• Search
      • Search Interactions Search Categories
    • Browse
      • Browse Categories Browse Sources
    • Information
      • About Publications Interaction Types & Directionalities Interaction Score & Query Score API Documentation FAQ Known Data Clients News Contact
    • Downloads
      • Data Source Code

SLC6A4 Gene Record

  • Summary
  • Interactions
  • Claims
  • SLC6A4 6532 Druggable Genome

    Alternate Names:

    6532
    SOLUTE CARRIER FAMILY 6 MEMBER 4
    SLC6A4
    5-HTT
    5-HTTLPR
    5HTT
    HTT
    OCD1
    SERT
    SERT1
    hSERT
    182138
    11050
    ENSG00000108576
    OTTHUMG00000132751
    P31645
    SODIUM-DEPENDENT SEROTONIN TRANSPORTER (5HT TRANSPORTER) (5HTT). [SOURCE:UNIPROT/SWISSPROT;ACC:P31645]
    SC6A4_HUMAN
    SODIUM-DEPENDENT SEROTONIN TRANSPORTER
    PA312
    5HT transporter

    Gene Info:

    Human Readable Name DRUGGABLE GENOME
    Uniprot Evidence 1: Evidence at protein level
    Interpro Type Family
    Interpro Short Name Na/ntran_symport
    Interpro Name Sodium:neurotransmitter symporter
    Uniprot Status Swiss-Prot
    Interpro Acc IPR000175
    Human Readable Name TRANSPORTER
    Target Class Transporters
    Target Subclass TC:2.A.22.1.1
    Target Class Transporter
    Target Subclass Other
    Transmembrane Helix Count 12
    Target Subclass SLC
    Target Subclass SLC6
    Target Main Class Transporters
    Gene Biotype PROTEIN_CODING
    (6 More Sources)

    Gene Categories: Category Details

    TRANSPORTER
    DRUGGABLE GENOME

    Publications:

