DGIdb - DRD4 Gene Record

DRD4 1815 Druggable Genome

Alternate Names:

1815
DOPAMINE RECEPTOR D4
DRD4
D4DR
126452
3025
ENSG00000069696
OTTHUMG00000133312
DOPAMINE RECEPTOR D4 [SOURCE:REFSEQ_PEPTIDE;ACC:NP_000788]
NP_000788.2
BE0000389
P21917
217
NM_000797
D<sub>4</sub> receptor
NP_000788
D(4) dopamine receptor
D(2C) dopamine receptor
Dopamine D4 receptor
DRD4_HUMAN
D4R
T24983

Gene Info:

Human Readable Name	G PROTEIN COUPLED RECEPTOR
Human Readable Name	DRUGGABLE GENOME
GuideToPharmacology Gene Category Name	Dopamine receptors
GuideToPharmacology Gene Category ID	20
Target Class	Receptors
Target Subclass	GPCR
Target Subclass	Rhodopsin
Interpro Type	Family
Interpro Short Name	7TM_GPCR_Rhodpsn
Interpro Name	GPCR, rhodopsin-like, 7TM
Uniprot Status	Swiss-Prot
Interpro Acc	IPR000276
Uniprot Evidence	1: Evidence at protein level
Transmembrane Helix Count	7
Target Main Class	Receptors
Gene Biotype	PROTEIN_CODING

(8 More Sources)

Gene Categories: Category Details

G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME

Publications:

Kuballa et al., Central effects of nafadotride, a dopamine D3 receptor antagonist, in rats. Comparison with haloperidol and clozapine., Pharmacol Rep
Glatt et al., 2003, Schizophrenia is not associated with DRD4 48-base-pair-repeat length or individual alleles: results of a meta-analysis., Biol. Psychiatry
Nakane et al., 2005, 2-[4-(3,4-Dimethylphenyl)piperazin-1-ylmethyl]-1H benzoimidazole (A-381393), a selective dopamine D4 receptor antagonist., Neuropharmacology
Zhao et al., 2005, Dopamine D4 receptor gene exon III polymorphism and interindividual variation in response to clozapine., Int. J. Neurosci.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Patel et al., 2003, Pharmacological and functional characterisation of dopamine D4 receptors in the rat retina., Neuropharmacology
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Shahid et al., 2009, Asenapine: a novel psychopharmacologic agent with a unique human receptor signature., J. Psychopharmacol. (Oxford)
Citrome, 2011, Role of sublingual asenapine in treatment of schizophrenia., Neuropsychiatr Dis Treat
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Roth et al., 1995, D4 dopamine receptor binding affinity does not distinguish between typical and atypical antipsychotic drugs., Psychopharmacology (Berl.)
Kvernmo et al., 2008, Receptor-binding and pharmacokinetic properties of dopaminergic agonists., Curr Top Med Chem
Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry
Li P et al., 2016, Dopamine Targeting Drugs for the Treatment of Schizophrenia: Past, Present and Future., Curr Top Med Chem
Piercey MF, 1998, Pharmacology of pramipexole, a dopamine D3-preferring agonist useful in treating Parkinson's disease., Clin Neuropharmacol
Mierau et al., 1995, Pramipexole binding and activation of cloned and expressed dopamine D2, D3 and D4 receptors., Eur. J. Pharmacol.
Dooley M et al., 1998, Pramipexole. A review of its use in the management of early and advanced Parkinson's disease., Drugs Aging
Green et al., 2004, Focus on levomepromazine., Curr Med Res Opin
Burstein et al., 2005, Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist., J. Pharmacol. Exp. Ther.
Brafford MV et al., 2014, Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting., J Adv Pract Oncol
Hutchison et al., 2006, The effect of olanzapine on craving and alcohol consumption., Neuropsychopharmacology
de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
Shill HA et al., 2009, Update on ropinirole in the treatment of Parkinson's disease., Neuropsychiatr Dis Treat
Bobo, 2013, Asenapine, iloperidone and lurasidone: critical appraisal of the most recently approved pharmacotherapies for schizophrenia in adults., Expert Rev Clin Pharmacol
Leysen et al., 1994, Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity., J Clin Psychiatry
Megens et al., 1994, Survey on the pharmacodynamics of the new antipsychotic risperidone., Psychopharmacology (Berl.)
LeWitt PA, 2004, Subcutaneously administered apomorphine: pharmacokinetics and metabolism., Neurology
Melis et al., 2006, PIP3EA and PD-168077, two selective dopamine D4 receptor agonists, induce penile erection in male rats: site and mechanism of action in the brain., Eur. J. Neurosci.
Succu et al., 2007, Stimulation of dopamine receptors in the paraventricular nucleus of the hypothalamus of male rats induces penile erection and increases extra-cellular dopamine in the nucleus accumbens: Involvement of central oxytocin., Neuropharmacology
Boeckler et al., 2004, FAUC 213, a highly selective dopamine D4 receptor full antagonist, exhibits atypical antipsychotic properties in behavioural and neurochemical models of schizophrenia., Psychopharmacology (Berl.)
Sanner et al., 1998, Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist., Bioorg. Med. Chem. Lett.
Mansbach et al., 1998, Selective dopamine D4 receptor antagonists reverse apomorphine-induced blockade of prepulse inhibition., Psychopharmacology (Berl.)
Newman-Tancredi et al., 2002, Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor., J. Pharmacol. Exp. Ther.
Ostadali et al., 2004, The Detection of Dopamine Gene Receptors (DRD1-DRD5) Expression on Human Peripheral Blood Lymphocytes by Real Time PCR., Iran J Allergy Asthma Immunol
Deleu et al., 2002, Clinical pharmacokinetic and pharmacodynamic properties of drugs used in the treatment of Parkinson's disease., Clin Pharmacokinet
Onofrj et al., 2008, An expert opinion on safinamide in Parkinson's disease., Expert Opin Investig Drugs
Koller et al., 1998, Mechanism of action of dopaminergic agents in Parkinson's disease., Neurology
Seeman et al., 1997, Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptors., Neuropsychopharmacology
Kishi T et al., 2013, Efficacy and tolerability of perospirone in schizophrenia: a systematic review and meta-analysis of randomized controlled trials., CNS Drugs
Gilliland SL et al., 2000, Characterization of dopaminergic compounds at hD2short, hD4.2 and hD4.7 receptors in agonist-stimulated [35S]GTPgammaS binding assays., Naunyn Schmiedebergs Arch Pharmacol
Deeks, 2015, Flibanserin: First Global Approval., Drugs
Invernizzi et al., 2003, Flibanserin, a potential antidepressant drug, lowers 5-HT and raises dopamine and noradrenaline in the rat prefrontal cortex dialysate: role of 5-HT(1A) receptors., Br. J. Pharmacol.
Borsini et al., 2002, Pharmacology of flibanserin., CNS Drug Rev
Schotte et al., 1996, Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding., Psychopharmacology (Berl.)
Howland RH, 2015, Buspirone: Back to the Future., J Psychosoc Nurs Ment Health Serv

PRAMIPEXOLE DRD4

Interaction Score: 1.25

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name Mirapex

Novel drug target Established target

PMIDs:
9617505 18691132 7664822 9638397 11752352

Sources:
TEND TdgClinicalTrial DrugBank
SONEPIPRAZOLE DRD4

Interaction Score: 0.78

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
CHEMBL219182 DRD4

Interaction Score: 0.78

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
GuideToPharmacology
ROPINIROLE DRD4

Interaction Score: 0.78

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name JZP-7

Novel drug target Established target

PMIDs:
19557097 18691132 11752352

Sources:
TdgClinicalTrial DrugBank
ROTIGOTINE DRD4

Interaction Score: 0.56

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction D2-like dopamine receptor agonist

