Page last updated: 2024-12-07

aj 76

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Description

5-methoxy-1-methyl-2-(n-propylamino)tetralin: RN given refers to cis-(+)-isomer; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

(1S,2R)-5-methoxy-1-methyl-2-(propylamino)tetralin : A secondary amino compound that consists of tetralin bearing methyl, propylamino and methoxy groups at positions 1, 2 and 5 respectively. Dopamine receptor antagonist with preferential action at presynaptic receptors (pKi values are 6.95, 6.67, 6.37, 6.21 and 6.07 at hD3. hD4, hD2S, hD2L and rD2 receptors respectively). [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID122334
CHEMBL ID27441
CHEBI ID64117
SCHEMBL ID276252
MeSH IDM0145735

Synonyms (36)

Synonym
(5-methoxy-1-methyl-1,2,3,4-tetrahydro-naphthalen-2-yl)-propyl-amine
aj76(+)
((1s,2r)-5-methoxy-1-methyl-1,2,3,4-tetrahydro-naphthalen-2-yl)-propyl-amine
(+)-(5-methoxy-1-methyl-1,2,3,4-tetrahydro-naphthalen-2-yl)-propyl-amine
(1s,2r)-(5-methoxy-1-methyl-1,2,3,4-tetrahydro-naphthalen-2-yl)-propyl-amine
bdbm50041959
BRD-K76677554-001-01-7
(+)-aj76
gtpl970
tocris-0678
NCGC00024726-01
BIOMOL-NT_000004
BPBIO1_001129
PDSP2_000777
NCGC00024726-02
aj-76
aj 76
2-naphthalenamine, 1,2,3,4-tetrahydro-5-methoxy-1-methyl-n-propyl-, (1s-cis)-
5-methoxy-1-methyl-2-(n-propylamino)tetralin
85379-09-5
CHEMBL27441 ,
chebi:64117 ,
(1s,2r)-5-methoxy-1-methyl-n-propyl-1,2,3,4-tetrahydronaphthalen-2-amine
cas_85379-09-5
aj76
bdbm81797
(+)-aj 76
(1s,2r)-5-methoxy-1-methyl-2-(propylamino)tetralin
cis-(+)-5-methoxy-1-methyl-2-(propylamino)tetralin
SCHEMBL276252
DTXSID1043889
a j76
Q27074361
(+)-aj 76; (1s,2r)-aj 76
BRD-K76677554-003-01-3
aj76-(+)

Research Excerpts

Overview

(+)-AJ 76 is a stimulant dopamine (DA) antagonist. It has a putative preferential action at DA nerve terminal autoreceptors.

ExcerptReferenceRelevance
"(+)-AJ 76 is a presumed preferential dopamine (DA) autoreceptor antagonist which, in previous behavioral investigations, has displayed properties characteristic of both DA agonists and DA antagonists. "( Antagonism of cocaine self-administration by the preferential dopamine autoreceptor antagonist, (+)-AJ 76.
Collins, RJ; Myers, JE; Piercey, MF; Richardson, NR; Roberts, DC; Svensson, K, 1993
)
1.06
"(+)-AJ 76 is a stimulant dopamine (DA) antagonist, which has a putative preferential action at DA nerve terminal autoreceptors. "( Antagonism of cocaine's stimulant effects on local cerebral glucose utilization by the preferential autoreceptor antagonist (+)-AJ 76.
Casey, BL; Piercey, MF; Ray, CA, 1996
)
1.06

Treatment

ExcerptReferenceRelevance
"(+)-AJ 76/cocaine treatment significantly increased locomotor activity (p < 0.001); central locomotor behavior was not affected, however, time course data showed significant increases at 10, 20, 40, 50 and 80 min."( Neurochemical and behavioral evidence supporting (+)-AJ 76 as a potential pharmacotherapy for cocaine abuse.
Broderick, PA; Piercey, MF, 1998
)
1.03

Compound-Compound Interactions

ExcerptReferenceRelevance
" When combined with saline, partial substitution for cocaine was seen in one of three monkeys with AJ and in none with CLZ."( Evaluation of the reinforcing and discriminative stimulus effects of cocaine in combination with (+)-AJ76 or clozapine.
Piercey, MF; Vanover, KE; Woolverton, WL, 1993
)
0.29