    Hunziker et al., 2005, Duloxetine hydrochloride: a new dual-acting medication for the treatment of major depressive disorder., Clin Ther
    Karpa et al., 2002, Duloxetine pharmacology: profile of a dual monoamine modulator., CNS Drug Rev
    Gould et al., 2007, Effect of chronic administration of duloxetine on serotonin and norepinephrine transporter binding sites in rat brain., Biol. Psychiatry
    Trivedi et al., 2008, Clinical evidence for serotonin and norepinephrine reuptake inhibition of duloxetine., Int Clin Psychopharmacol
    Chen et al., 2005, The S-enantiomer of R,S-citalopram, increases inhibitor binding to the human serotonin transporter by an allosteric mechanism. Comparison with other serotonin transporter inhibitors., Eur Neuropsychopharmacol
    Troelsen et al., 2005, Chronic treatment with duloxetine is necessary for an anxiolytic-like response in the mouse zero maze: the role of the serotonin transporter., Psychopharmacology (Berl.)
    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
    Vaishnavi et al., 2004, Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity., Biol. Psychiatry
    Jost et al., 2004, Duloxetine: mechanism of action at the lower urinary tract and Onuf's nucleus., Clin. Auton. Res.
    Mirza et al., 2007, Serotonin transporter density and anxiolytic-like effects of antidepressants in mice., Prog. Neuropsychopharmacol. 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.
    Khullar et al., 2010, Mixed incontinence: current evidence and future perspectives., Neurourol. Urodyn.
    Carter et al., 2009, Duloxetine: a review of its use in the treatment of generalized anxiety disorder., CNS Drugs
    Béïque et al., 1998, Affinities of venlafaxine and various reuptake inhibitors for the serotonin and norepinephrine transporters., Eur. J. Pharmacol.
    Stahl, 2008, Selective histamine H1 antagonism: novel hypnotic and pharmacologic actions challenge classical notions of antihistamines., CNS Spectr
    Tatsumi et al., 1997, Pharmacological profile of antidepressants and related compounds at human monoamine transporters., Eur. J. Pharmacol.
    Crist RC et al., 2018, Pharmacogenetic analysis of opioid dependence treatment dose and dropout rate., Am J Drug Alcohol Abuse
    Hu Y et al., 2012, Berberine and evodiamine influence serotonin transporter (5-HTT) expression via the 5-HTT-linked polymorphic region., Pharmacogenomics J
    Patkar et al., 2002, Serotonin transporter polymorphisms and measures of impulsivity, aggression, and sensation seeking among African-American cocaine-dependent individuals., Psychiatry Res
    Barker et al., 1999, Transmembrane domain I contributes to the permeation pathway for serotonin and ions in the serotonin transporter., J. Neurosci.
    Carrera et al., 2004, Cocaine pharmacology and current pharmacotherapies for its abuse., Bioorg. Med. Chem.
    Corey et al., 1994, A cocaine-sensitive Drosophila serotonin transporter: cloning, expression, and electrophysiological characterization., Proc. Natl. Acad. Sci. U.S.A.
    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
    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
    Perry et al., 2009, Desvenlafaxine: a new serotonin-norepinephrine reuptake inhibitor for the treatment of adults with major depressive disorder., Clin Ther
    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.
    Kamath et al., 2008, Desvenlafaxine succinate for major depressive disorder: a critical review of the evidence., Expert Rev Neurother
    Calabrò M et al., 2020, Psychiatric disorders and SLC6A4 gene variants: possible effects on alcohol dependence and alzheimer's disease., Mol Biol Rep
    Ushijima et al., 2005, Chronopharmacological study of antidepressants in forced swimming test of mice., J. Pharmacol. Exp. Ther.
    Werling et al., 2007, A comparison of the binding profiles of dextromethorphan, memantine, fluoxetine and amitriptyline: treatment of involuntary emotional expression disorder., Exp. Neurol.
    Kalia, 2005, Neurobiological basis of depression: an update., Metab. Clin. Exp.
    Gould et al., 2006, A comparison of the chronic treatment effects of venlafaxine and other antidepressants on serotonin and norepinephrine transporters., Biol. Psychiatry
    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
    Shang et al., 2007, Displacement of serotonin and dopamine transporters by venlafaxine extended release capsule at steady state: a [123I]2beta-carbomethoxy-3beta-(4-iodophenyl)-tropane single photon emission computed tomography imaging study., J Clin Psychopharmacol
    Malizia et al., 1997, Demonstration of clomipramine and venlafaxine occupation at serotonin reuptake sites in man in vivo., J. Psychopharmacol. (Oxford)
    Westenberg, 2009, Recent advances in understanding and treating social anxiety disorder., CNS Spectr
    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
    Sindrup et al., 2005, Antidepressants in the treatment of neuropathic pain., Basic Clin. Pharmacol. Toxicol.
    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
    Spurlock et al., Lack of effect of antidepressant drugs on the levels of mRNAs encoding serotonergic receptors, synthetic enzymes and 5HT transporter., Neuropharmacology
    Diamond et al., 2006, Antidepressants suppress production of the Th1 cytokine interferon-gamma, independent of monoamine transporter blockade., Eur Neuropsychopharmacol
    Whale R et al., 2000, Serotonin transporter (5-HTT) promoter genotype may influence the prolactin response to clomipramine., Psychopharmacology (Berl)
    Gillman, 2007, Tricyclic antidepressant pharmacology and therapeutic drug interactions updated., Br. J. Pharmacol.
    Borkowska et al., [The effect of sertraline on cognitive functions in patients with obsessive-compulsive disorder]., Psychiatr. Pol.
    Suhara et al., 2003, High levels of serotonin transporter occupancy with low-dose clomipramine in comparative occupancy study with fluvoxamine using positron emission tomography., Arch. Gen. Psychiatry