Trial Name Neupro

PMIDs:
18691132

Sources:
TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions
APOMORPHINE DRD4

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name intranasal apomorphine

Trial Name inhaled apomorphine hydrochloride, VR004, VR-040, VR-400

Trial Name apomorphine hydrochloride,Apokyn, APO-go

PMIDs:
15037665 17067298 18691132 17164075 15007532 9871530 11752352 9497025

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
PEROSPIRONE DRD4

Interaction Score: 0.33

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
23812802

Sources:
DrugBank GuideToPharmacology
FLIBANSERIN DRD4

Interaction Score: 0.31

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

PMIDs:
26412054 12890707 12177684

Sources:
DrugBank
THIETHYLPERAZINE DRD4

Interaction Score: 0.28

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17139284 17016423

Sources:
TEND TdgClinicalTrial
SUMANIROLE DRD4

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
BENPERIDOL DRD4

Interaction Score: 0.26

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
APOMORPHINE HYDROCHLORIDE DRD4

Interaction Score: 0.26

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction D2-like dopamine receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions
DEXPRAMIPEXOLE DRD4

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name dexpramipexole, KNS-760704

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
PRAMIPEXOLE DIHYDROCHLORIDE DRD4

Interaction Score: 0.26

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
WAY-100,635 DRD4

Interaction Score: 0.26

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
None found

Sources:
GuideToPharmacology
PARDOPRUNOX DRD4

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name pardoprunox, SLV 308

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial DrugBank
PROPIOMAZINE DRD4

Interaction Score: 0.22

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17139284 17016423

Sources:
TEND TdgClinicalTrial
PHENYLTOLOXAMINE DRD4

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
NEMONAPRIDE DRD4

Interaction Score: 0.19

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
HALOPERIDOL DECANOATE DRD4

Interaction Score: 0.19

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor inverse agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ROPINIROLE HYDROCHLORIDE DRD4

Interaction Score: 0.19

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SARIZOTAN HYDROCHLORIDE DRD4

Interaction Score: 0.19

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Dopamine D4 receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions
ZICRONAPINE DRD4

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name LU-31130

PMIDs:
None found

Sources:
TdgClinicalTrial
HALOPERIDOL LACTATE DRD4

Interaction Score: 0.19

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction D2-like dopamine receptor inverse agonist

PMIDs:
None found

Sources:
ChemblInteractions
ASENAPINE DRD4

Interaction Score: 0.18

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Asenapine

Novel drug target Established target

PMIDs:
18308814 21655346 10592235

Sources:
TdgClinicalTrial DrugBank
PERGOLIDE DRD4

Interaction Score: 0.17

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
10832603 18691132

Sources:
DrugBank GuideToPharmacology
PROMAZINE DRD4

Interaction Score: 0.17

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17139284 17016423

Sources:
TEND TdgClinicalTrial
BUSPIRONE DRD4

Interaction Score: 0.16

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
26535760

Sources:
DrugBank
OLANZAPINE PAMOATE DRD4

Interaction Score: 0.16

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
REMOXIPRIDE DRD4

Interaction Score: 0.16

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
9015795

Sources:
DrugBank
CABERGOLINE DRD4

Interaction Score: 0.16

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
12388667 18691132

Sources:
DrugBank GuideToPharmacology
LOXAPINE HYDROCHLORIDE DRD4

Interaction Score: 0.16

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ETILEVODOPA DRD4

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name etilevodopa, TV-1203

PMIDs:
None found

Sources:
TdgClinicalTrial
LISURIDE DRD4

Interaction Score: 0.14

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
18691132

Sources:
DrugBank GuideToPharmacology
PIPAMPERONE DRD4

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
8935801

Sources:
DrugBank
ETICLOPRIDE DRD4

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
LOXAPINE SUCCINATE DRD4

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PERGOLIDE MESYLATE DRD4

Interaction Score: 0.11

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Dopamine receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MELEVODOPA DRD4

