Page last updated: 2024-12-04

sk&f 81297

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID1218
CHEMBL ID353335
CHEBI ID91517
SCHEMBL ID398776
MeSH IDM0184029

Synonyms (44)

Synonym
gtpl938
r(+)skf81297
skf-81,297
PDSP2_001510
skf 81297
PDSP1_001526
NCGC00163159-01
sk&f 81297
skf-81297
6-chloro-2,3,4,5-tetrahydro-1-phenyl-1h-3-benzazepine-7,8-diol
1h-3-benzazepine-7,8-diol, 6-chloro-2,3,4,5-tetrahydro-1-phenyl-
sk&f-81297
LOPAC0_001162
NCGC00025166-02
6-chloro-pb hydrobromide
NCGC00015910-04
6-chloro-1-phenyl-2,3,4,5-tetrahydro-1h-3-benzazepine-7,8-diol
L000565
71636-61-8
CHEMBL353335
9-chloro-5-phenyl-2,3,4,5-tetrahydro-1h-3-benzazepine-7,8-diol
skf81297
CCG-205236
cas_1218
6-chloro-1-phenyl-2,3,4,5-tetrahydro-1h-benzo[d]azepine-7,8-diol; hydrobromide
cid_11957706
nsc_1218
bdbm86282
NCGC00015910-03
unii-9gbp09e08k
9gbp09e08k ,
1h-3-benzazepine-7,8-diol,6-chloro-2,3,4,5-tetrahydro-1-phenyl-
DTXSID3043815
GHWJEDJMOVUXEC-UHFFFAOYSA-N
6-chloro-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1h-3-benzazepine
SCHEMBL398776
6-chloro-1-phenyl-2,3,4,5-tetrahydro-1h-benzo[d]azepine-7,8-diol
CHEBI:91517
BRD-A09828896-004-04-5
SDCCGSBI-0051129.P002
NCGC00015910-08
(r)-skf-81297 (hydrobromide)
1h-3-benzazepine-7,8-diol, 6-chloro-2,3,4,5-tetrahydro-1-phenyl-, hydrobromide, (1r)- (9ci)
6-chlor-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1h-3-benzazepin