    Alvarez et al., 1999, Decreased platelet serotonin transporter sites and increased platelet inositol triphosphate levels in patients with unipolar depression: effects of clomipramine and fluoxetine., Clin. Pharmacol. Ther.
    Larsen et al., 2004, Selectivity of (3)H-MADAM binding to 5-hydroxytryptamine transporters in vitro and in vivo in mice; correlation with behavioural effects., Br. J. Pharmacol.
    Heusser et al., 2006, Influence of sibutramine treatment on sympathetic vasomotor tone in obese subjects., Clin. Pharmacol. Ther.
    Gomis Barbará, [Pharmacological treatment of obesity]., Rev Med Univ Navarra
    Birkenfeld et al., 2005, Paradoxical effect of sibutramine on autonomic cardiovascular regulation in obese hypertensive patients--sibutramine and blood pressure., Clin. Auton. Res.
    Jordan et al., 2005, Influence of Sibutramine on blood pressure: evidence from placebo-controlled trials., Int J Obes (Lond)
    Birkenfeld et al., 2002, Paradoxical effect of sibutramine on autonomic cardiovascular regulation., Circulation
    Krahn et al., 2001, Narcolepsy and obesity: remission of severe cataplexy with sibutramine., Sleep Med.
    Vazquez Roque et al., 2007, Alteration of gastric functions and candidate genes associated with weight reduction in response to sibutramine., Clin. Gastroenterol. Hepatol.
    Tziomalos et al., 2009, The use of sibutramine in the management of obesity and related disorders: an update., Vasc Health Risk Manag
    Berke et al., 2000, Medical management of obesity., Am Fam Physician
    Heusser et al., 2007, Sympathetic vasomotor tone determines blood pressure response to long-term sibutramine treatment., J. Clin. Endocrinol. Metab.
    Sharma et al., 2008, Sibutramine: current status as an anti-obesity drug and its future perspectives., Expert Opin Pharmacother
    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.
    Wee et al., 2004, Reinforcing effect of pseudoephedrine isomers and the mechanism of action., Eur. J. Pharmacol.
    Frink et al., 1996, Influence of tramadol on neurotransmitter systems of the rat brain., Arzneimittelforschung
    Barann et al., 2006, Effects of tramadol and O-demethyl-tramadol on human 5-HT reuptake carriers and human 5-HT3A receptors: a possible mechanism for tramadol-induced early emesis., Eur. J. Pharmacol.
    Driessen et al., 1992, Interaction of the central analgesic, tramadol, with the uptake and release of 5-hydroxytryptamine in the rat brain in vitro., Br. J. Pharmacol.
    Barakat A, 2019, Revisiting Tramadol: A Multi-Modal Agent for Pain Management., CNS Drugs
    Williams et al., 2010, Selective serotonin reuptake inhibitors (SSRIs) for autism spectrum disorders (ASD)., Cochrane Database Syst Rev
    Miolo et al., 2002, Photoisomerization of fluvoxamine generates an isomer that has reduced activity on the 5-hydroxytryptamine transporter and does not affect cell proliferation., Eur. J. Pharmacol.
    Millan et al., 2003, Blockade of serotonin 5-HT1B and 5-HT2A receptors suppresses the induction of locomotor activity by 5-HT reuptake inhibitors, citalopram and fluvoxamine, in NMRI mice exposed to a novel environment: a comparison to other 5-HT receptor subtypes., Psychopharmacology (Berl.)
    Dell'Osso et al., 2005, Fluvoxamine: a selective serotonin re-uptake inhibitor for the treatment of obsessive-compulsive disorder., Expert Opin Pharmacother
    Irons, 2005, Fluvoxamine in the treatment of anxiety disorders., Neuropsychiatr Dis Treat
    Inoue, 2004, [Analysis and its application for prevention of side-effects of drugs and for evaluation of drug responsiveness]., Yakugaku Zasshi
    McMahon et al., 2001, Role of 5-HT(2a) and 5-HT(2B/2C) receptors in the behavioral interactions between serotonin and catecholamine reuptake inhibitors., Neuropsychopharmacology
    Kakiuchi et al., 2001, Effects of aging on serotonin transporter availability and its response to fluvoxamine in the living brain: PET study with [(11)C](+)McN5652 and [(11)C](-)McN5652 in conscious monkeys., Synapse
    Yoshida et al., 2002, Influence of the serotonin transporter gene-linked polymorphic region on the antidepressant response to fluvoxamine in Japanese depressed patients., Prog. Neuropsychopharmacol. Biol. Psychiatry
    Rasmussen et al., 2009, A single nucleotide polymorphism in the human serotonin transporter introduces a new site for N-linked glycosylation., Neuropharmacology
    Schloss et al., 1995, Heterogeneity of antidepressant binding sites on the recombinant rat serotonin transporter SERT1., Biochemistry
    Plenge et al., 2005, High- and low-affinity binding of S-citalopram to the human serotonin transporter mutated at 20 putatively important amino acid positions., Neurosci. Lett.
    Dugar et al., 2001, Compensatory responses in the aging hippocampal serotonergic system following neurodegenerative injury with 5,7-dihydroxytryptamine., Synapse
    Bareggi et al., 2007, The use of escitalopram beyond major depression: pharmacological aspects, efficacy and tolerability in anxiety disorders., Expert Opin Drug Metab Toxicol
    Vicentic et al., 1999, Serotonin transporter production and degradation rates: studies with RTI-76., Brain Res.
    Eriksson et al., 1999, Effects of mCPP on the extracellular concentrations of serotonin and dopamine in rat brain., Neuropsychopharmacology
    Dutta et al., 2001, Structure-activity relationship studies of 4-[2-(diphenylmethoxy)ethyl]-1-benzylpiperidine derivatives and their N-analogues: evaluation of O-and N-analogues and their binding to monoamine transporters., J. Med. Chem.
    Zhong et al., 2009, An allosteric binding site at the human serotonin transporter mediates the inhibition of escitalopram by R-citalopram: kinetic binding studies with the ALI/VFL-SI/TT mutant., Neurosci. Lett.
    Maines et al., 1999, Corticosterone regulation of serotonin transporter and 5-HT1A receptor expression in the aging brain., Synapse