Dosage Studied

ExcerptRelevanceReference
"25-5 mg/kg) did not alter the cocaine dose-response curve."( Effects of the putative dopamine autoreceptor antagonists (+)-AJ 76 and (+)-UH 232 on the discriminative stimulus properties of cocaine.
Callahan, PM; Cunningham, KA; Piercey, MF, 1992
)
0.52
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
dopaminergic antagonistA drug that binds to but does not activate dopamine receptors, thereby blocking the actions of dopamine or exogenous agonists.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
tetralinsCompounds containing a tetralin skeleton.
secondary amino compoundA compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency0.28180.003245.467312,589.2998AID2517
regulator of G-protein signaling 4Homo sapiens (human)Potency2.37780.531815.435837.6858AID504845
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency0.25120.00207.533739.8107AID891
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
D(2) dopamine receptorHomo sapiens (human)Ki0.01400.00000.651810.0000AID62743
D(2) dopamine receptorBos taurus (cattle)Ki0.15150.00000.58366.1000AID62337; AID62338
D(4) dopamine receptorHomo sapiens (human)Ki0.11700.00000.436210.0000AID63849
D(3) dopamine receptorHomo sapiens (human)Ki0.04800.00000.602010.0000AID65133; AID65786
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.31820.00000.437510.0000AID65415; AID65559; AID65560
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (127)

Processvia Protein(s)Taxonomy
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(2) dopamine receptorHomo sapiens (human)
response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein phosphorylationD(2) dopamine receptorHomo sapiens (human)
response to amphetamineD(2) dopamine receptorHomo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressureD(2) dopamine receptorHomo sapiens (human)
regulation of heart rateD(2) dopamine receptorHomo sapiens (human)
regulation of sodium ion transportD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(2) dopamine receptorHomo sapiens (human)
positive regulation of neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
positive regulation of receptor internalizationD(2) dopamine receptorHomo sapiens (human)
autophagyD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
neuron-neuron synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
axonogenesisD(2) dopamine receptorHomo sapiens (human)
synapse assemblyD(2) dopamine receptorHomo sapiens (human)
sensory perception of smellD(2) dopamine receptorHomo sapiens (human)
long-term memoryD(2) dopamine receptorHomo sapiens (human)
grooming behaviorD(2) dopamine receptorHomo sapiens (human)
locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
adult walking behaviorD(2) dopamine receptorHomo sapiens (human)
protein localizationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell population proliferationD(2) dopamine receptorHomo sapiens (human)
associative learningD(2) dopamine receptorHomo sapiens (human)
visual learningD(2) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(2) dopamine receptorHomo sapiens (human)
response to light stimulusD(2) dopamine receptorHomo sapiens (human)
response to toxic substanceD(2) dopamine receptorHomo sapiens (human)
response to iron ionD(2) dopamine receptorHomo sapiens (human)
response to inactivityD(2) dopamine receptorHomo sapiens (human)
Wnt signaling pathwayD(2) dopamine receptorHomo sapiens (human)
striatum developmentD(2) dopamine receptorHomo sapiens (human)
orbitofrontal cortex developmentD(2) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(2) dopamine receptorHomo sapiens (human)
adenohypophysis developmentD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell migrationD(2) dopamine receptorHomo sapiens (human)
peristalsisD(2) dopamine receptorHomo sapiens (human)
auditory behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of synaptic transmission, GABAergicD(2) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(2) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
response to histamineD(2) dopamine receptorHomo sapiens (human)
response to nicotineD(2) dopamine receptorHomo sapiens (human)
positive regulation of urine volumeD(2) dopamine receptorHomo sapiens (human)
positive regulation of renal sodium excretionD(2) dopamine receptorHomo sapiens (human)
positive regulation of multicellular organism growthD(2) dopamine receptorHomo sapiens (human)
response to cocaineD(2) dopamine receptorHomo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleepD(2) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(2) dopamine receptorHomo sapiens (human)
drinking behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(2) dopamine receptorHomo sapiens (human)
response to morphineD(2) dopamine receptorHomo sapiens (human)
pigmentationD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(2) dopamine receptorHomo sapiens (human)
negative regulation of innate immune responseD(2) dopamine receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IID(2) dopamine receptorHomo sapiens (human)
negative regulation of insulin secretionD(2) dopamine receptorHomo sapiens (human)
acid secretionD(2) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(2) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(2) dopamine receptorHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityD(2) dopamine receptorHomo sapiens (human)