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name V-1512, CHF-1512,Levomet Complex, Sirio

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
DROPERIDOL DRD4

Interaction Score: 0.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PALIPERIDONE DRD4

Interaction Score: 0.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
7520908 7531353

Sources:
DrugBank
BROMOCRIPTINE MESYLATE DRD4

Interaction Score: 0.11

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ZIPRASIDONE DRD4

Interaction Score: 0.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
17848919 17139284 17016423

Sources:
TEND DrugBank
LEVOMEPROMAZINE DRD4

Interaction Score: 0.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor antagonist

Direct Interaction yes

PMIDs:
15701205

Sources:
DrugBank ChemblInteractions
CLOZAPINE DRD4

Interaction Score: 0.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Novel drug target Established target

PMIDs:
15886414 13129658 15992586 16223700 11752352 12763097

Sources:
TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology
LEVODOPA DRD4

Interaction Score: 0.11

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name entacapone/levodopa/carbidopa,Stalevo

Novel drug target Established target

Trial Name levodopa + carbidopa,Duodopa

PMIDs:
11978145 18549347 9633680

Sources:
TdgClinicalTrial DrugBank
PROMAZINE HYDROCHLORIDE DRD4

Interaction Score: 0.1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ILOPERIDONE DRD4

Interaction Score: 0.1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
23272794

Sources:
DrugBank
AMOXAPINE DRD4

Interaction Score: 0.08

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Dopamine receptor antagonist

PMIDs:
16135699

Sources:
DrugBank ChemblInteractions
CHLORPROMAZINE DRD4

Interaction Score: 0.08

Interaction Types & Directionality:

binder

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction D2-like dopamine receptor antagonist

Specific Action of the Ligand Antagonist

PMIDs:
8524985

Sources:
DrugBank GuideToPharmacology ChemblInteractions
QUINPIROLE DRD4

Interaction Score: 0.08

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
OLANZAPINE DRD4

Interaction Score: 0.08

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor antagonist

Direct Interaction yes

Trial Name olanzapine,Zyprexa, Zypadhera, Zyprexa Relprevv

PMIDs:
11752352 25032030 16237394

Sources:
TEND TdgClinicalTrial DrugBank ChemblInteractions
BROMOCRIPTINE DRD4

Interaction Score: 0.07

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
18691132

Sources:
DrugBank GuideToPharmacology
DOPAMINE DRD4

Interaction Score: 0.07

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? True

Direct Interaction? True

PMIDs:
17301410

Sources:
DrugBank GuideToPharmacology
LOXAPINE DRD4

Interaction Score: 0.07

Interaction Types & Directionality:

binder

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor antagonist

Direct Interaction yes

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
DrugBank GuideToPharmacology ChemblInteractions
TRIFLUOPERAZINE HYDROCHLORIDE DRD4

Interaction Score: 0.07

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
FENOLDOPAM DRD4

Interaction Score: 0.06

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
ERGOLOID MESYLATES DRD4

Interaction Score: 0.06

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Dopamine receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PIRIBEDIL DRD4

Interaction Score: 0.06

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
TERGURIDE DRD4

Interaction Score: 0.06

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
ROXINDOLE DRD4

Interaction Score: 0.06

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
THIORIDAZINE HYDROCHLORIDE DRD4

Interaction Score: 0.05

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
QUETIAPINE DRD4

Interaction Score: 0.05

Interaction Types & Directionality:

ligand

antagonist (inhibitory)

Interaction Info:

PMIDs:
17848919 27291902

Sources:
DrugBank
ARIPIPRAZOLE DRD4

Interaction Score: 0.05

Interaction Types & Directionality:

partial agonist (activating)

antagonist (inhibitory)

Interaction Info:

PMIDs:
17848919 26346901

Sources:
DrugBank
ZOTEPINE DRD4

Interaction Score: 0.05

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
CHLORPROMAZINE HYDROCHLORIDE DRD4