    Coleman JA et al., 2016, X-ray structures and mechanism of the human serotonin transporter., Nature
    Sangkuhl K et al., 2011, PharmGKB summary: citalopram pharmacokinetics pathway., Pharmacogenet Genomics
    Zhu XL et al., 2020, Correlations of analgesic dosage of morphine with SLC6A4 gene polymorphisms in patients with lung cancer., Eur Rev Med Pharmacol Sci
    Frazer et al., 1998, Serotonin transporter function in vivo: assessment by chronoamperometry., Ann. N. Y. Acad. Sci.
    Kovachich et al., 1992, Effect of repeated administration of antidepressants on serotonin uptake sites in limbic and neocortical structures of rat brain determined by quantitative autoradiography., Neuropsychopharmacology
    McDougle et al., 1998, Evidence for linkage disequilibrium between serotonin transporter protein gene (SLC6A4) and obsessive compulsive disorder., Mol. Psychiatry
    Daws et al., 1998, In vivo chronoamperometric measures of extracellular serotonin clearance in rat dorsal hippocampus: contribution of serotonin and norepinephrine transporters., J. Pharmacol. Exp. Ther.
    Rouillon et al., 1996, [Pharmaco-epidemiologic study of the use of antidepressant drugs in the general population]., Encephale
    Numachi et al., 2007, Methamphetamine-induced hyperthermia and lethal toxicity: role of the dopamine and serotonin transporters., Eur. J. Pharmacol.
    Sora et al., 2009, Monoamine transporter as a target molecule for psychostimulants., Int. Rev. Neurobiol.
    Tellez et al., 2010, Autoradiographic study of serotonin transporter during memory formation., Behav. Brain Res.
    Benmansour et al., 2002, Serotonin clearance in vivo is altered to a greater extent by antidepressant-induced downregulation of the serotonin transporter than by acute blockade of this transporter., J. Neurosci.
    Benmansour et al., 1999, Effects of chronic antidepressant treatments on serotonin transporter function, density, and mRNA level., J. Neurosci.
    Iehlé et al., 1993, Baculovirus-directed expression of human prostatic steroid 5 alpha-reductase 1 in an active form., J. Steroid Biochem. Mol. Biol.
    Chen et al., 2005, Characterization of an allosteric citalopram-binding site at the serotonin transporter., J. Neurochem.
    Durham et al., 2004, The serotonin transporter polymorphism, 5HTTLPR, is associated with a faster response time to sertraline in an elderly population with major depressive disorder., Psychopharmacology (Berl.)
    David et al., 2001, Comparison of antidepressant activity in 4- and 40-week-old male mice in the forced swimming test: involvement of 5-HT1A and 5-HT1B receptors in old mice., Psychopharmacology (Berl.)
    Muneoka et al., 2009, Brain region-specific effects of short-term treatment with duloxetine, venlafaxine, milnacipran and sertraline on monoamine metabolism in rats., Neurochem. Res.
    Rogóz et al., Mechanism of synergistic action following co-treatment with pramipexole and fluoxetine or sertraline in the forced swimming test in rats., Pharmacol Rep
    Johnson BA et al., 2011, Pharmacogenetic approach at the serotonin transporter gene as a method of reducing the severity of alcohol drinking., Am J Psychiatry
    Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
    Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
    Schloss P et al., 1998, The serotonin transporter: a primary target for antidepressant drugs., J Psychopharmacol
    Rausch et al., 2003, Initial platelet serotonin (5-HT) transport kinetics predict nortriptyline treatment outcome., J Clin Psychopharmacol
    Joyce et al., 2003, Age-dependent antidepressant pharmacogenomics: polymorphisms of the serotonin transporter and G protein beta3 subunit as predictors of response to fluoxetine and nortriptyline., Int. J. Neuropsychopharmacol.
    Wisner et al., 2006, Postpartum depression: a randomized trial of sertraline versus nortriptyline., J Clin Psychopharmacol
    Pollock et al., 2000, Allelic variation in the serotonin transporter promoter affects onset of paroxetine treatment response in late-life depression., Neuropsychopharmacology
    Gören et al., 2007, Fluoxetine partly exerts its actions through GABA: a neurochemical evidence., Neurochem. Res.
    Sanders et al., 2007, Chronic blockade or constitutive deletion of the serotonin transporter reduces operant responding for food reward., Neuropsychopharmacology
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Richman et al., 2007, Seizure prophylaxis in an animal model of epilepsy by dietary fluoxetine supplementation., Epilepsy Res.
    Iceta et al., 2007, Effect of long-term fluoxetine treatment on the human serotonin transporter in Caco-2 cells., Life Sci.
    Ranganathan et al., 2001, Mutations in the Caenorhabditis elegans serotonin reuptake transporter MOD-5 reveal serotonin-dependent and -independent activities of fluoxetine., J. Neurosci.
    Davis et al., 1997, Nefazodone. A review of its pharmacology and clinical efficacy in the management of major depression., Drugs
    Taylor et al., 1995, Pharmacology and neurochemistry of nefazodone, a novel antidepressant drug., J Clin Psychiatry
    Narayan et al., 1998, Serotonin transporter-blocking properties of nefazodone assessed by measurement of platelet serotonin., J Clin Psychopharmacol
    Owens et al., 1995, The serotonergic antidepressant nefazodone inhibits the serotonin transporter: in vivo and ex vivo studies., Life Sci.
    Leboyer et al., 1999, Decreased serotonin transporter binding in unaffected relatives of manic depressive patients., Biol. Psychiatry
    Barkan et al., 2004, Biochemical and pharmacological characterization of the serotonin transporter in human peripheral blood lymphocytes., Eur Neuropsychopharmacol
    Scholze et al., 2000, Transporter-mediated release: a superfusion study on human embryonic kidney cells stably expressing the human serotonin transporter., J. Pharmacol. Exp. Ther.
    Quintin et al., 2001, Clinical and neurochemical effect of acute tryptophan depletion in unaffected relatives of patients with bipolar affective disorder., Biol. Psychiatry
