DGIdb - SLC6A3 Gene Record

SLC6A3 6531 Druggable Genome

Alternate Names:

6531
SOLUTE CARRIER FAMILY 6 MEMBER 3
SLC6A3
DAT
DAT1
PKDYS
126455
11049
ENSG00000142319
OTTHUMG00000131016
DA TRANSPORTER
Q01959
SODIUM-DEPENDENT DOPAMINE TRANSPORTER
DOPAMINE TRANSPORTER
SC6A3_HUMAN
SODIUM-DEPENDENT DOPAMINE TRANSPORTER (DA TRANSPORTER) (DAT). [SOURCE:UNIPROT/SWISSPROT;ACC:Q01959]
PA311
T55959
PKDYS1

Gene Info:

Uniprot Status	Swiss-Prot
Interpro Name	Sodium:neurotransmitter symporter
Interpro Acc	IPR000175
Interpro Type	Family
Human Readable Name	TRANSPORTER
Uniprot Evidence	1: Evidence at protein level
Interpro Short Name	Na/ntran_symport
Human Readable Name	DRUGGABLE GENOME
Target Class	Transporters
Target Subclass	TC:2.A.22.1.3
Target Subclass	SLC
Transmembrane Helix Count	12
Target Subclass	SLC6
Target Main Class	Transporters
Target Subclass	Other
Gene Biotype	PROTEIN_CODING

(9 More Sources)

Gene Categories: Category Details

TRANSPORTER
CELL SURFACE
DRUGGABLE GENOME

Publications:

Madras et al., 2006, Modafinil occupies dopamine and norepinephrine transporters in vivo and modulates the transporters and trace amine activity in vitro., J. Pharmacol. Exp. Ther.
Swanson, 2003, Role of executive function in ADHD., J Clin Psychiatry
Zhou et al., 2004, Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization., J. Med. Chem.
Wisor et al., 2001, Dopaminergic role in stimulant-induced wakefulness., J. Neurosci.
Dopheide et al., 2007, Modafinil evokes striatal [(3)H]dopamine release and alters the subjective properties of stimulants., Eur. J. Pharmacol.
Hashimoto et al., 2004, Effects of N-acetyl-L-cysteine on the reduction of brain dopamine transporters in monkey treated with methamphetamine., Ann. N. Y. Acad. Sci.
Spencer et al., 2007, Further evidence of dopamine transporter dysregulation in ADHD: a controlled PET imaging study using altropane., Biol. Psychiatry
Seyfried, 1983, Dopamine uptake inhibiting versus dopamine releasing properties of fencamfamine: an in vitro study., Biochem. Pharmacol.
Li et al., 2006, Interactions of cocaine with dopamine uptake inhibitors or dopamine releasers in rats discriminating cocaine., J. Pharmacol. Exp. Ther.
Galici et al., 2003, Selective decreases in amphetamine self-administration and regulation of dopamine transporter function in diabetic rats., Neuroendocrinology
Garcia et al., 2005, Akt is essential for insulin modulation of amphetamine-induced human dopamine transporter cell-surface redistribution., Mol. Pharmacol.
Fone et al., 2005, Stimulants: use and abuse in the treatment of attention deficit hyperactivity disorder., Curr Opin Pharmacol
Lott et al., 2005, Dopamine transporter gene associated with diminished subjective response to amphetamine., Neuropsychopharmacology
Madras et al., 2005, The dopamine transporter and attention-deficit/hyperactivity disorder., Biol. Psychiatry
Miller et al., 2005, Primate trace amine receptor 1 modulation by the dopamine transporter., J. Pharmacol. Exp. Ther.
Kahlig et al., 2005, Amphetamine induces dopamine efflux through a dopamine transporter channel., Proc. Natl. Acad. Sci. U.S.A.
Volkow et al., 1999, Comparable changes in synaptic dopamine induced by methylphenidate and by cocaine in the baboon brain., Synapse
Volkow et al., 1999, Methylphenidate and cocaine have a similar in vivo potency to block dopamine transporters in the human brain., Life Sci.
Markowitz et al., 2008, Differential pharmacokinetics and pharmacodynamics of methylphenidate enantiomers: does chirality matter?, J Clin Psychopharmacol
Wayment et al., 1999, Effects of methylphenidate analogues on phenethylamine substrates for the striatal dopamine transporter: potential as amphetamine antagonists?, J. Neurochem.
Viggiano et al., 2004, Dysfunctions in dopamine systems and ADHD: evidence from animals and modeling., Neural Plast.
Tatsumi et al., 1997, Pharmacological profile of antidepressants and related compounds at human monoamine transporters., Eur. J. Pharmacol.
Davids et al., 2002, Stereoselective effects of methylphenidate on motor hyperactivity in juvenile rats induced by neonatal 6-hydroxydopamine lesioning., Psychopharmacology (Berl.)
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Dresel et al., 1999, In vivo imaging of serotonin transporters with [99mTc]TRODAT-1 in nonhuman primates., Eur J Nucl Med
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.)
Tilley et al., 2008, The effects of methylphenidate on knockin mice with a methylphenidate-resistant dopamine transporter., J. Pharmacol. Exp. Ther.
Izenwasser et al., 1999, Chronic methylphenidate alters locomotor activity and dopamine transporters differently from cocaine., Eur. J. Pharmacol.
Hamidovic et al., 2010, Polymorphisms in dopamine transporter (SLC6A3) are associated with stimulant effects of D-amphetamine: an exploratory pharmacogenetic study using healthy volunteers., Behav. Genet.
Stein et al., 2005, Dopamine transporter genotype and methylphenidate dose response in children with ADHD., Neuropsychopharmacology
Cheon et al., 2005, The homozygosity for 10-repeat allele at dopamine transporter gene and dopamine transporter density in Korean children with attention deficit hyperactivity disorder: relating to treatment response to methylphenidate., Eur Neuropsychopharmacol
Trinh et al., 2003, Differential psychostimulant-induced activation of neural circuits in dopamine transporter knockout and wild type mice., Neuroscience
Markowitz JS et al., 2006, A comprehensive in vitro screening of d-, l-, and dl-threo-methylphenidate: an exploratory study., 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
Wee et al., 2004, Reinforcing effect of pseudoephedrine isomers and the mechanism of action., Eur. J. Pharmacol.
Foley et al., 2002, Stereospecific inhibition of monoamine uptake transporters by meta-hydroxyephedrine isomers., J Neural Transm (Vienna)
Kuczenski et al., 1995, Hippocampus norepinephrine, caudate dopamine and serotonin, and behavioral responses to the stereoisomers of amphetamine and methamphetamine., J. Neurosci.
Rothman et al., 2009, Studies of the biogenic amine transporters. 13. Identification of "agonist" and "antagonist" allosteric modulators of amphetamine-induced dopamine release., J. Pharmacol. Exp. Ther.
Zhen et al., 2005, Differences in interactions with the dopamine transporter as revealed by diminishment of Na(+) gradient and membrane potential: dopamine versus other substrates., Neuropharmacology
Gomis Barbará, [Pharmacological treatment of obesity]., Rev Med Univ Navarra
Nakagawa et al., 2001, Effects of sibutramine on the central dopaminergic system in rodents., Neurotox Res
Krahn et al., 2001, Narcolepsy and obesity: remission of severe cataplexy with sibutramine., Sleep Med.
Balcioglu et al., 2000, Sibutramine, a serotonin uptake inhibitor, increases dopamine concentrations in rat striatal and hypothalamic extracellular fluid., Neuropharmacology
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
Escubedo et al., 2009, Involvement of nicotinic receptors in methamphetamine- and MDMA-induced neurotoxicity: pharmacological implications., Int. Rev. Neurobiol.
