEPERIDINE SLC6A2

Interaction Score: 0.14

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
20980153 15743177

Sources:
DrugBank
VORTIOXETINE SLC6A2

Interaction Score: 0.13

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

PMIDs:
21486038

Sources:
DrugBank
PSEUDOEPHEDRINE SLC6A2

Interaction Score: 0.13

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name fexofenadine + ps/

Novel drug target Established target

PMIDs:
12373557 15189772

Sources:
TdgClinicalTrial DrugBank
AMITRIPTYLINE SLC6A2

Interaction Score: 0.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
14744476 9537821 8736630

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
CYCLOBENZAPRINE SLC6A2

Interaction Score: 0.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
21975349

Sources:
DrugBank
METHAMPHETAMINE SLC6A2

Interaction Score: 0.11

Interaction Types & Directionality:

negative modulator (inhibitory)

Interaction Info:

Trial Name low dose intravenous methamphetamine

Novel drug target Established target

PMIDs:
17209801 15955613

Sources:
TdgClinicalTrial DrugBank
AMPHETAMINE SLC6A2

Interaction Score: 0.11

Interaction Types & Directionality:

stimulator (activating)

Interaction Info:

PMIDs:
7700252 12954796

Sources:
DrugBank
PAROXETINE SLC6A2

Interaction Score: 0.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
14566196 12359676 9537821 11203183

Sources:
DrugBank
SERTRALINE SLC6A2

Interaction Score: 0.09

Interaction Types & Directionality:

negative modulator (inhibitory)

inhibitor (inhibitory)

Interaction Info:

PMIDs:
9537821 23086945

Sources:
DrugBank
ZOTEPINE SLC6A2

Interaction Score: 0.09

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
DrugBank GuideToPharmacology
ESCITALOPRAM SLC6A2

Interaction Score: 0.08

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
24424469 17916059

Sources:
DrugBank
KETAMINE SLC6A2

Interaction Score: 0.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
508488

Sources:
DrugBank
DEXTROMETHORPHAN SLC6A2

Interaction Score: 0.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
7562497

Sources:
DrugBank
TEDATIOXETINE SLC6A2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Lu AA24530

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
MIANSERIN SLC6A2

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
9537821

Sources:
DrugBank
TRAZODONE SLC6A2

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TEND
DOPAMINE SLC6A2

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
11071707

Sources:
DrugBank
PHENELZINE SLC6A2

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
LOXAPINE SLC6A2

Interaction Score: 0.02

Interaction Types & Directionality:

binder

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
CITALOPRAM SLC6A2

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of [3H]dopamine uptake at human NET expressed in COS7 cells.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
QUETIAPINE SLC6A2

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Ensembl: ENSG00000103546
- Version: 101_38
Alternate Names:

SLC6A2 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TdgClinicalTrial: P23975
- Version: January-2014
Alternate Names:

SLC6A2 Gene Symbol

SLCA2 Gene Symbol

Gene Info:

Target Class Transporters

Target Subclass TC:2.A.22.1.2

Publications:
RussLampel: ENSG00000103546
- Version: 26-July-2011
Alternate Names:

SODIUM-DEPENDENT NORADRENALINE TRANSPORTER (NOREPINEPHRINE TRANSPORTER) (NET). [SOURCE:UNIPROT/SWISSPROT;ACC:P23975] Description

ENSG00000103546 Ensembl Gene Id

SLC6A2 Display Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
HopkinsGroom: P23975
- Version: 11-September-2012
Alternate Names:

6530 Entrez Gene Id

SC6A2_HUMAN Uniprot Id

SLC6A2 Uniprot Gene Name

Gene Info:

Interpro Short Name Na/ntran_symport

Human Readable Name DRUGGABLE GENOME

Interpro Acc IPR000175

Gene Categories:

TRANSPORTER, DRUGGABLE GENOME

Publications:
TEND: P23975
- Version: 01-August-2011
Alternate Names:

6530 Entrez Gene Id

SLC6A2 Gene Symbol

P23975 Uniprot Accession

Gene Info:

Target Subclass Other

Target Subclass SLC

Target Subclass SLC6

Publications:
GuideToPharmacology: 6530
- Version: 29-September-2020
Alternate Names:

11048 HUGO Gene ID

11048 HUGO Gene Symbol

solute carrier family 6 member 2 HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Monoamine transporter subfamily

GuideToPharmacology Gene Category ID 176

Gene Categories:

TRANSPORTER

Publications:

PharmGKB: SLC6A2

Version: 18-August-2020

Alternate Names:

PA310 PharmGKB ID

Gene Info:

Publications:

Ramoz N et al., 2009, A haplotype of the norepinephrine transporter (Net) gene Slc6a2 is associated with clinical response to atomoxetine in attention-deficit hyperactivity disorder (ADHD)., Neuropsychopharmacology

Yang L et al., 2013, Adrenergic neurotransmitter system transporter and receptor genes associated with atomoxetine response in attention-deficit hyperactivity disorder children., J Neural Transm (Vienna)

Marshe VS et al., 2017, Norepinephrine Transporter Gene Variants and Remission From Depression With Venlafaxine Treatment in Older Adults., Am J Psychiatry

DrugBank: BE0000486

Version: 5.1.7

Alternate Names:

SLC6A2 DrugBank Gene Name

P23975 UniProt Accession

6530 Entrez Gene Id

Gene Info:

Publications:

Wall et al., 1995, Biogenic amine flux mediated by cloned transporters stably expressed in cultured cell lines: amphetamine specificity for inhibition and efflux., Mol. Pharmacol.

Rothman et al., 2003, In vitro characterization of ephedrine-related stereoisomers at biogenic amine transporters and the receptorome reveals selective actions as norepinephrine transporter substrates., J. Pharmacol. Exp. Ther.

Proietto et al., 2000, Novel anti-obesity drugs., Expert Opin Investig Drugs

NCI: SLC6A2
- Version: 14-September-2017
Alternate Names:

Gene Info:

Publications:

Xiao et al., 1995, Acute administration of alpha-methyl-para-tyrosine alters levels of norepinephrine transporter mRNA in the rat brainstem., Brain Res. Mol. Brain Res.

DTC: SLC6A2

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Hampel T et al., 2014, Synthesis and biological effects of new hybrid compounds composed of benzylguanidines and the alkylating group of busulfan on neuroblastoma cells., Bioorg Med Chem Lett

Paczkowski FA et al., 2007, chi-Conotoxin and tricyclic antidepressant interactions at the norepinephrine transporter define a new transporter model., J Biol Chem

Timple JM et al., 2013, The lignan (-)-hinokinin displays modulatory effects on human monoamine and GABA transporter activities., J Nat Prod

HingoraniCasas: ENSG00000103546
- Version: 31-May-2017
Alternate Names:

ENSG00000103546 Gene Symbol

SLC6A2 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
Pharos: SLC6A2
- Version: 03-September-2020
Alternate Names:

Sodium-dependent noradrenaline transporter Gene Name

P23975 UniProt ID

Gene Info:

Gene Categories:

TRANSPORTER

Publications:
GO: SLC6A2
- Version: 05-September-2020
Alternate Names:

NAT1 GO Gene Synonym

NET1 GO Gene Synonym

SLC6A5 GO Gene Synonym

Gene Info:

Gene Categories:

CELL SURFACE, DRUG RESISTANCE

Publications:

Direct Interaction?	True
Endogenous Drug?	False
Specific Action of the Ligand	Inhibition

Novel drug target	Established target
Trial Name	sibutramine HCl monohydrate,Meridia, Reductil, Reduxade, Zelium
Specific Action of the Ligand	Inhibition

Details of the Assay for Interaction	In a NE reuptake assay in HEK293 cells expressing hNET.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Details of the Assay for Interaction	Inhibition of [<sup>3</sup>H]nisoxetine binding to CHO cells expressing hNET.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Trial Name	Cymbalta
Novel drug target	Established target
Specific Action of the Ligand	Inhibition

Trial Name	Effexor
Novel drug target	Established target
Specific Action of the Ligand	Inhibition

Details of the Assay for Interaction	Dissociation constant of [3H]- nisoxatine <i>vs</i>. nefazodone.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Trial Name	BVF-033,Aplenzin
Novel drug target	Established target
Trial Name	Contrave

Trial Name	methylphenidate HCl,Ritalin LA
Trial Name	methylphenidate HCl,Metadate CD, Equasym
Novel drug target	Established target

Trial Name	PTI-601
Novel drug target	Established target
Trial Name	tramadol extended-release,Raliva ER

Trial Name	fexofenadine + ps/
Novel drug target	Established target

Trial Name	low dose intravenous methamphetamine
Novel drug target	Established target

Details of the Assay for Interaction	Inhibition of [<sup>3</sup>H]dopamine uptake at human NET expressed in COS7 cells.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

SODIUM-DEPENDENT NORADRENALINE TRANSPORTER (NOREPINEPHRINE TRANSPORTER) (NET). [SOURCE:UNIPROT/SWISSPROT;ACC:P23975]	Description
ENSG00000103546	Ensembl Gene Id
SLC6A2	Display Id