    Goulet et al., 2001, Non-amines, drugs without an amine nitrogen, potently block serotonin transport: novel antidepressant candidates?, Synapse
    Russell et al., 2001, The effect of (R)-HA966 or ACEA 1021 on dexfenfluramine or (S)-MDMA-induced changes in temperature, activity, and neurotoxicity., Pharmacol. Biochem. Behav.
    Eddahibi et al., 2001, Dexfenfluramine-associated changes in 5-hydroxytryptamine transporter expression and development of hypoxic pulmonary hypertension in rats., J. Pharmacol. Exp. Ther.
    Wang et al., 2004, 3,4-methylenedioxymethamphetamine (MDMA) administration to rats decreases brain tissue serotonin but not serotonin transporter protein and glial fibrillary acidic protein., Synapse
    Rothman et al., 2003, High-dose fenfluramine administration decreases serotonin transporter binding, but not serotonin transporter protein levels, in rat forebrain., Synapse
    Johnson et al., 2003, The effect of the anorectic agent, d-fenfluramine, and its primary metabolite, d-norfenfluramine, on intact human platelet serotonin uptake and efflux., J. Thromb. Haemost.
    Rothman et al., 1999, Aminorex, fenfluramine, and chlorphentermine are serotonin transporter substrates. Implications for primary pulmonary hypertension., Circulation
    Mekontso-Dessap et al., 2006, Deficiency of the 5-hydroxytryptamine transporter gene leads to cardiac fibrosis and valvulopathy in mice., Circulation
    Zolkowska et al., 2006, Amphetamine analogs increase plasma serotonin: implications for cardiac and pulmonary disease., J. Pharmacol. Exp. Ther.
    John et al., 2007, Voltammetric characterization of the effect of monoamine uptake inhibitors and releasers on dopamine and serotonin uptake in mouse caudate-putamen and substantia nigra slices., Neuropharmacology
    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
    Stahl SM, 2009, Mechanism of action of trazodone: a multifunctional drug., CNS Spectr
    Dresel et al., 1999, In vivo imaging of serotonin transporters with [99mTc]TRODAT-1 in nonhuman primates., Eur J Nucl Med
    Stehouwer et al., 2006, Synthesis, radiosynthesis, and biological evaluation of carbon-11 labeled 2beta-carbomethoxy-3beta-(3'-((Z)-2-haloethenyl)phenyl)nortropanes: candidate radioligands for in vivo imaging of the serotonin transporter with positron emission tomography., J. Med. Chem.
    Izenwasser et al., 1999, Chronic methylphenidate alters locomotor activity and dopamine transporters differently from cocaine., Eur. J. Pharmacol.
    López-Rodríguez R et al., 2013, Pharmacodynamic genetic variants related to antipsychotic adverse reactions in healthy volunteers., Pharmacogenomics
    Vázquez-Bourgon J et al., 2010, Serotonin transporter polymorphisms and early response to antipsychotic treatment in first episode of psychosis., Psychiatry Res
    Hoffman et al., 1998, In vivo electrochemical studies of dopamine clearance in the rat substantia nigra: effects of locally applied uptake inhibitors and unilateral 6-hydroxydopamine lesions., J. Neurochem.
    Holmes et al., 2002, Evaluation of antidepressant-related behavioral responses in mice lacking the serotonin transporter., Neuropsychopharmacology
    Zhou et al., 2006, Evidence that serotonin reuptake modulators increase the density of serotonin innervation in the forebrain., J. Neurochem.
    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
    Vanover KE et al., 2019, Dopamine D<sub>2</sub> receptor occupancy of lumateperone (ITI-007): a Positron Emission Tomography Study in patients with schizophrenia., Neuropsychopharmacology
    Cloonan SM et al., 2009, Synthesis and serotonin transporter activity of sulphur-substituted alpha-alkyl phenethylamines as a new class of anticancer agents., Eur J Med Chem
    Porcelli S et al., 2016, Possible biomarkers modulating haloperidol efficacy and/or tolerability., Pharmacogenomics
    Quaak M et al., 2012, Genetic variants in the serotonin transporter influence the efficacy of bupropion and nortriptyline in smoking cessation., Addiction
    Preuss et al., 2000, Serotonin transporter gene regulatory region polymorphism (5-HTTLPR), [3H]paroxetine binding in healthy control subjects and alcohol-dependent patients and their relationships to impulsivity., Psychiatry Res
    Wihlbäck et al., 2001, Influence of postmenopausal hormone replacement therapy on platelet serotonin uptake site and serotonin 2A receptor binding., Obstet Gynecol
    Haughey et al., 2000, The effects of methamphetamine on serotonin transporter activity: role of dopamine and hyperthermia., J. Neurochem.
    Davis BA et al., 2016, Mechanism of Paroxetine (Paxil) Inhibition of the Serotonin Transporter., Sci Rep
    Foster RH et al., 1997, Paroxetine : a review of its pharmacology and therapeutic potential in the management of panic disorder., CNS Drugs
    Kohlrausch FB et al., 2010, Influence of serotonin transporter gene polymorphisms on clozapine response in Brazilian schizophrenics., J Psychiatr Res
    Fabre et al., [Mechanisms of action of antidepressants: new data from Escitalopram]., Encephale
    Owens et al., 2001, Second-generation SSRIs: human monoamine transporter binding profile of escitalopram and R-fluoxetine., Biol. Psychiatry
    Waugh et al., 2003, Escitalopram : a review of its use in the management of major depressive and anxiety disorders., CNS Drugs
    Sánchez et al., 2003, Escitalopram, the S-(+)-enantiomer of citalopram, is a selective serotonin reuptake inhibitor with potent effects in animal models predictive of antidepressant and anxiolytic activities., Psychopharmacology (Berl.)
    Burke, 2002, Escitalopram., Expert Opin Investig Drugs
    Owens et al., [Second generation SSRIS: human monoamine transporter binding profile of escitalopram and R-fluoxetine]., Encephale
    Sanchez C et al., 2014, A comparative review of escitalopram, paroxetine, and sertraline: Are they all alike?, Int Clin Psychopharmacol
  • DEXFENFLURAMINE   SLC6A4