response to axon injuryD(2) dopamine receptorHomo sapiens (human)
branching morphogenesis of a nerveD(2) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(2) dopamine receptorHomo sapiens (human)
epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(2) dopamine receptorHomo sapiens (human)
release of sequestered calcium ion into cytosolD(2) dopamine receptorHomo sapiens (human)
dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of synapse structural plasticityD(2) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(2) dopamine receptorHomo sapiens (human)
excitatory postsynaptic potentialD(2) dopamine receptorHomo sapiens (human)
positive regulation of growth hormone secretionD(2) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeD(2) dopamine receptorHomo sapiens (human)
regulation of locomotion involved in locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
negative regulation of cellular response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor productionD(2) dopamine receptorHomo sapiens (human)
positive regulation of long-term synaptic potentiationD(2) dopamine receptorHomo sapiens (human)
hyaloid vascular plexus regressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of neuron migrationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(2) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(2) dopamine receptorBos taurus (cattle)
negative regulation of prolactin secretionD(2) dopamine receptorBos taurus (cattle)
negative regulation of lactationD(2) dopamine receptorBos taurus (cattle)
positive regulation of mammary gland involutionD(2) dopamine receptorBos taurus (cattle)
hyaloid vascular plexus regressionD(2) dopamine receptorBos taurus (cattle)
positive regulation of MAP kinase activityD(4) dopamine receptorHomo sapiens (human)
behavioral fear responseD(4) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(4) dopamine receptorHomo sapiens (human)
response to amphetamineD(4) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(4) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
adult locomotory behaviorD(4) dopamine receptorHomo sapiens (human)
positive regulation of sodium:proton antiporter activityD(4) dopamine receptorHomo sapiens (human)
positive regulation of kinase activityD(4) dopamine receptorHomo sapiens (human)
response to histamineD(4) dopamine receptorHomo sapiens (human)
social behaviorD(4) dopamine receptorHomo sapiens (human)
regulation of dopamine metabolic processD(4) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(4) dopamine receptorHomo sapiens (human)
fear responseD(4) dopamine receptorHomo sapiens (human)
regulation of circadian rhythmD(4) dopamine receptorHomo sapiens (human)
positive regulation of MAP kinase activityD(4) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(4) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(4) dopamine receptorHomo sapiens (human)
rhythmic processD(4) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(4) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(4) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(4) dopamine receptorHomo sapiens (human)
inhibitory postsynaptic potentialD(4) dopamine receptorHomo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationD(4) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(4) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerD(4) dopamine receptorHomo sapiens (human)
chemical synaptic transmissionD(4) dopamine receptorHomo sapiens (human)
response to ethanolD(3) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(3) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
learning or memoryD(3) dopamine receptorHomo sapiens (human)
learningD(3) dopamine receptorHomo sapiens (human)
locomotory behaviorD(3) dopamine receptorHomo sapiens (human)
visual learningD(3) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(3) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(3) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(3) dopamine receptorHomo sapiens (human)
response to histamineD(3) dopamine receptorHomo sapiens (human)
social behaviorD(3) dopamine receptorHomo sapiens (human)
response to cocaineD(3) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(3) dopamine receptorHomo sapiens (human)
response to morphineD(3) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(3) dopamine receptorHomo sapiens (human)
positive regulation of mitotic nuclear divisionD(3) dopamine receptorHomo sapiens (human)
acid secretionD(3) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(3) dopamine receptorHomo sapiens (human)
negative regulation of oligodendrocyte differentiationD(3) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(3) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(3) dopamine receptorHomo sapiens (human)
musculoskeletal movement, spinal reflex actionD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(3) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(3) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(3) dopamine receptorHomo sapiens (human)
positive regulation of dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(3) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(3) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(3) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(3) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(3) dopamine receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (18)