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
"0 mg/kg) produced dose-dependent rightward shifts of the (+/-)BAY k 8644 dose-response curve."( Modification of the behavioral effects of (+/-)BAY k 8644, cocaine and d-amphetamine by L-type calcium channel blockers in squirrel monkeys.
Barrett, JE; Rosenzweig-Lipson, S, 1995
)
0.29
"The objective of the present study was to demonstrate an enhancement of the acoustic startle response by dopamine D1 receptor agonists and to characterize this effect pharmacologically in terms of dose-response and selective antagonism at both the dopamine D1 and D2 receptor using a varied range of startle-eliciting intensities."( Enhancement of the acoustic startle response in rats by the dopamine D1 receptor agonist SKF 82958.
Davis, M; Meloni, EG, 1999
)
0.3
" Mild and advanced parkinsonism in nonhuman primates can be produced with fixed dosing regimens of MPTP."( D(1) dopamine receptor agonists are more effective in alleviating advanced than mild parkinsonism in 1-methyl-4-phenyl-1,2,3, 6-tetrahydropyridine-treated monkeys.
Goulet, M; Madras, BK, 2000
)
0.31
" Furthermore, the inhibitory effects on striatal nerve cell firing rate by the D1 receptor agonist SKF 81297 were not different in noninnervated or reinnervated areas of the striatum compared to the control side as seen from the dose-response curves."( Fetal ventral mesencephalic grafts functionally reduce the dopamine D2 receptor supersensitivity in partially dopamine reinnervated host striatum.
Andbjer, B; Fuxe, K; Kehr, J; Strömberg, I, 2000
)
0.31
" In this case, increasing concentrations of spiperone caused a change in the dose-response curve from hyperbolic to bell-shaped as the concentration of spiperone was increased."( Patterns of cyclic AMP formation by coexpressed D1 and D2L dopamine receptors in HEK 293 cells.
Ashby, B; Sakolsky, DJ, 2001
)
0.31
" Stimulus-generalization curves were generated by cumulative dosing for d-amphetamine (0."( Caffeine induces differential cross tolerance to the amphetamine-like discriminative stimulus effects of dopaminergic agonists.
Holtzman, SG; Jain, R, 2005
)
0.33
" drug injection, combining heroin with cocaine shifted the heroin dose-response function leftward, and isobolographic analysis indicated that the combined effects were dose-additive."( Modulation of heroin and cocaine self-administration by dopamine D1- and D2-like receptor agonists in rhesus monkeys.
Platt, DM; Rowlett, JK; Spealman, RD; Yao, WD, 2007
)
0.34
" We dosed wild-type mice, dopamine 1 receptor knockout mice and dopamine 5 receptor knockout mice undergoing casting-induced disuse atrophy with SKF 81297 to determine if activation of the dopamine 1 and dopamine 5 receptors results in hypertrophy of non-atrophying skeletal muscle and preservation of atrophying skeletal muscle mass and force production."( Activation of the dopamine 1 and dopamine 5 receptors increase skeletal muscle mass and force production under non-atrophying and atrophying conditions.
Dietrich, JA; Dolan, ET; Hinkle, RT; Isfort, RJ; Lefever, FR; Reichart, DL; Sibley, DR, 2011
)
0.37
" Dosing dopamine 5 receptor knockout mice with SKF 81297 did not significantly preserve EDL and soleus muscle mass and force although wild-type mouse EDL mass and force was significantly preserved SKF 81297 treatment."( Activation of the dopamine 1 and dopamine 5 receptors increase skeletal muscle mass and force production under non-atrophying and atrophying conditions.
Dietrich, JA; Dolan, ET; Hinkle, RT; Isfort, RJ; Lefever, FR; Reichart, DL; Sibley, DR, 2011
)
0.37
" Following a 2-day drug-free period, dose-response curves for hyperactivity produced by MDMA (2."( Repeated exposure to MDMA and amphetamine: sensitization, cross-sensitization, and response to dopamine D₁- and D₂-like agonists.
Bradbury, S; Gittings, D; Schenk, S, 2012
)
0.38
" This dose-response curve was shifted to the left in stressed animals as the effectiveness of SKF 81297 (as compared with either vehicle-treated controls or stressed animals) was found only after the administration of lower drug doses (0."( Dopamine D1 receptor modulation of set shifting: the role of stress exposure.
Nikiforuk, A, 2012
)
0.38
" These changes include a leftward shift in the dose-response to a D1-like agonist that indicates a behavioral D1R hypersensitivity, a shift from PKA to ERK intracellular signaling cascades upon D1R activation, and a reduction in the density of bridging collaterals from D1R-expressing neurons to pallidal areas."( D1 receptor hypersensitivity in mice with low striatal D2 receptors facilitates select cocaine behaviors.
Alvarez, VA; Bocarsly, ME; Bock, R; Dobbs, LK; Eberhart, L; Kaplan, AR; Phamluong, K; Ron, D; Shin, JH, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzazepineA group of two-ring heterocyclic compounds consisting of a benzene ring fused to an azepine ring.
[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 (19)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
dopamine D1 receptorHomo sapiens (human)Potency0.00650.00521.30228.1995AID624455
glp-1 receptor, partialHomo sapiens (human)Potency7.30780.01846.806014.1254AID624148
thioredoxin reductaseRattus norvegicus (Norway rat)Potency23.77810.100020.879379.4328AID488773; AID588453
phosphopantetheinyl transferaseBacillus subtilisPotency50.11870.141337.9142100.0000AID1490
GLS proteinHomo sapiens (human)Potency1.12200.35487.935539.8107AID624146
TDP1 proteinHomo sapiens (human)Potency8.19950.000811.382244.6684AID686978; AID686979
DNA polymerase III, partialBacillus subtilisPotency26.67951.062114.152826.6795AID485295
hypothetical protein, conservedTrypanosoma bruceiPotency33.80780.223911.245135.4813AID624147
regulator of G-protein signaling 4Homo sapiens (human)Potency17.84770.531815.435837.6858AID504845
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency6.56660.035520.977089.1251AID504332
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency26.12160.016525.307841.3999AID602332
D(1A) dopamine receptorHomo sapiens (human)Potency0.04320.02245.944922.3872AID488981; AID488982; AID488983
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency50.11870.354828.065989.1251AID504847
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency26.12160.00378.618923.2809AID2668
survival motor neuron protein isoform dHomo sapiens (human)Potency35.48130.125912.234435.4813AID1458
Ataxin-2Homo sapiens (human)Potency39.81070.011912.222168.7989AID588378
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency2.39340.060110.745337.9330AID485368
[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(1A) dopamine receptorHomo sapiens (human)Ki0.01500.00010.836310.0000AID1633730
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
D(1A) dopamine receptorHomo sapiens (human)EC50 (µMol)3.28820.00020.47959.5000AID1598361; AID1633726; AID1633728
D(1B) dopamine receptorHomo sapiens (human)EC50 (µMol)0.00140.00140.04100.1000AID1633736
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (70)