Fleckenstein et al., 2007, New insights into the mechanism of action of amphetamines., Annu. Rev. Pharmacol. Toxicol.
Miller et al., 2002, Bupropion inhibits nicotine-evoked [(3)H]overflow from rat striatal slices preloaded with [(3)H]dopamine and from rat hippocampal slices preloaded with [(3)H]norepinephrine., J. Pharmacol. Exp. Ther.
Kugaya et al., 2003, Changes in human in vivo serotonin and dopamine transporter availabilities during chronic antidepressant administration., Neuropsychopharmacology
Szabó et al., 2004, [Change of dopamine transporter activity (DAT) during the action of bupropion (in depression)]., Neuropsychopharmacol Hung
Meyer et al., 2002, Bupropion occupancy of the dopamine transporter is low during clinical treatment., Psychopharmacology (Berl.)
Learned-Coughlin et al., 2003, In vivo activity of bupropion at the human dopamine transporter as measured by positron emission tomography., Biol. Psychiatry
Stahl et al., 2004, A Review of the Neuropharmacology of Bupropion, a Dual Norepinephrine and Dopamine Reuptake Inhibitor., Prim Care Companion J Clin Psychiatry
Shalabi AR et al., 2017, Deconstructed Analogues of Bupropion Reveal Structural Requirements for Transporter Inhibition versus Substrate-Induced Neurotransmitter Release., ACS Chem Neurosci
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
Simonsen U et al., 2016, Modulation of Dopaminergic Pathways to Treat Erectile Dysfunction., Basic Clin Pharmacol Toxicol
Rothman et al., 2002, Interaction of the anorectic medication, phendimetrazine, and its metabolites with monoamine transporters in rat brain., Eur. J. Pharmacol.
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
Rothman et al., 2006, Therapeutic potential of monoamine transporter substrates., Curr Top Med Chem
Yu et al., 2000, Uptake and release effects of diethylpropion and its metabolites with biogenic amine transporters., Bioorg. Med. Chem.
Arias et al., 2009, Pharmacological and neurotoxicological actions mediated by bupropion and diethylpropion., Int. Rev. Neurobiol.
Porcelli S et al., 2016, Possible biomarkers modulating haloperidol efficacy and/or tolerability., Pharmacogenomics
Audrain-McGovern et al., 2004, Interacting effects of genetic predisposition and depression on adolescent smoking progression., Am J Psychiatry
Lemke, 2007, [Antidepressant effects of dopamine agonists. Experimental and clinical findings]., Nervenarzt
Nemeroff et al., 2004, Pharmacologic differences among the SSRIs: focus on monoamine transporters and the HPA axis., CNS Spectr
Ghanizadeh, 2008, Sertraline-associated hair loss., J Drugs Dermatol
Goodnick et al., 1998, Selective serotonin reuptake inhibitors in affective disorders--I. Basic pharmacology., J. Psychopharmacol. (Oxford)
Wilson et al., 1996, Striatal dopamine, dopamine transporter, and vesicular monoamine transporter in chronic cocaine users., Ann. Neurol.
Rothman et al., 1999, Discovery of novel peptidic dopamine transporter ligands by screening a positional scanning combinatorial hexapeptide library., Synapse
Carrera et al., 2004, Cocaine pharmacology and current pharmacotherapies for its abuse., Bioorg. Med. Chem.
Kim et al., 2003, Synthesis and pharmacology of site specific cocaine abuse treatment agents: 8-substituted isotropane (3-azabicyclo[3.2.1]octane) dopamine uptake inhibitors., J. Med. Chem.
Verma V, 2015, Classic Studies on the Interaction of Cocaine and the Dopamine Transporter., Clin Psychopharmacol Neurosci
Gruner et al., 2009, The roles of dopamine transport inhibition and dopamine release facilitation in wake enhancement and rebound hypersomnolence induced by dopaminergic agents., Sleep
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
Xu M et al., 2010, Pharacogenetic effects of dopamine transporter gene polymorphisms on response to chlorpromazine and clozapine and on extrapyramidal syndrome in schizophrenia., Prog Neuropsychopharmacol Biol Psychiatry
Tidjane Corera et al., 2001, Differential sensitivity to NaCl for inhibitors and substrates that recognize mutually exclusive binding sites on the neuronal transporter of dopamine in rat striatal membranes., Neurosci. Res.
Houlihan et al., 2002, Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter., J. Med. Chem.
Goettl et al., 2000, Retinal cholinergic and dopaminergic deficits of aged rats are improved following treatment with GM1 ganglioside., Brain Res.
Itzhak et al., 1999, Effects of cocaine, nicotine, dizocipline and alcohol on mice locomotor activity: cocaine-alcohol cross-sensitization involves upregulation of striatal dopamine transporter binding sites., Brain Res.
Kulkarni et al., 2002, Three-dimensional quantitative structure-activity relationships of mazindol analogues at the dopamine transporter., J. Med. Chem.
Purkerson-Parker et al., 2001, Dopamine transporter binding in the rat striatum is increased by gestational, perinatal, and adolescent exposure to heptachlor., Toxicol. Sci.
Saunders et al., 2000, Amphetamine-induced loss of human dopamine transporter activity: an internalization-dependent and cocaine-sensitive mechanism., Proc. Natl. Acad. Sci. U.S.A.
Loland et al., 2012, R-modafinil (armodafinil): a unique dopamine uptake inhibitor and potential medication for psychostimulant abuse., Biol. Psychiatry
Han et al., 1999, D2 autoreceptors are not involved in the down-regulation of the striatal dopamine transporter caused by alpha-methyl-p-tyrosine., Res. Commun. Mol. Pathol. Pharmacol.
Timple JM et al., 2013, The lignan (-)-hinokinin displays modulatory effects on human monoamine and GABA transporter activities., J Nat Prod
Hansen et al., 2002, Methylenedioxymethamphetamine decreases plasmalemmal and vesicular dopamine transport: mechanisms and implications for neurotoxicity., J. Pharmacol. Exp. Ther.
Fitzgerald et al., 1990, Effects of methylenedioxymethamphetamine on the release of monoamines from rat brain slices., Eur. J. Pharmacol.
Moreau C et al., 2015, Polymorphism of the dopamine transporter type 1 gene modifies the treatment response in Parkinson's disease., Brain