Processvia Protein(s)Taxonomy
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(2) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(2) dopamine receptorHomo sapiens (human)
protein bindingD(2) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(2) dopamine receptorHomo sapiens (human)
dopamine bindingD(2) dopamine receptorHomo sapiens (human)
ionotropic glutamate receptor bindingD(2) dopamine receptorHomo sapiens (human)
identical protein bindingD(2) dopamine receptorHomo sapiens (human)
heterocyclic compound bindingD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(2) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(4) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(4) dopamine receptorHomo sapiens (human)
protein bindingD(4) dopamine receptorHomo sapiens (human)
potassium channel regulator activityD(4) dopamine receptorHomo sapiens (human)
SH3 domain bindingD(4) dopamine receptorHomo sapiens (human)
dopamine bindingD(4) dopamine receptorHomo sapiens (human)
identical protein bindingD(4) dopamine receptorHomo sapiens (human)
metal ion bindingD(4) dopamine receptorHomo sapiens (human)
epinephrine bindingD(4) dopamine receptorHomo sapiens (human)
norepinephrine bindingD(4) dopamine receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityD(4) dopamine receptorHomo sapiens (human)
neurotransmitter receptor activityD(4) dopamine receptorHomo sapiens (human)
serotonin bindingD(4) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(3) dopamine receptorHomo sapiens (human)
protein bindingD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(3) dopamine receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Processvia Protein(s)Taxonomy
Golgi membraneD(2) dopamine receptorHomo sapiens (human)
acrosomal vesicleD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliumD(2) dopamine receptorHomo sapiens (human)
lateral plasma membraneD(2) dopamine receptorHomo sapiens (human)
endocytic vesicleD(2) dopamine receptorHomo sapiens (human)
axonD(2) dopamine receptorHomo sapiens (human)
dendriteD(2) dopamine receptorHomo sapiens (human)
synaptic vesicle membraneD(2) dopamine receptorHomo sapiens (human)
sperm flagellumD(2) dopamine receptorHomo sapiens (human)
dendritic spineD(2) dopamine receptorHomo sapiens (human)
perikaryonD(2) dopamine receptorHomo sapiens (human)
axon terminusD(2) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(2) dopamine receptorHomo sapiens (human)
ciliary membraneD(2) dopamine receptorHomo sapiens (human)
non-motile ciliumD(2) dopamine receptorHomo sapiens (human)
dopaminergic synapseD(2) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(2) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(2) dopamine receptorHomo sapiens (human)
presynaptic membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
Golgi membraneD(2) dopamine receptorBos taurus (cattle)
centrosomeD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(4) dopamine receptorHomo sapiens (human)
membraneD(4) dopamine receptorHomo sapiens (human)
postsynapseD(4) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(4) dopamine receptorHomo sapiens (human)
dendriteD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
synapseD(3) dopamine receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (50)