Processvia Protein(s)Taxonomy
temperature homeostasisD(1A) dopamine receptorHomo sapiens (human)
conditioned taste aversionD(1A) dopamine receptorHomo sapiens (human)
behavioral fear responseD(1A) dopamine receptorHomo sapiens (human)
regulation of protein phosphorylationD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(1A) dopamine receptorHomo sapiens (human)
response to amphetamineD(1A) dopamine receptorHomo sapiens (human)
protein import into nucleusD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
activation of adenylate cyclase activityD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
synapse assemblyD(1A) dopamine receptorHomo sapiens (human)
memoryD(1A) dopamine receptorHomo sapiens (human)
mating behaviorD(1A) dopamine receptorHomo sapiens (human)
grooming behaviorD(1A) dopamine receptorHomo sapiens (human)
adult walking behaviorD(1A) dopamine receptorHomo sapiens (human)
visual learningD(1A) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(1A) dopamine receptorHomo sapiens (human)
astrocyte developmentD(1A) dopamine receptorHomo sapiens (human)
dopamine transportD(1A) dopamine receptorHomo sapiens (human)
transmission of nerve impulseD(1A) dopamine receptorHomo sapiens (human)
neuronal action potentialD(1A) dopamine receptorHomo sapiens (human)
dentate gyrus developmentD(1A) dopamine receptorHomo sapiens (human)
striatum developmentD(1A) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(1A) dopamine receptorHomo sapiens (human)
positive regulation of cell migrationD(1A) dopamine receptorHomo sapiens (human)
peristalsisD(1A) dopamine receptorHomo sapiens (human)
operant conditioningD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, glutamatergicD(1A) dopamine receptorHomo sapiens (human)
regulation of dopamine metabolic processD(1A) dopamine receptorHomo sapiens (human)
vasodilationD(1A) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(1A) dopamine receptorHomo sapiens (human)
maternal behaviorD(1A) dopamine receptorHomo sapiens (human)
positive regulation of potassium ion transportD(1A) dopamine receptorHomo sapiens (human)
glucose importD(1A) dopamine receptorHomo sapiens (human)
habituationD(1A) dopamine receptorHomo sapiens (human)
sensitizationD(1A) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(1A) dopamine receptorHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolD(1A) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(1A) dopamine receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicD(1A) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(1A) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
long-term synaptic potentiationD(1A) dopamine receptorHomo sapiens (human)
long-term synaptic depressionD(1A) dopamine receptorHomo sapiens (human)
cellular response to catecholamine stimulusD(1A) dopamine receptorHomo sapiens (human)
modification of postsynaptic structureD(1A) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(1A) dopamine receptorHomo sapiens (human)
positive regulation of neuron migrationD(1A) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(1B) dopamine receptorHomo sapiens (human)
response to amphetamineD(1B) dopamine receptorHomo sapiens (human)
regulation of systemic arterial blood pressure by vasopressinD(1B) dopamine receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureD(1B) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(1B) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayD(1B) dopamine receptorHomo sapiens (human)
activation of adenylate cyclase activityD(1B) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(1B) dopamine receptorHomo sapiens (human)
chemical synaptic transmissionD(1B) dopamine receptorHomo sapiens (human)
associative learningD(1B) dopamine receptorHomo sapiens (human)
transmission of nerve impulseD(1B) dopamine receptorHomo sapiens (human)
negative regulation of NAD(P)H oxidase activityD(1B) dopamine receptorHomo sapiens (human)
wound healingD(1B) dopamine receptorHomo sapiens (human)
response to cocaineD(1B) dopamine receptorHomo sapiens (human)
positive regulation of adenylate cyclase activityD(1B) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(1B) dopamine receptorHomo sapiens (human)
regulation of female receptivityD(1B) dopamine receptorHomo sapiens (human)
sensitizationD(1B) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(1B) dopamine receptorHomo sapiens (human)
long-term synaptic depressionD(1B) dopamine receptorHomo sapiens (human)
cellular response to catecholamine stimulusD(1B) dopamine receptorHomo sapiens (human)
reactive oxygen species metabolic processD(1B) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(1B) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(1B) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(1B) dopamine receptorHomo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (11)