DEXMETHYLPHENIDATE SLC6A3

Interaction Score: 7.88

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Focalin

Novel drug target Established target

PMIDs:
10025684 10403500 18480678 10037500 15303308 9537821 11862378 11752352 10199939 9181638 18698001 10414438

Sources:
TdgClinicalTrial
FENCAMFAMIN SLC6A3

Interaction Score: 4.85

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
6136281 16478825

Sources:
TdgClinicalTrial TEND
PHENMETRAZINE SLC6A3

Interaction Score: 4.24

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12106802 17016423 17139284 17017961

Sources:
TdgClinicalTrial TEND TTD
MAZINDOL SLC6A3

Interaction Score: 3.64

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Monoamine transporter inhibitor

Direct Interaction yes

PMIDs:
11248372 12213053 10980236 10082805 9537821 12213055 11719704 10823899

Sources:
ChemblInteractions
ALTROPANE SLC6A3

Interaction Score: 3.64

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name altropane

Novel drug target Established target

PMIDs:
17511972

Sources:
TdgClinicalTrial TTD
DIETHYLPROPION SLC6A3

Interaction Score: 2.42

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11131159 19897080

Sources:
TdgClinicalTrial TEND
ARMODAFINIL SLC6A3

Interaction Score: 1.82

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Dopamine transporter inhibitor

Direct Interaction yes

Trial Name armodafinil, R-modafinil,Nuvigil

PMIDs:
22537794

Sources:
TdgClinicalTrial ChemblInteractions
SIBUTRAMINE SLC6A3

Interaction Score: 1.7

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

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

PMIDs:
15382615 15111248 11152984 10974319 19475780 10929704

Sources:
TdgClinicalTrial
RTI-336 SLC6A3

Interaction Score: 1.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PHENTERMINE SLC6A3

Interaction Score: 1.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
19928382 17459426

Sources:
TdgClinicalTrial TEND
ALTROPANE I-123 SLC6A3

Interaction Score: 1.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
DEXTROAMPHETAMINE SLC6A3

Interaction Score: 1.21

Interaction Types & Directionality:

negative modulator (inhibitory)

inhibitor (inhibitory)

