ArticleNature neuroscience2008
The binding sites for cocaine and dopamine in the dopamine transporter overlap.
Article in Nature neuroscience, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 221 papers.
What it found
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
221 citing papers in PubMed, 348 citations in OpenAlex.
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- Mitochondrial calcium influx-driven bioenergetics selectively enable drug addiction.Nature neuroscience · 2026Article
- Synthesis, Antidepressant-like and Anxiolytic-like Effects of Novel Thiadiazole Derivatives: Behavioral Assessment and Mechanistic Investigation.Pharmaceuticals (Basel, Switzerland) · 2026Article
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- Neuroprotective Effect of D-Pinitol Against MPTP-Induced Parkinsonism in C57BL/6J Mice.Antioxidants (Basel, Switzerland) · 2026Article
- Modulation of monoaminergic neurotransmission in substance use disorders: a neuropharmacological perspective focusing on plant-derived metabolites.Frontiers in pharmacology · 2026Review
- Using miniscopes and deep learning to compare neurobehavioral representations of psychostimulant and opioid self-administration.Addiction neuroscience · 2025Article
- RDS-04-010: a novel atypical DAT inhibitor that inhibits cocaine taking and seeking and itself has low abuse potential in experimental animals.Translational psychiatry · 2025Article
- Revealing the location and dynamics of a concealed binding site in the dopamine transporter.Nature communications · 2025Article
- Article
- Cocaine Differentially Affects Mitochondrial Function Depending on Exposure Time.International journal of molecular sciences · 2025Article
- The WAVE complex in developmental and adulthood brain disorders.Experimental & molecular medicine · 2025Review
- Substrate Binding and Conformational Dynamics of the Monoamine Transporters.Advances in neurobiology · 2025Review
- Electrophysiological Methods to Explore the Function of Monoamine Transporters.Advances in neurobiology · 2025Review
- Pharmacological Mechanisms of SLC6 Neurotransmitter Transporter Inhibition.Advances in neurobiology · 2025Review
- Novel Ways of Targeting the Dopamine Transporter.Advances in neurobiology · 2025Review
- Structure-Activity Relationship of Synthetic Cathinones: An Updated Review.ACS pharmacology & translational science · 2024Review
- Article
161 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
11 authors at 4 institutions in 2 countries.
Funding
Abstract
Cocaine is a widely abused substance with psychostimulant effects that are attributed to inhibition of the dopamine transporter (DAT). We present molecular models for DAT binding of cocaine and cocaine analogs constructed from the high-resolution structure of the bacterial transporter homolog LeuT. Our models suggest that the binding site for cocaine and cocaine analogs is deeply buried between transmembrane segments 1, 3, 6 and 8, and overlaps with the binding sites for the substrates dopamine and amphetamine, as well as for benztropine-like DAT inhibitors. We validated our models by detailed mutagenesis and by trapping the radiolabeled cocaine analog [3H]CFT in the transporter, either by cross-linking engineered cysteines or with an engineered Zn2+-binding site that was situated extracellularly to the predicted common binding pocket. Our data demonstrate the molecular basis for the competitive inhibition of dopamine transport by cocaine.
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What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.