Evidence map›Paper›PMID 21097933›Full record

ArticleScience (New York, N.Y.)2010

Structure of the human dopamine D3 receptor in complex with a D2/D3 selective antagonist.

Ellen Y T Chien, Wei Liu, Qiang Zhao, Vsevolod Katritch, Gye Won Han, Michael A Hanson, Lei Shi, Amy Hauck Newman, Jonathan A Javitch, Vadim Cherezov and 1 more

Abstract read
In one paragraph

Article in Science (New York, N.Y.), 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 510 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
510citing papers in PubMed, 1 pooled it
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

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.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

510 citing papers in PubMed, 1 synthesis or guideline pooled it.

  1. Pooled it
  2. Article
  3. The structure of the dopamine DScience advances · 2026
    Article
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  19. 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as DInternational journal of molecular sciences · 2025
    Article
  20. Article

450 more citing papers are in PubMed but not listed here.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

11 authors.

Ellen Y T ChienDepartment of Molecular Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
Wei Liu
Qiang Zhao
Vsevolod Katritch
Gye Won Han
Michael A Hanson
Lei Shi
Amy Hauck Newman
Jonathan A Javitch
Vadim Cherezov
Raymond C Stevens

Funding

JCSG Center:Innovative Membrane Protein Technology (RMI)P50GM073197 · NIGMS · SCRIPPS RESEARCH INSTITUTE, THE · PI STEVENS, RAYMOND C · 2004 to 2013
$26.8M
Novel Dopamine D3 Receptor Ligands ZIADA000424 · NIDA · NATIONAL INSTITUTE ON DRUG ABUSE · PI NEWMAN, AMY HAUCK · 2009 to 2025
$25.9M
Sub-project 5U54GM074961 · NIGMS · EMERALD BIOSTRUCTURES · PI STEWART, LANCE J · 2005 to 2009
$19.3M
Project 3U54GM094618 · NIGMS · UNIVERSITY OF SOUTHERN CALIFORNIA · PI KUHN, PETER · 2010 to 2014
$17.1M
Structure of the Dopamine D2-Like Receptor Binding SitesR01MH054137 · NIMH · NEW YORK STATE PSYCHIATRIC INSTITUTE DBA RESEARCH FOUNDATION FOR MENTAL HYGIENE, INC · PI JAVITCH, JONATHAN A · 1995 to 2025
$12.0M
Molecular Mechanism of Allosteric Modulation of the Oxytocin Receptor by SterolsR01GM089857 · NIGMS · UNIVERSITY OF SOUTHERN CALIFORNIA · PI CHEREZOV, VADIM · 2010 to 2014
$1.7M
Molecular Determinants for the Action of PsychostimulantsK05DA022413 · NIDA · COLUMBIA UNIVERSITY HEALTH SCIENCES · PI JAVITCH, JONATHAN A · 2007 to 2016
$1.3M
Membrane Proteins. Crystallogenesis/X-ray Structure(RMI)R01GM075915 · NIGMS · UNIVERSITY OF LIMERICK · PI CAFFREY, MARTIN D. · 2005 to 2009
$984k
The Neurotransmitter: Sodium Symporter Permeation PathwayR00DA023694 · NIDA · WEILL MEDICAL COLL OF CORNELL UNIV · PI SHI, LEI · 2010 to 2012
$725k
Automated Pre-screening System for in meso Membrane protein crystallizationR21RR025336 · NCRR · SCRIPPS RESEARCH INSTITUTE, THE · PI CHEREZOV, VADIM · 2010 to 2011
$472k
Intramural NIH HHSNCI NIH HHS Y1-CO-1020NCRR NIH HHS R21 RR025336NIDA NIH HHS DA022413NIDA NIH HHS DA023694NIDA NIH HHS K05 DA022413NIDA NIH HHS R00 DA023694NIGMS NIH HHS GM075915NIGMS NIH HHS P50 GM073197NIGMS NIH HHS R01 GM089857NIGMS NIH HHS U54 GM074961NIGMS NIH HHS U54 GM094618NIGMS NIH HHS Y1-GM-1104NIMH NIH HHS MH54137NIMH NIH HHS R01 MH054137
6 · The paper itself

Abstract

Dopamine modulates movement, cognition, and emotion through activation of dopamine G protein-coupled receptors in the brain. The crystal structure of the human dopamine D3 receptor (D3R) in complex with the small molecule D2R/D3R-specific antagonist eticlopride reveals important features of the ligand binding pocket and extracellular loops. On the intracellular side of the receptor, a locked conformation of the ionic lock and two distinctly different conformations of intracellular loop 2 are observed. Docking of R-22, a D3R-selective antagonist, reveals an extracellular extension of the eticlopride binding site that comprises a second binding pocket for the aryl amide of R-22, which differs between the highly homologous D2R and D3R. This difference provides direction to the design of D3R-selective agents for treating drug abuse and other neuropsychiatric indications.

Indexed as

AnimalsArginineBinding SitesCell LineCrystallography, X-RayDopamine AntagonistsDopamine D2 Receptor AntagonistsHumansModels, MolecularProtein ConformationReceptors, Dopamine D3Recombinant ProteinsSalicylamidesSpodopteraArginineDopamine AntagonistsDopamine D2 Receptor AntagonistseticloprideReceptors, Dopamine D3Recombinant ProteinsSalicylamides

Identifiers

PMID21097933
PMCPMC3058422

What OpenQuestion holds

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Read underepoch 390

Registered trials

None linked

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.