Interaction Info:

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

Novel drug target Established target

Direct Interaction yes

PMIDs:
7869099 19244097 16122767

Sources:
TdgClinicalTrial ChemblInteractions TEND
AMITIFADINE SLC6A3

Interaction Score: 1.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
AMPHETAMINE SLC6A3

Interaction Score: 1.03

Interaction Types & Directionality:

negative modulator (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Dopamine transporter releasing agent

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

PMIDs:
12624535 15795321 15661631 15602501 15950014 15764732 15728379

Sources:
TdgClinicalTrial ChemblInteractions NCI TEND
MIDOMAFETAMINE SLC6A3

Interaction Score: 0.97

Interaction Types & Directionality:

negative modulator (inhibitory)

Interaction Info:

PMIDs:
11861820 1982265 17209801

Sources:
TTD
MODAFINIL SLC6A3

Interaction Score: 0.97

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Dopamine transporter inhibitor

Trial Name modafinil,Provigil, Sparlon

PMIDs:
16885432 14658934 15537337 11222668 17477916

Sources:
TdgClinicalTrial ChemblInteractions TTD
BUPROPION SLC6A3

Interaction Score: 0.93

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name BVF-033,Aplenzin

Novel drug target Established target

Trial Name Contrave

PMIDs:
12183670 12589396 9537821 15787205 12185406 14550679 11752352 15361919 28220701 16923164 27541930

Sources:
TdgClinicalTrial TEND
LISDEXAMFETAMINE SLC6A3

Interaction Score: 0.91

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
20091113

Sources:
TdgClinicalTrial TEND
HINOKININ SLC6A3

Interaction Score: 0.81

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24112084

Sources:
DTC
DASOTRALINE SLC6A3

Interaction Score: 0.81

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Monoamine transporter inhibitor

PMIDs:
None found

Sources:
ChemblInteractions TTD
BENZTROPINE SLC6A3

Interaction Score: 0.81

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
LISDEXAMFETAMINE DIMESYLATE SLC6A3

Interaction Score: 0.61

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Vyvanse

Novel drug target Established target

Mechanism of Interaction Dopamine transporter releasing agent

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
METHYLPHENIDATE HYDROCHLORIDE SLC6A3

Interaction Score: 0.61

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Dopamine transporter inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BUPROPION HYDROBROMIDE SLC6A3

Interaction Score: 0.61

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Dopamine transporter inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
AMPHETAMINE ASPARTATE SLC6A3

Interaction Score: 0.61

Interaction Types & Directionality:

n/a

Interaction Info:

Mechanism of Interaction Dopamine transporter releasing agent

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SPIROGLUMIDE SLC6A3

Interaction Score: 0.61

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
DEXMETHYLPHENIDATE HYDROCHLORIDE SLC6A3

Interaction Score: 0.61

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Dopamine transporter inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PHENMETRAZINE HYDROCHLORIDE SLC6A3

Interaction Score: 0.61

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Dopamine transporter inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
AMPHETAMINE SULFATE SLC6A3

Interaction Score: 0.61

Interaction Types & Directionality:

n/a

Interaction Info:

Mechanism of Interaction Dopamine transporter releasing agent

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
AMPHETAMINE ADIPATE SLC6A3

Interaction Score: 0.61

Interaction Types & Directionality:

n/a

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Dopamine transporter releasing agent

PMIDs:
None found

Sources:
ChemblInteractions
DIETHYLPROPION HYDROCHLORIDE SLC6A3

Interaction Score: 0.61

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Dopamine transporter inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
PHENDIMETRAZINE TARTRATE SLC6A3

Interaction Score: 0.61

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Dopamine transporter inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
COCAINE SLC6A3

Interaction Score: 0.58

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8797532 10420171 15351386 12672245 9537821 26598579

Sources:
TdgClinicalTrial TEND PharmGKB TTD
METHYLPHENIDATE SLC6A3

Interaction Score: 0.51

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Dopamine transporter inhibitor