6530	Entrez Gene Id
SC6A2_HUMAN	Uniprot Id
SLC6A2	Uniprot Gene Name

11048	HUGO Gene ID
11048	HUGO Gene Symbol
solute carrier family 6 member 2	HUGO Gene Name

SLC6A2	DrugBank Gene Name
P23975	UniProt Accession
6530	Entrez Gene Id

Sodium-dependent noradrenaline transporter	Gene Name
P23975	UniProt ID

SLC6A2 Gene Record

SLC6A2 6530 Druggable GenomeDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? True Endogenous Drug? False Specific Action of the Ligand Inhibition

PMIDs: 12388649 16893531 12623106 15878511 16633143 11249515

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: partial agonist (activating)

Interaction Info:

PMIDs: 3896742 6351026 17139284 17016423 6850722

Sources: DrugBank

Interaction Types & Directionality: inducer (activating)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 16126010 8710929 11403930

Sources: TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Focalin Novel drug target Established target

PMIDs: 11160413 18480678 15322419 17218796 9537821 9181638 16246598 17611273 18698001 11862378

Sources: TdgClinicalTrial DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 12106802 17139284 17016423 17017961

Sources: TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 19897080 17139284 17016423

Sources: TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name sibutramine HCl monohydrate,Meridia, Reductil, Reduxade, Zelium Specific Action of the Ligand Inhibition

PMIDs: 16678551 19475780 11152984 15685250 15382615 12417543 10929704 18671470 11752352 17284621 15944869

Sources: TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? True

PMIDs: 14709944 16142049 19387424 23266789 12547466 12523874 18033153 19445548 9537821 12862507 12456942 26859445 15801334

Sources: TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 27230580

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name Pristiq Direct Interaction? True

PMIDs: 17673606 16675639 19698900 19919295 19086875 20944767

Sources: TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction In a NE reuptake assay in HEK293 cells expressing hNET. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: 29891587

Sources: TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: 16954558 10966747 9537821 12885787 15300361 2120386

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Inhibition of [<sup>3</sup>H]nisoxetine binding to CHO cells expressing hNET. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: 9537821 17139284 17016423 8684598

Sources: TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 11060745 16119498 7902561 17139284 17016423

Sources: TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17139284 17016423

Sources: DrugBank

Interaction Types & Directionality: inverse agonist (inhibitory)

Interaction Info:

PMIDs: 17209801 12757963 14570629 15955613

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? True

PMIDs: 16869117 3005901

Sources: TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? True

PMIDs: None found

Sources: TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Cymbalta Novel drug target Established target Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
12388649 16893531 12623106 15878511 16633143 11249515

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

partial agonist (activating)

PMIDs:
3896742 6351026 17139284 17016423 6850722

Sources:
DrugBank

Interaction Types & Directionality:

inducer (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
16126010 8710929 11403930

Sources:
TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Focalin

Novel drug target Established target

PMIDs:
11160413 18480678 15322419 17218796 9537821 9181638 16246598 17611273 18698001 11862378

Sources:
TdgClinicalTrial DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12106802 17139284 17016423 17017961

Sources:
TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
19897080 17139284 17016423

Sources:
TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name sibutramine HCl monohydrate,Meridia, Reductil, Reduxade, Zelium

Specific Action of the Ligand Inhibition

PMIDs:
16678551 19475780 11152984 15685250 15382615 12417543 10929704 18671470 11752352 17284621 15944869

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
14709944 16142049 19387424 23266789 12547466 12523874 18033153 19445548 9537821 12862507 12456942 26859445 15801334

Sources:
TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
27230580

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Pristiq

Direct Interaction? True

PMIDs:
17673606 16675639 19698900 19919295 19086875 20944767

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a NE reuptake assay in HEK293 cells expressing hNET.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
29891587

Sources:
TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
16954558 10966747 9537821 12885787 15300361 2120386

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of [<sup>3</sup>H]nisoxetine binding to CHO cells expressing hNET.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
9537821 17139284 17016423 8684598

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
11060745 16119498 7902561 17139284 17016423

Sources:
TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
17139284 17016423

Sources:
DrugBank

Interaction Types & Directionality:

inverse agonist (inhibitory)

PMIDs:
17209801 12757963 14570629 15955613

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
16869117 3005901

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Cymbalta

Novel drug target Established target

Specific Action of the Ligand Inhibition

PMIDs:
16139169 9669506 14744476 19480470 15316838 16650830 15892657 16199241 11752352 2784100 12481192 18408530 15184278 20432324 17335951

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Effexor

Novel drug target Established target

Specific Action of the Ligand Inhibition

PMIDs:
19728573 9669506 16893531 14744476 19238127 15910402 10884561 11750180 28068779

Sources:
TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

inducer (activating)

PMIDs:
16126010 5431666 8710929 12401623 8740147

Sources:
DrugBank

Interaction Types & Directionality:

n/a