    Interaction Score: 8.32

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    11325413 11259539 15266556 14515341 14675103


    Sources:
    TdgClinicalTrial TEND

  • SIBUTRAMINE   SLC6A4

    Interaction Score: 3.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name sibutramine HCl monohydrate,Meridia, Reductil, Reduxade, Zelium
    Novel drug target Established target

    PMIDs:
    16678551 15382615 15944869 15685250 12417543 11152984 17544870 19475780 10929704 17284621 18671470


    Sources:
    TdgClinicalTrial TEND

  • 4-METHYLTHIOAMPHETAMINE   SLC6A4

    Interaction Score: 2.38

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19717215


    Sources:
    DTC

  • PHENTERMINE   SLC6A4

    Interaction Score: 2.08

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    10458725 16380550 16644904 14675103 17459426


    Sources:
    TdgClinicalTrial TEND

  • DESVENLAFAXINE   SLC6A4

    Interaction Score: 1.9

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Pristiq
    Novel drug target Established target

    PMIDs:
    19919295 20944767 19698900 17673606 16675639 19086875


    Sources:
    TdgClinicalTrial TEND

  • PROTRIPTYLINE   SLC6A4

    Interaction Score: 1.36

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    9928259 1476595 9672904 9537821 9694957 8767026


    Sources:
    TdgClinicalTrial TEND

  • EVODIAMINE   SLC6A4

    Interaction Score: 1.19

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21647174


    Sources:
    PharmGKB

  • FLUVOXAMINE   SLC6A4

    Interaction Score: 1.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name fluvoxamine , fluvoxamine-CR,Luvox
    Novel drug target Established target

    PMIDs:
    20687077 12208313 12721776 12695316 16316311 18568110 15170064 11166521 11304754 11817517


    Sources:
    TdgClinicalTrial TEND

  • DULOXETINE   SLC6A4

    Interaction Score: 1.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Cymbalta
    Novel drug target Established target

    PMIDs:
    16199241 12481192 16650830 18408530 15695064 16032412 2784100 14744476 15316838 17335951 15892657 20432324 19480470 9669506


    Sources:
    TdgClinicalTrial TEND

  • CLOMIPRAMINE   SLC6A4

    Interaction Score: 1.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    10867985 17471183 12647451 9537821 12695316 9305421 10613618 14993096


    Sources:
    TdgClinicalTrial TEND PharmGKB

  • MINAPRINE   SLC6A4

    Interaction Score: 0.99

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    17016423 17139284 9694022


    Sources:
    TdgClinicalTrial TEND

  • IMIPRAMINE   SLC6A4

    Interaction Score: 0.97

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    10624553 7548008 9537821 15056483 10869387 11513817 11746710


    Sources:
    TdgClinicalTrial TEND

  • MILNACIPRAN   SLC6A4

    Interaction Score: 0.95

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Milnacipran
    Novel drug target Established target

    PMIDs:
    16869117 3005901


    Sources:
    TdgClinicalTrial TEND

  • VENLAFAXINE   SLC6A4

    Interaction Score: 0.95

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Effexor
    Novel drug target Established target

    PMIDs:
    19728573 15695064 17224717 9537821 9305421 19238127 16140280 10884561 15910402 11750180


    Sources:
    TdgClinicalTrial TEND

  • AMITRIPTYLINE   SLC6A4

    Interaction Score: 0.91

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name amitriptyline + ketamine,Epicept NP-1
    Novel drug target Established target
    Trial Name OMS-103HP

    PMIDs:
    16079297 17689532 14744476 15877309 9537821 16032412 16140280 8736630


    Sources:
    TdgClinicalTrial TEND

  • NORTRIPTYLINE   SLC6A4

    Interaction Score: 0.86

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name CRx-191
    Novel drug target Established target
    Trial Name CRx-170

    PMIDs:
    12640215 9537821 14744476 14604448 16855451 11027924


    Sources:
    TdgClinicalTrial TEND

  • NEFAZODONE   SLC6A4

    Interaction Score: 0.83

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    9098663 9537821 7649970 9472845 7475971