Direct Interaction yes

Trial Name Daytrana

PMIDs:
10025684 10403500 10037500 15303308 9537821 11752352 10199939 18698001 10414438 15827573 15572278 12699766 17201613 16806100

Sources:
TdgClinicalTrial ChemblInteractions NCI TEND TTD
METHAMPHETAMINE SLC6A3

Interaction Score: 0.42

Interaction Types & Directionality:

negative modulator (inhibitory)

Interaction Info:

Trial Name low dose intravenous methamphetamine

Novel drug target Established target

PMIDs:
15795321 19897077 15661631 15602501 15950014 15764732 17209801 15728379

Sources:
TdgClinicalTrial
LIAFENSINE SLC6A3

Interaction Score: 0.4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Monoamine transporter inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BUPROPION HYDROCHLORIDE SLC6A3

Interaction Score: 0.4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Dopamine transporter inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DEXTROAMPHETAMINE ADIPATE SLC6A3

Interaction Score: 0.4

Interaction Types & Directionality:

n/a

Interaction Info:

Mechanism of Interaction Dopamine transporter releasing agent

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
METHAMPHETAMINE HYDROCHLORIDE SLC6A3

Interaction Score: 0.4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Monoamine transporter inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DEXTROAMPHETAMINE SULFATE SLC6A3

Interaction Score: 0.4

Interaction Types & Directionality:

n/a

Interaction Info:

Mechanism of Interaction Dopamine transporter releasing agent

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SERTRALINE SLC6A3

Interaction Score: 0.35

Interaction Types & Directionality:

binder

inhibitor (inhibitory)

Interaction Info:

Trial Name Zoloft

Novel drug target Established target

PMIDs:
17187269 15181382 18664165 9537821 9808077

Sources:
TdgClinicalTrial
METYROSINE SLC6A3

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10741383

Sources:
NCI
PSEUDOEPHEDRINE SLC6A3

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name fexofenadine + ps/

Novel drug target Established target

PMIDs:
15189772 12373557

Sources:
TdgClinicalTrial
SIBUTRAMINE HYDROCHLORIDE SLC6A3

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Monoamine transporter inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TEDATIOXETINE SLC6A3

Interaction Score: 0.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Dopamine transporter inhibitor

Direct Interaction yes

Trial Name Lu AA24530

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
ACETYLCYSTEINE SLC6A3

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15542721

Sources:
NCI
LEVODOPA SLC6A3

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25805645

Sources:
PharmGKB
NICOTINE SLC6A3

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15229055

Sources:
NCI
CLOZAPINE SLC6A3

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20580759

Sources:
PharmGKB
HALOPERIDOL SLC6A3

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27023437

Sources:
PharmGKB
DISULFIRAM SLC6A3

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB

Ensembl: ENSG00000142319
- Version: 101_38
Alternate Names:

SLC6A3 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: Q01959
- Version: 11-September-2012
Alternate Names:

SLC6A3 Uniprot Gene Name

Q01959 Uniprot Accession

SODIUM-DEPENDENT DOPAMINE TRANSPORTER Uniprot Protein Name

Gene Info:

Uniprot Status Swiss-Prot

Interpro Name Sodium:neurotransmitter symporter

Interpro Acc IPR000175

Gene Categories:

TRANSPORTER, DRUGGABLE GENOME

Publications:
RussLampel: ENSG00000142319
- Version: 26-July-2011
Alternate Names:

SLC6A3 Display Id

SODIUM-DEPENDENT DOPAMINE TRANSPORTER (DA TRANSPORTER) (DAT). [SOURCE:UNIPROT/SWISSPROT;ACC:Q01959] Description

ENSG00000142319 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TEND: Q01959
- Version: 01-August-2011
Alternate Names:

Q01959 Uniprot Accession

SC6A3_HUMAN Uniprot Id

SLC6A3 Gene Symbol

Gene Info:

Target Subclass SLC

Transmembrane Helix Count 12

Target Subclass SLC6

Publications:
TdgClinicalTrial: Q01959
- Version: January-2014
Alternate Names:

SLC6A3 Gene Symbol

Gene Info:

Target Class Transporters

Target Subclass TC:2.A.22.1.3

Publications:

PharmGKB: SLC6A3

Version: 18-August-2020

Alternate Names:

PA311 PharmGKB ID

Gene Info:

Publications:

Porcelli S et al., 2016, Possible biomarkers modulating haloperidol efficacy and/or tolerability., Pharmacogenomics

Xu M et al., 2010, Pharacogenetic effects of dopamine transporter gene polymorphisms on response to chlorpromazine and clozapine and on extrapyramidal syndrome in schizophrenia., Prog Neuropsychopharmacol Biol Psychiatry

Moreau C et al., 2015, Polymorphism of the dopamine transporter type 1 gene modifies the treatment response in Parkinson's disease., Brain

NCI: SLC6A3

Version: 14-September-2017

Alternate Names:

Gene Info:

Publications:

Hashimoto et al., 2004, Effects of N-acetyl-L-cysteine on the reduction of brain dopamine transporters in monkey treated with methamphetamine., Ann. N. Y. Acad. Sci.

Han et al., 1999, D2 autoreceptors are not involved in the down-regulation of the striatal dopamine transporter caused by alpha-methyl-p-tyrosine., Res. Commun. Mol. Pathol. Pharmacol.

Wilcox et al., 2000, On the relationship between the dopamine transporter and the reinforcing effects of local anesthetics in rhesus monkeys: practical and theoretical concerns., Psychopharmacology (Berl.)

DTC: SLC6A3
- Version: 02-September-2020
Alternate Names:

Gene Info:

Publications:

Timple JM et al., 2013, The lignan (-)-hinokinin displays modulatory effects on human monoamine and GABA transporter activities., J Nat Prod
ChemblInteractions: DAT1
- Version: chembl_23
Alternate Names:

DAT1 GENE_SYMBOL

SLC6A3 GENE_SYMBOL

Sodium-dependent dopamine transporter UNIPROT

Gene Info:

Publications:
HingoraniCasas: ENSG00000142319
- Version: 31-May-2017
Alternate Names:

ENSG00000142319 Gene Symbol

SLC6A3 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
GO: SLC6A3
- Version: 01-February-2022
Alternate Names:

DAT1 GO Gene Synonym

Gene Info:

Gene Categories:

CELL SURFACE

Publications:
TTD: Dopamine transporter
- Version: 2020.06.01
Alternate Names:

DAT TTD Gene Abbreviation

T55959 TTD Target ID

Gene Info:

Publications:
Pharos: SLC6A3
- Version: 01-February-2022
Alternate Names:

Sodium-dependent dopamine transporter Gene Name

Q01959 UniProt ID

Gene Info:

Gene Categories:

TRANSPORTER

Publications:

Mechanism of Interaction	Monoamine transporter inhibitor
Direct Interaction	yes

Mechanism of Interaction	Dopamine transporter inhibitor
Direct Interaction	yes
Trial Name	armodafinil, R-modafinil,Nuvigil

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

Trial Name	SLI 381, SPD 465,Adderall, Adderall XR, Adderall IR
Novel drug target	Established target
Direct Interaction	yes

Direct Interaction	yes
Mechanism of Interaction	Dopamine transporter releasing agent
Trial Name	SLI 381, SPD 465,Adderall, Adderall XR, Adderall IR

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

Trial Name	Vyvanse
Novel drug target	Established target
Mechanism of Interaction	Dopamine transporter releasing agent

Trial Name	low dose intravenous methamphetamine
Novel drug target	Established target

Trial Name	fexofenadine + ps/
Novel drug target	Established target

SLC6A3	Uniprot Gene Name
Q01959	Uniprot Accession
SODIUM-DEPENDENT DOPAMINE TRANSPORTER	Uniprot Protein Name

antagonist (inhibitory)
inhibitor (inhibitory)

negative modulator (inhibitory)
inhibitor (inhibitory)

SLC6A3	Display Id
SODIUM-DEPENDENT DOPAMINE TRANSPORTER (DA TRANSPORTER) (DAT). [SOURCE:UNIPROT/SWISSPROT;ACC:Q01959]	Description
ENSG00000142319	Ensembl Gene Id