Interaction Score: 0.05

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SPIPERONE DRD4

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
SERTINDOLE DRD4

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
GuideToPharmacology
THIORIDAZINE DRD4

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction D2-like dopamine receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions
PROCHLORPERAZINE DRD4

Interaction Score: 0.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
TRIFLUOPERAZINE DRD4

Interaction Score: 0.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
PIMOZIDE DRD4

Interaction Score: 0.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Dopamine receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HALOPERIDOL DRD4

Interaction Score: 0.02

Interaction Types & Directionality:

inverse agonist (inhibitory)

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor inverse agonist

Direct Interaction yes

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions

Ensembl: ENSG00000069696
- Version: 101_38
Alternate Names:

DRD4 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TEND: P21917
- Version: 01-August-2011
Alternate Names:

1815 Entrez Gene Id

P21917 Uniprot Accession

DRD4 Gene Symbol

Gene Info:

Transmembrane Helix Count 7

Target Subclass GPCR

Target Main Class Receptors

Publications:
TdgClinicalTrial: P21917
- Version: January-2014
Alternate Names:

DRD4 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:
HopkinsGroom: P21917
- Version: 11-September-2012
Alternate Names:

1815 Entrez Gene Id

DRD4 Uniprot Gene Name

ENSG00000069696 Ensembl Gene Id

Gene Info:

Interpro Type Family

Human Readable Name G PROTEIN COUPLED RECEPTOR

Human Readable Name DRUGGABLE GENOME

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:
RussLampel: ENSG00000069696
- Version: 26-July-2011
Alternate Names:

NP_000788.2 Display Id

ENSG00000069696 Ensembl Gene Id

DOPAMINE RECEPTOR D4 [SOURCE:REFSEQ_PEPTIDE;ACC:NP_000788] Description

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
GuideToPharmacology: 1815
- Version: 29-September-2020
Alternate Names:

3025 HUGO Gene ID

3025 HUGO Gene Symbol

dopamine receptor D4 HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Dopamine receptors

GuideToPharmacology Gene Category ID 20

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:

DrugBank: BE0000389

Version: 5.1.7

Alternate Names:

DRD4 DrugBank Gene Name

P21917 UniProt Accession

1815 Entrez Gene Id

Gene Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

ChemblInteractions: DRD4
- Version: chembl_23
Alternate Names:

DRD4 GENE_SYMBOL

D(4) dopamine receptor UNIPROT

D(2C) dopamine receptor UNIPROT

Gene Info:

Publications:
HingoraniCasas: ENSG00000069696
- Version: 31-May-2017
Alternate Names:

ENSG00000069696 Gene Symbol

DRD4 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
dGene: DRD4
- Version: 27-Jun-2013
Alternate Names:

1815 Gene ID

D4DR dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
TTD: Dopamine D4 receptor
- Version: 2020.06.01
Alternate Names:

D4R TTD Gene Abbreviation

T24983 TTD Target ID

Gene Info:

Publications:
GO: DRD4
- Version: 05-September-2020
Alternate Names:

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:

Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

Specific Action of the Ligand	Full agonist
Endogenous Drug?	False
Direct Interaction?	True

Direct Interaction	yes
Mechanism of Interaction	D2-like dopamine receptor agonist
Trial Name	Neupro

Trial Name	intranasal apomorphine
Trial Name	inhaled apomorphine hydrochloride, VR004, VR-040, VR-400
Trial Name	apomorphine hydrochloride,Apokyn, APO-go

Trial Name	dexpramipexole, KNS-760704
Novel drug target	Established target

Trial Name	pardoprunox, SLV 308
Novel drug target	Established target

Mechanism of Interaction	D2-like dopamine receptor inverse agonist
Direct Interaction	yes

Direct Interaction	yes
Mechanism of Interaction	Dopamine D4 receptor agonist

Specific Action of the Ligand	Partial agonist
Endogenous Drug?	False

Mechanism of Interaction	D2-like dopamine receptor antagonist
Direct Interaction	yes

agonist (activating)
antagonist (inhibitory)