    Sources:
    TdgClinicalTrial TEND

  • TESOFENSINE   SLC6A4

    Interaction Score: 0.79

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name tesofensine, NS-2330
    Novel drug target Established target

    PMIDs:
    17112503


    Sources:
    TdgClinicalTrial

  • ESCITALOPRAM   SLC6A4

    Interaction Score: 0.73

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Cipralex, escitalopram,Lexapro
    Novel drug target Established target

    PMIDs:
    12876551 17916059 19616061 11543737 12665392 12719960 12387707 12232544 24424469


    Sources:
    TdgClinicalTrial TEND

  • SERTRALINE   SLC6A4

    Interaction Score: 0.68

    Interaction Types & Directionality:
    negative modulator (inhibitory)
    binder
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Zoloft
    Novel drug target Established target

    PMIDs:
    12151556 10575045 8664165 9537821 15606893 12647451 12955294 11243491 18751896 16963794


    Sources:
    TdgClinicalTrial TEND

  • TRIMIPRAMINE   SLC6A4

    Interaction Score: 0.68

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    9537821 16388933


    Sources:
    TdgClinicalTrial TEND

  • SOLRIAMFETOL   SLC6A4

    Interaction Score: 0.59

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name YKP-10A
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • DAPOXETINE   SLC6A4

    Interaction Score: 0.59

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name dapoxetine,Priligy
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • LEVOMILNACIPRAN   SLC6A4

    Interaction Score: 0.59

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name levomilnacipran, F2695
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • BERBERINE   SLC6A4

    Interaction Score: 0.59

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21647174


    Sources:
    PharmGKB

  • DESIPRAMINE   SLC6A4

    Interaction Score: 0.55

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    9422361 12464448 16140280 9537821 16300628


    Sources:
    TdgClinicalTrial TEND

  • CITALOPRAM   SLC6A4

    Interaction Score: 0.54

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    19500602 7548008 15955412 11180498 17916059 9537821 10546982 10063489 11300876 19616061 10188639 27049939 21546862


    Sources:
    TdgClinicalTrial TEND

  • PAROXETINE   SLC6A4

    Interaction Score: 0.5

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name CRx-139
    Novel drug target Established target
    Trial Name paroxetine hydrochloride,Paxil, Seroxat

    PMIDs:
    10980326 9537821 10869387 11530128 11027924 10987842 27032980 23338224


    Sources:
    TdgClinicalTrial TEND

  • FLUOXETINE   SLC6A4

    Interaction Score: 0.48

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Olanzapine/fluoxetine combination,Symbyax (Zyprexa/Prozac)
    Trial Name NPL-2008, Fluoxetine
    Trial Name fluoxetine HCl,Prozac

    PMIDs:
    17486443 17356573 9537821 11752352 17335951 17215106 17289086 11487610


    Sources:
    TdgClinicalTrial NCI TEND

  • LUMATEPERONE   SLC6A4

    Interaction Score: 0.48

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name ITI-007, ITI-722
    Novel drug target Established target

    PMIDs:
    30449883


    Sources:
    TdgClinicalTrial

  • TRAMADOL   SLC6A4

    Interaction Score: 0.4

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    8955860 16427041 1596676 31004280


    Sources:
    TdgClinicalTrial TEND

  • VORTIOXETINE   SLC6A4

    Interaction Score: 0.4

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name Lu AA21004

    PMIDs:
    21486038


    Sources:
    TdgClinicalTrial

  • COCAINE   SLC6A4

    Interaction Score: 0.4

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    12057823 9537821 10366604 15351386 8302852


    Sources:
    TdgClinicalTrial TEND

  • TRAZODONE   SLC6A4

    Interaction Score: 0.37

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name trazodone extended release, DDS-04A,Oleptro
    Novel drug target Established target

    PMIDs:
    9537821 20095366


    Sources:
    TdgClinicalTrial TEND

  • AMOXAPINE   SLC6A4

    Interaction Score: 0.34

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name CRx-150, amoxapine plus dipyridamole
    Novel drug target Established target
    Trial Name CRx-119

    PMIDs:
    7984281 9537821


    Sources:
    TdgClinicalTrial TEND

  • ONDANSETRON   SLC6A4

    Interaction Score: 0.26

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21247998


    Sources:
    PharmGKB

  • DOXEPIN   SLC6A4

    Interaction Score: 0.26

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name doxepin nasal solution,Dolorac
    Novel drug target Established target
    Trial Name Silenor (SO-101)

    PMIDs:
    19179941 9537821


    Sources:
    TdgClinicalTrial TEND

  • BUPRENORPHINE   SLC6A4

    Interaction Score: 0.24

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29333880


    Sources:
    PharmGKB

  • METHAMPHETAMINE   SLC6A4

    Interaction Score: 0.18

    Interaction Types & Directionality:
    negative modulator (inhibitory)

