Protein / target
D(4) dopamine receptor
Protein at a glance
Biological role
Dopamine neurotransmitter receptor activity, coupled via Gi/Go
Strongest disease association
Schizophrenia
Therapeutic position
Established drug target
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function overview
Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior.
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Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Activated by dopamine, but also by epinephrine and norepinephrine, and by numerous synthetic agonists and drugs (PubMed:16423344, PubMed:27659709, PubMed:29051383, PubMed:9003072). Agonist binding triggers signaling via G proteins that inhibit adenylyl cyclase (PubMed:16423344, PubMed:27659709, PubMed:29051383, PubMed:7512953, PubMed:7643093). Modulates the circadian rhythm of contrast sensitivity by regulating the rhythmic expression of NPAS2 in the retinal ganglion cells (By similarity)
Subcellular location
Domains and Gene Ontology detail (39)Hide
Gene Ontology
- Cdendrite
- Cglutamatergic synapse
- Cmembrane
- Cplasma membrane
- Cpostsynapse
- Fdopamine binding
- Fdopamine neurotransmitter receptor activity
- Fdopamine neurotransmitter receptor activity, coupled via Gi/Go
- Fepinephrine binding
- FG protein-coupled serotonin receptor activity
- Fidentical protein binding
- Fmetal ion binding
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
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Inhibitory neurotransmission
- ·inhibitory postsynaptic potential
G protein-coupled signalling
- ·G protein-coupled serotonin receptor activity
- ·adenylate cyclase-modulating G protein-coupled receptor signaling pathway
- ·G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messen…
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Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Interaction neighbourhood
Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.
Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.
Approved medicines with mapped indications
Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.
30 medicines meet Open Targets' target-level approved-medicine definition; the 3 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.
Drugs targeting this protein
How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.
D2-like dopamine receptor antagonist
Indicated for Bipolar Disorder, Mental Disorders, Psychomotor Agitation, Psychotic Disorders
D2-like dopamine receptor inverse agonist
Indicated for Conduct Disorder, Psychotic Disorders, Schizophrenia, Tourette's Syndrome
D2-like dopamine receptor antagonist
Indicated for Bipolar Disorder, Mental Disorders, Psychomotor Agitation, Psychotic Disorders
ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.
Translational evidence
Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.
Strongest disease associations · via encoding gene DRD4
Gene-level evidence surfaced through the gene DRD4that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.
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The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the per-type scores above show the calculation.
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Drug development
33 compounds recorded · 30 approved · 2 in clinical development · 1 earlier-stage
View all recorded compounds (10)Hide
Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.
Tractability
Small molecules — Strong
Antibodies — Emerging
Protein degraders — Emerging
Other modalities — Strong
View underlying tractability evidence (10)Hide
Raw Open Targets tractability assessment buckets, by modality.
Safety-related annotations
Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.
Clinical trials
Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.
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ClinicalTrials.gov via the drug-target graph.
What's happening now
Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for 2 drugs that target this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.
- Label change
Label change: OLANZAPINE (ANDA076133)
- Label change
Label change: OLANZAPINE (ANDA076255)
- Regulatory approval
Approval: HALOPERIDOL (ANDA214470)
- Label change
Label change: OLANZAPINE (ANDA076133)
- Label change
Label change: OLANZAPINE (ANDA076255)
- Withdrawn from market
Market withdrawal: Olanzapine Apotex (EMA)
- Label change
Label change: OLANZAPINE (ANDA076255)
- Safety communication
Drug Safety Update: Haloperidol (Haldol): reminder of risks when used in elderly patients for the acute treatment of delirium
- New publicationOlanzapine for the Prevention of Postdischarge Nausea and Vomiting after Ambulatory Surgery: A Randomized Controlled Trial.
- New publicationMitigation of Olanzapine-Induced Weight Gain With Samidorphan, an Opioid Antagonist: A Randomized Double-Blind Phase 2 Study in Patients With Schizophrenia.
- New publicationCanadian Network for Mood and Anxiety Treatments (CANMAT) and International Society for Bipolar Disorders (ISBD) 2018 guidelines for the management of patients with bipolar disorder.
- New publicationEffectiveness of antipsychotic drugs in patients with chronic schizophrenia.
Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.
Related family literature
Papers about “Receptors, Dopamine” — a broader family this protein belongs to. Shown as context; not counted as papers specifically about this protein.
via Receptors, Dopamine
via Receptors, Dopamine
Europe PMC literature, reached through curated HGNC family membership. Membership is a taxonomic relationship — it does not imply this protein participates in every mechanism these papers discuss.
Related literature
Papers indexed under “Receptors, Dopamine D4” — a subject heading that covers this protein without being specific to it. Shown as context; not counted as this protein's own research activity.
Europe PMC literature, reached through a MeSH descriptor linked to this protein.