Mechanism of Interaction	Dopamine receptor agonist
Direct Interaction	yes

Trial Name	V-1512, CHF-1512,Levomet Complex, Sirio
Novel drug target	Established target

Trial Name	entacapone/levodopa/carbidopa,Stalevo
Novel drug target	Established target
Trial Name	levodopa + carbidopa,Duodopa

Direct Interaction	yes
Mechanism of Interaction	Dopamine receptor antagonist

1815	Entrez Gene Id
DRD4	Uniprot Gene Name
ENSG00000069696	Ensembl Gene Id

NP_000788.2	Display Id
ENSG00000069696	Ensembl Gene Id
DOPAMINE RECEPTOR D4 [SOURCE:REFSEQ_PEPTIDE;ACC:NP_000788]	Description

3025	HUGO Gene ID
3025	HUGO Gene Symbol
dopamine receptor D4	HUGO Gene Name

DRD4	DrugBank Gene Name
P21917	UniProt Accession
1815	Entrez Gene Id

DRD4	GENE_SYMBOL
D(4) dopamine receptor	UNIPROT
D(2C) dopamine receptor	UNIPROT

DRD4 Gene Record

DRD4 1815 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name Mirapex Novel drug target Established target

PMIDs: 9617505 18691132 7664822 9638397 11752352

Sources: TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info: Specific Action of the Ligand Full agonist Endogenous Drug? False Direct Interaction? True

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name JZP-7 Novel drug target Established target

PMIDs: 19557097 18691132 11752352

Sources: TdgClinicalTrial DrugBank

Interaction Types & Directionality: agonist (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction D2-like dopamine receptor agonist Trial Name Neupro

PMIDs: 18691132

Sources: TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name intranasal apomorphine Trial Name inhaled apomorphine hydrochloride, VR004, VR-040, VR-400 Trial Name apomorphine hydrochloride,Apokyn, APO-go

PMIDs: 15037665 17067298 18691132 17164075 15007532 9871530 11752352 9497025

Sources: TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? True

PMIDs: 23812802

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: agonist (activating) antagonist (inhibitory)

Interaction Info:

PMIDs: 26412054 12890707 12177684

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17139284 17016423

Sources: TEND TdgClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction D2-like dopamine receptor agonist

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info: Trial Name dexpramipexole, KNS-760704 Novel drug target Established target

PMIDs: None found

Sources: TdgClinicalTrial

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction D2-like dopamine receptor agonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: agonist (activating)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Full agonist

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info: Trial Name pardoprunox, SLV 308 Novel drug target Established target

PMIDs: None found

Sources: TdgClinicalTrial DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 17139284 17016423

Sources: TEND TdgClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Endogenous Drug? False Specific Action of the Ligand Antagonist

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name Mirapex

Novel drug target Established target

PMIDs:
9617505 18691132 7664822 9638397 11752352

Sources:
TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name JZP-7

Novel drug target Established target

PMIDs:
19557097 18691132 11752352

Sources:
TdgClinicalTrial DrugBank

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction D2-like dopamine receptor agonist

Trial Name Neupro

PMIDs:
18691132

Sources:
TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name intranasal apomorphine

Trial Name inhaled apomorphine hydrochloride, VR004, VR-040, VR-400

Trial Name apomorphine hydrochloride,Apokyn, APO-go

PMIDs:
15037665 17067298 18691132 17164075 15007532 9871530 11752352 9497025

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
23812802

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

PMIDs:
26412054 12890707 12177684

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17139284 17016423

Sources:
TEND TdgClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction D2-like dopamine receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name dexpramipexole, KNS-760704

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name pardoprunox, SLV 308

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17139284 17016423

Sources:
TEND TdgClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor inverse agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor agonist

Direct Interaction yes

PMIDs:
None found