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SLC6A2 Gene Record

  • Summary
  • Interactions
  • Claims
  • 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
    Palmer et al., Guanadrel sulfate: a postganglionic sympathetic inhibitor for the treatment of mild to moderate hypertension., Pharmacotherapy
    Malinow, 1983, Comparison of guanadrel and guanethidine efficacy and side effects., Clin Ther
    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
    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.
    Lin CW et al., 2018, Discovery and Preclinical Development of Netarsudil, a Novel Ocular Hypotensive Agent for the Treatment of Glaucoma., J Ocul Pharmacol Ther
    Zheng G et al., 2016, Exploring the Inhibitory Mechanism of Approved Selective Norepinephrine Reuptake Inhibitors and Reboxetine Enantiomers by Molecular Dynamics Study., Sci Rep
    Rothman RB et al., 2008, Dopamine transport inhibitors based on GBR12909 and benztropine as potential medications to treat cocaine addiction., Biochem Pharmacol
    Mestres J et al., 2011, Linking pharmacology to clinical reports: cyclobenzaprine and its possible association with serotonin syndrome., Clin Pharmacol Ther
    Bang-Andersen et al., 2011, Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder., J. Med. Chem.
    Sørensen L et al., 2012, Interaction of antidepressants with the serotonin and norepinephrine transporters: mutational studies of the S1 substrate binding pocket., J Biol Chem
  • 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 [<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

  • 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 <i>vs</i>. 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 [<sup>3</sup>H]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:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21