Processvia Protein(s)Taxonomy
dopamine neurotransmitter receptor activity, coupled via GsD(1A) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(1A) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(1A) dopamine receptorHomo sapiens (human)
protein bindingD(1A) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(1A) dopamine receptorHomo sapiens (human)
dopamine bindingD(1A) dopamine receptorHomo sapiens (human)
arrestin family protein bindingD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(1A) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via GsD(1B) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(1B) dopamine receptorHomo sapiens (human)
protein bindingD(1B) dopamine receptorHomo sapiens (human)
dopamine bindingD(1B) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(1B) dopamine receptorHomo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
nucleusD(1A) dopamine receptorHomo sapiens (human)
endoplasmic reticulum membraneD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1A) dopamine receptorHomo sapiens (human)
ciliumD(1A) dopamine receptorHomo sapiens (human)
presynaptic membraneD(1A) dopamine receptorHomo sapiens (human)
dendritic spineD(1A) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(1A) dopamine receptorHomo sapiens (human)
ciliary membraneD(1A) dopamine receptorHomo sapiens (human)
non-motile ciliumD(1A) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(1A) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1B) dopamine receptorHomo sapiens (human)
ciliumD(1B) dopamine receptorHomo sapiens (human)
brush border membraneD(1B) dopamine receptorHomo sapiens (human)
synapseD(1B) dopamine receptorHomo sapiens (human)
ciliary membraneD(1B) dopamine receptorHomo sapiens (human)
non-motile ciliumD(1B) dopamine receptorHomo sapiens (human)
plasma membraneD(1B) dopamine receptorHomo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (46)

Assay IDTitleYearJournalArticle
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
AID1633731Bias factor, ratio of EC50 for agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay to EC50 for agonist activity at wild type human D1R expresse2019ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5
Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists.
AID1633728Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay2019ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5
Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists.
AID1633727Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay relative to dopamine2019ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5
Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists.
AID1633732Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay2019ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5
Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists.
AID59135Effective Dose (ED15) required to decrease renal vascular resistance by 15% in anesthetized dogs administered intravenously1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Separation of potent central and renal dopamine agonist activity in substituted 6-chloro-2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepines.
AID1633734Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay2019ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5
Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists.
AID1633730Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay2019ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5
Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists.
AID57838Potency was expressed as the average maximum cumulative dose required to decrease renal vascular resistance by 15%1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Separation of potent central and renal dopamine agonist activity in substituted 6-chloro-2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepines.
AID1633737Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay relative to dopamine2019ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5
Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists.
AID1633726Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay2019ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5
Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists.
AID189189Central dopaminergic activity was determined by testing compound for its ability to produce contralateral rotation in lesioned rat after intracerebrally administration1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Separation of potent central and renal dopamine agonist activity in substituted 6-chloro-2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepines.
AID189190Central dopaminergic activity was determined by testing compound for its ability to produce contralateral rotation in lesioned rat after ip administration1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Separation of potent central and renal dopamine agonist activity in substituted 6-chloro-2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepines.
AID175474Central dopaminergic activity was determined by testing compound for dopamine agonist activity mediated by adenylase cyclase in rat1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Separation of potent central and renal dopamine agonist activity in substituted 6-chloro-2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepines.
AID1633735Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay relative to dopamine2019ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5
Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists.
AID1633729Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay relative to dopamine2019ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5
Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists.
AID234665Renal vasodilator activity was measured between ED20, heart rate (HR) test, and ED15 RVR.1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Separation of potent central and renal dopamine agonist activity in substituted 6-chloro-2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepines.
AID1598361Agonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
AID234666Renal vasodilator activity was measured between ED20, measure of mean arterial blood pressure (MABP) test, and ED15 RVR.1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Separation of potent central and renal dopamine agonist activity in substituted 6-chloro-2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepines.
AID234667Renal vasodilator activity was measured between ED30, measure in iliac vascular resistance (IVR) test, and ED15 RVR1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Separation of potent central and renal dopamine agonist activity in substituted 6-chloro-2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepines.
AID1633736Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay2019ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5
Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists.
AID1633733Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay relative to dopamine2019ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5
Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists.
AID1347167Vero cells viability 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.
AID1347153Confirmatory 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.
AID1347152Confirmatory screen NINDS 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.
AID1347149Furin counterscreen 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.
AID1347169Tertiary RLuc qRT-PCR qHTS assay 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.
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.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508628Confirmatory 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.
AID1347168HepG2 cells viability 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.
AID1347161Confirmatory screen NINDS Rhodamine 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.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1347015Rat D1 receptor (Dopamine receptors)1990European journal of pharmacology, Jun-12, Volume: 188, Issue:6
Dopamine receptor agonists: selectivity and dopamine D1 receptor efficacy.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (267)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (0.37)18.7374
1990's45 (16.85)18.2507
2000's129 (48.31)29.6817
2010's83 (31.09)24.3611
2020's9 (3.37)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.29

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.29 (24.57)
Research Supply Index5.62 (2.92)
Research Growth Index6.91 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.29)

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%
Other274 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]