    Interaction Info:
    Trial Name low dose intravenous methamphetamine
    Novel drug target Established target

    PMIDs:
    17673199 19607959 20226815


    Sources:
    TdgClinicalTrial

  • BUPROPION   SLC6A4

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21658141


    Sources:
    PharmGKB

  • PSEUDOEPHEDRINE   SLC6A4

    Interaction Score: 0.14

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name fexofenadine + ps/
    Novel drug target Established target

    PMIDs:
    15189772


    Sources:
    TdgClinicalTrial

  • QUETIAPINE   SLC6A4

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23859574 20031235


    Sources:
    PharmGKB

  • METHYLPHENIDATE   SLC6A4

    Interaction Score: 0.13

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name methylphenidate HCl,Concerta
    Novel drug target Established target
    Trial Name methylphenidate HCl,Metadate CD, Equasym

    PMIDs:
    10199939 17154506 10414438


    Sources:
    TdgClinicalTrial TEND

  • TEDATIOXETINE   SLC6A4

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name Lu AA24530
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • METHADONE   SLC6A4

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29333880


    Sources:
    PharmGKB

  • MORPHINE   SLC6A4

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    32432768


    Sources:
    PharmGKB

  • RISPERIDONE   SLC6A4

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23859574 20031235


    Sources:
    PharmGKB

  • HALOPERIDOL   SLC6A4

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27023437 20031235


    Sources:
    PharmGKB

  • OLANZAPINE   SLC6A4

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23859574 20031235


    Sources:
    PharmGKB

  • CLOZAPINE   SLC6A4

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20452607


    Sources:
    PharmGKB

  • RIBAVIRIN   SLC6A4

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • ALCOHOL   SLC6A4

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    31595439


    Sources:
    PharmGKB

  • Ensembl: ENSG00000108576

    • Version: 101_38

    Alternate Names:
    SLC6A4 Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • RussLampel: ENSG00000108576

    • Version: 26-July-2011

    Alternate Names:
    SODIUM-DEPENDENT SEROTONIN TRANSPORTER (5HT TRANSPORTER) (5HTT). [SOURCE:UNIPROT/SWISSPROT;ACC:P31645] Description
    SLC6A4 Display Id
    ENSG00000108576 Ensembl Gene Id

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • HopkinsGroom: P31645

    • Version: 11-September-2012

    Alternate Names:
    6532 Entrez Gene Id
    P31645 Uniprot Accession
    SODIUM-DEPENDENT SEROTONIN TRANSPORTER Uniprot Protein Name

    Gene Info:
    Uniprot Evidence 1: Evidence at protein level
    Interpro Type Family
    Interpro Short Name Na/ntran_symport

    Gene Categories:
    TRANSPORTER, DRUGGABLE GENOME

    Publications:

  • TdgClinicalTrial: P31645

    • Version: January-2014

    Alternate Names:
    SLC6A4 Gene Symbol

    Gene Info:
    Target Class Transporters
    Target Subclass TC:2.A.22.1.1
    Target Class Transporter

    Publications:

  • TEND: P31645

    • Version: 01-August-2011

    Alternate Names:
    SC6A4_HUMAN Uniprot Id
    SLC6A4 Gene Symbol
    P31645 Uniprot Accession

    Gene Info:
    Target Subclass Other
    Transmembrane Helix Count 12
    Target Subclass SLC

    Publications:

  • PharmGKB: SLC6A4

    • Version: 18-August-2020

    Alternate Names:
    PA312 PharmGKB ID

    Gene Info:

    Publications:
    Crist RC et al., 2018, Pharmacogenetic analysis of opioid dependence treatment dose and dropout rate., Am J Drug Alcohol Abuse
    Hu Y et al., 2012, Berberine and evodiamine influence serotonin transporter (5-HTT) expression via the 5-HTT-linked polymorphic region., Pharmacogenomics J
    Porcelli S et al., 2016, Possible biomarkers modulating haloperidol efficacy and/or tolerability., Pharmacogenomics

  • NCI: SLC6A4

    • Version: 14-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Lu et al., 2003, Ovarian steroid regulation of serotonin reuptake transporter (SERT) binding, distribution, and function in female macaques., Mol. Psychiatry
    Ranganathan et al., 2001, Mutations in the Caenorhabditis elegans serotonin reuptake transporter MOD-5 reveal serotonin-dependent and -independent activities of fluoxetine., J. Neurosci.

  • DTC: SLC6A4

    • Version: 02-September-2020

    Alternate Names:

    Gene Info:

    Publications:
    Cloonan SM et al., 2009, Synthesis and serotonin transporter activity of sulphur-substituted alpha-alkyl phenethylamines as a new class of anticancer agents., Eur J Med Chem

  • HingoraniCasas: ENSG00000108576

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000108576 Gene Symbol
    SLC6A4 Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • Pharos: SLC6A4

    • Version: 01-February-2022

    Alternate Names:
    Sodium-dependent serotonin transporter Gene Name
    P31645 UniProt ID

    Gene Info:

    Gene Categories:
    TRANSPORTER

    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.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

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