DAT1	GENE_SYMBOL
SLC6A3	GENE_SYMBOL
Sodium-dependent dopamine transporter	UNIPROT

Sodium-dependent dopamine transporter	Gene Name
Q01959	UniProt ID

SLC6A3 Gene Record

SLC6A3 6531 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Focalin Novel drug target Established target

PMIDs: 10025684 10403500 18480678 10037500 15303308 9537821 11862378 11752352 10199939 9181638 18698001 10414438

Sources: TdgClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 6136281 16478825

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 12106802 17016423 17139284 17017961

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Monoamine transporter inhibitor Direct Interaction yes

PMIDs: 11248372 12213053 10980236 10082805 9537821 12213055 11719704 10823899

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info: Trial Name altropane Novel drug target Established target

PMIDs: 17511972

Sources: TdgClinicalTrial TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 11131159 19897080

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory) inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Dopamine transporter inhibitor Direct Interaction yes Trial Name armodafinil, R-modafinil,Nuvigil

PMIDs: 22537794

Sources: TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 15382615 15111248 11152984 10974319 19475780 10929704

Sources: TdgClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 19928382 17459426

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

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

Interaction Info: Trial Name SLI 381, SPD 465,Adderall, Adderall XR, Adderall IR Novel drug target Established target Direct Interaction yes

PMIDs: 7869099 19244097 16122767

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: negative modulator (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Dopamine transporter releasing agent Trial Name SLI 381, SPD 465,Adderall, Adderall XR, Adderall IR

PMIDs: 12624535 15795321 15661631 15602501 15950014 15764732 15728379

Sources: TdgClinicalTrial ChemblInteractions NCI TEND

Interaction Types & Directionality: negative modulator (inhibitory)

Interaction Info:

PMIDs: 11861820 1982265 17209801

Sources: TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Dopamine transporter inhibitor Trial Name modafinil,Provigil, Sparlon

PMIDs: 16885432 14658934 15537337 11222668 17477916

Sources: TdgClinicalTrial ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 12183670 12589396 9537821 15787205 12185406 14550679 11752352 15361919 28220701 16923164 27541930

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 20091113

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Focalin

Novel drug target Established target

PMIDs:
10025684 10403500 18480678 10037500 15303308 9537821 11862378 11752352 10199939 9181638 18698001 10414438

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
6136281 16478825

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12106802 17016423 17139284 17017961

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Monoamine transporter inhibitor

Direct Interaction yes

PMIDs:
11248372 12213053 10980236 10082805 9537821 12213055 11719704 10823899

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name altropane

Novel drug target Established target

PMIDs:
17511972

Sources:
TdgClinicalTrial TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11131159 19897080

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Dopamine transporter inhibitor

Direct Interaction yes

Trial Name armodafinil, R-modafinil,Nuvigil

PMIDs:
22537794

Sources:
TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

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

PMIDs:
15382615 15111248 11152984 10974319 19475780 10929704

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
19928382 17459426

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

negative modulator (inhibitory)

inhibitor (inhibitory)

Interaction Info:

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

Novel drug target Established target

Direct Interaction yes

PMIDs:
7869099 19244097 16122767

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

negative modulator (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Dopamine transporter releasing agent

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

PMIDs:
12624535 15795321 15661631 15602501 15950014 15764732 15728379

Sources:
TdgClinicalTrial ChemblInteractions NCI TEND

Interaction Types & Directionality:

negative modulator (inhibitory)

PMIDs:
11861820 1982265 17209801

Sources:
TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Dopamine transporter inhibitor

Trial Name modafinil,Provigil, Sparlon

PMIDs:
16885432 14658934 15537337 11222668 17477916

Sources:
TdgClinicalTrial ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name BVF-033,Aplenzin

Novel drug target Established target

Trial Name Contrave

PMIDs:
12183670 12589396 9537821 15787205 12185406 14550679 11752352 15361919 28220701 16923164 27541930

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
20091113

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
24112084

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Monoamine transporter inhibitor

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a