Assay IDTitleYearJournalArticle
AID169627Evaluated for DOPAC level in nonpretreated habituated rats after subcuteneous dose of 100 micro mol/kg in rat striatum1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
AID176786In vivo DOPA accumulation in reserpine treated rat striatum system by subcutaneous administration; NT denotes not tested1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID176767In vivo DOPA accumulation in non pre-treated rat striatal system following s.c. administration.1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID62592Ability to displace the Dopamine receptor agonist DiPr-5,6-ADTN from rat striatal binding sites in vivo at a dose of 204 umol/kg by subcutaneous administration1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID168658Evaluated in rat accumbens for the effect on dopamine release and metabolism in brain dialysis model after administration of 50 umol / kg subcutaneously1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID169241Induced locomotor stimulation was determined in non pretreated rats at a dose of 13 umol/kg by subcutaneous administration1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID62743Compound was tested for agonistic activity against D2 receptor from cloned CHO cells, used [3H]U-86170 as radioligand1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Comparison of 5-HT1A and dopamine D2 pharmacophores. X-ray structures and affinities of conformationally constrained ligands.
AID176268Locomotory activity was determined in reserpine pretreated rats at a dose of 52 umol/kg by subcutaneous administration. Value is the accumulation counts/30 min;NT denotes not tested1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID65415Compound was tested for antagonistic activity against D2 receptor from rat striatum, used [3H]raclopride as radioligand1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Comparison of 5-HT1A and dopamine D2 pharmacophores. X-ray structures and affinities of conformationally constrained ligands.
AID65133Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybrid pharmacophore- and structure-based database searching approach.
AID168130Evaluated for DOPA accumulation in striatum of nonpretreated rat at 52 umol / kg administered subcutaneously1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID62338Evaluated for binding towards Dopamine receptor D2 using [3H]-spiperone as radioligand, in cloned mammalian receptors expressed in CHO-K1 cells1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID168320Evaluated for rat locomotor activity in nonpretreated habituated rats at 25 umol / kg1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID168657Evaluated in rat accumbens for the effect onDOPAC release and metabolism in brain dialysis model after administration of 50 umol / kg subcutaneously1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID196527Change in rectal temperature induced by DiPr-5,6-ADTN at a dose of 52 umol/kg of compound by subcutaneous administration1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID169399Induced locomotor stimulation in non pre-treated rats by 52 umol/kg s.c. administration.1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID168132Evaluated for DOPA accumulation in striatum of reserpine pretreated rat at 52 umol / kg administered subcutaneously1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID168003Evaluated for DOPA accumulation in limbic region of nonpretreated rat at 13 umol / kg administered subcutaneously1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID3480Binding affinity against 5-hydroxytryptamine 1A receptor from bovine hippocampus, used [3H]8-OH-DPAT as radioligand1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Comparison of 5-HT1A and dopamine D2 pharmacophores. X-ray structures and affinities of conformationally constrained ligands.
AID168030Rat locomotor activity in reserpine pretreated rats and accumulated counts / 30 min is calculated1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID65560Binding towards Dopamine receptor D2 using [3H]spiperone from rat striatal membrane1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID65786Binding towards Dopamine receptor D3 expressed in CHO-K1 cells using [3H]spiperone 1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID62597Ability to displace the Dopamine receptor agonist DiPr-5,6-ADTN from rat striatal binding sites in vivo at a dose of 52 umol/kg by subcutaneous administration1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID62589In vivo displacement of DiPr-5,6-ADTN from Dopamine receptors in rat striatum1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID62337Binding towards Dopamine receptor D2 expressed in CHO-K1 cells using [3H]U-861701993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID168660Evaluated in rat striatum for the effect on dopamine release and metabolism in brain dialysis model after administration of 50 umol / kg subcutaneously1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID63849Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone 1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID176785In vivo DOPA accumulation in reserpine treated rat limbic system by subcutaneous administration; NT denotes not tested1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID168318Evaluated for rat locomotor activity in nonpretreated habituated rats at 100 umol / kg1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID227608Intrinsic activity against dopamine D 2 receptor1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Comparison of 5-HT1A and dopamine D2 pharmacophores. X-ray structures and affinities of conformationally constrained ligands.
AID168127Evaluated for DOPA accumulation in striatum of nonpretreated rat at 13 umol / kg administered subcutaneously1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID170603((+)-UH-232) induced locomotor stimulation was determined in non pretreated rats at a dose of 204 umol/kg by subcutaneous administration1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID168659Evaluated in rat striatum for the effect on DOPAC release and metabolism in brain dialysis model after administration of 50 umol / kg subcutaneously1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID168124Evaluated for DOPA accumulation in limbic region of reserpine pretreated rat at 52 umol / kg administered subcutaneously1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID65559Evaluated for binding towards Dopamine receptor D2 using [3H]N-0437 as radioligand from rat striatal membrane1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID168317Evaluated for rat locomotor activity in nonhabituated rats at 52 umol / kg administered subcutaneously1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID13531Area under curve (AUC) is the drug concentrations in blood samples of rats with arterial catheters at 5 min and 12 hr plotted against time1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID168120Evaluated for DOPA accumulation in limbic region of nonpretreated rat at 52 umol / kg administered subcutaneously1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID176762In vivo DOPA accumulation in non pre-treated rat limbic system following s.c. administration.1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID169396Locomotory activity was determined in non pretreated rats at a dose of 3.2 umol/kg by subcutaneous administration1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID194723Evaluated biochemically in nonpretreated habituated rats for (100 uM/kg) subcuteneous dose, Value expressed as locomotor activity (LMA)1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
AID196525Change in rectal temperature induced by DiPr-5,6-ADTN at a dose of 204 umol/kg of compound by subcutaneous administration1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID196524Change in rectal temperature induced by DiPr-5,6-ADTN at a dose of 13 umol/kg of compound by subcutaneous administration1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID170605((+)-UH-232) induced locomotor stimulation was determined in non pretreated rats at a dose of 52 umol/kg by subcutaneous administration1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID168313Evaluated for rat locomotor activity in nonhabituated rats at 13 umol / kg administered subcutaneously1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1345898Rat D3 receptor (Dopamine receptors)1990Nature, Sep-13, Volume: 347, Issue:6289
Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.
AID1345833Human D3 receptor (Dopamine receptors)1995The Journal of pharmacology and experimental therapeutics, Nov, Volume: 275, Issue:2
Functional correlates of dopamine D3 receptor activation in the rat in vivo and their modulation by the selective antagonist, (+)-S 14297: 1. Activation of postsynaptic D3 receptors mediates hypothermia, whereas blockade of D2 receptors elicits prolactin
AID1345833Human D3 receptor (Dopamine receptors)1992European journal of pharmacology, Apr-10, Volume: 225, Issue:4
Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (37)

TimeframeStudies, This Drug (%)All Drugs %
pre-19908 (21.62)18.7374
1990's25 (67.57)18.2507
2000's2 (5.41)29.6817
2010's0 (0.00)24.3611
2020's2 (5.41)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.00

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index20.00 (24.57)
Research Supply Index3.64 (2.92)
Research Growth Index4.86 (4.65)
Search Engine Demand Index29.35 (26.88)
Search Engine Supply Index4.00 (0.95)

This Compound (20.00)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other37 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]