Page last updated: 2024-11-07

uh 301

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

Description

UH 301: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID122187
CHEMBL ID22778
SCHEMBL ID5658541
MeSH IDM0177115

Synonyms (40)

Synonym
(s)-uh301
gtpl61
(-)-uh 301
(s)-uh 301
uh301
(s)-7-(dipropylamino)-4-fluoro-5,6,7,8-tetrahydronaphthalen-1-ol
lopac-u-108
lopac-u-109
NCGC00016070-02
NCGC00016070-01
PDSP1_000933
PDSP2_000919
127126-21-0
uh-301
uh 301
1-naphthalenol, 7-(dipropylamino)-4-fluoro-5,6,7,8-tetrahydro-, (s)-
5-fhdpat
LOPAC0_001236
NCGC00162373-01
NCGC00162373-02
CHEMBL22778 ,
bdbm50013019
7-dipropylamino-4-fluoro-5,6,7,8-tetrahydro-naphthalen-1-ol ((s)-uh301)
(s)-7-dipropylamino-4-fluoro-5,6,7,8-tetrahydro-naphthalen-1-ol
(7s)-7-(dipropylamino)-4-fluoro-5,6,7,8-tetrahydronaphthalen-1-ol
CCG-205310
unii-1g916imd7l
1g916imd7l ,
(s)-(-)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin
(s)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin
1-naphthalenol, 7-(dipropylamino)-4-fluoro-5,6,7,8-tetrahydro-, (7s)-
uh-301 free base, (s)-
SCHEMBL5658541
(7s)-7-(dipropylamino)-4-fluoro-5,6,7,8-tetrahydro-1-naphthalenol
DTXSID30925792
s(-)-uh-301 hydrochloride(s(-)-5-fluoro-8-hydroxy-dpat hydroc
(s)-uh-301 free base
Q27088892
SDCCGSBI-0051203.P002
DTXSID201034408

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" The present study describes the pharmacokinetic properties of (S)-UH-301 after subcutaneous administration in rats, using a newly developed HPLC-UV bioanalytical method."( An integrative pharmacokinetic and pharmacodynamic study of the 5-HT1A receptor antagonist (S)-UH-301 in the rat.
Lewander, T; Yan, H; Yu, H, 2002
)
0.31

Bioavailability

ExcerptReferenceRelevance
" The maximum plasma concentration of intranasal (S)-UH-301 occurred in about 7 min and the absolute bioavailability seemed to be complete (F=1."( Nasal absorption of (S)-UH-301 and its transport into the cerebrospinal fluid of rats.
Björk, E; Dahlin, M, 2000
)
0.31

Dosage Studied

ExcerptRelevanceReference
") and the dose-response curve for this effect of (R)-8-OH-DPAT was markedly shifted to the right by pretreatment with (S)-UH-301 (1."( The 5-HT1A receptor antagonist (S)-UH-301 blocks the qR)-8-OH-DPAT-induced inhibition of serotonergic dorsal raphe cell firing in the rat.
Arborelius, L; Hacksell, U; Höök, BB; Svensson, TH, 1994
)
0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (22)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
dopamine D1 receptorHomo sapiens (human)Potency7.30780.00521.30228.1995AID624455
thioredoxin reductaseRattus norvegicus (Norway rat)Potency0.35480.100020.879379.4328AID588453
15-lipoxygenase, partialHomo sapiens (human)Potency39.81070.012610.691788.5700AID887
GLS proteinHomo sapiens (human)Potency14.12540.35487.935539.8107AID624146
thyroid stimulating hormone receptorHomo sapiens (human)Potency39.81070.001318.074339.8107AID926; AID938
arylsulfatase AHomo sapiens (human)Potency8.49211.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency31.62280.035520.977089.1251AID504332
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency1.10800.00207.533739.8107AID891
chromobox protein homolog 1Homo sapiens (human)Potency89.12510.006026.168889.1251AID488953
mitogen-activated protein kinase 1Homo sapiens (human)Potency39.81070.039816.784239.8107AID995
flap endonuclease 1Homo sapiens (human)Potency5.32330.133725.412989.1251AID588795
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency11.78260.00106.000935.4813AID943; AID944
pyruvate kinase PKM isoform bHomo sapiens (human)Potency0.00632.511912.262825.1189AID954; AID958
[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)
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.08700.00010.532610.0000AID3830
D(2) dopamine receptorHomo sapiens (human)Ki3.76000.00000.651810.0000AID55449
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki6.08000.00010.949010.0000AID37325
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.05200.00010.739610.0000AID4017
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki6.08000.00000.575110.0000AID37325
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki3.18000.00000.14803.1800AID6652
Alpha-1B adrenergic receptorHomo sapiens (human)Ki6.08000.00000.471310.0000AID37325
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki6.08000.00000.965010.0000AID37325
[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)
5-hydroxytryptamine receptor 1AHomo sapiens (human)Kd0.02510.00010.95285.0119AID438555
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (119)

Processvia Protein(s)Taxonomy
behavioral fear response5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
gamma-aminobutyric acid signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of serotonin secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of vasoconstriction5-hydroxytryptamine receptor 1AHomo sapiens (human)
exploration behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of dopamine metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of hormone secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1AHomo sapiens (human)
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)
G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1B adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of cardiac muscle contractionAlpha-1B adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (15)

Processvia Protein(s)Taxonomy
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
receptor-receptor interaction5-hydroxytryptamine receptor 1AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
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)
protein bindingAlpha-1B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1B adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (26)

Processvia Protein(s)Taxonomy
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1AHomo sapiens (human)
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)
nucleusAlpha-1B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
caveolaAlpha-1B adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (56)

Assay IDTitleYearJournalArticle
AID55449Binding affinity was measured on cloned Human D2A Receptor which is labeled by [3H]raclopride2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Derivatives of (R)-1,11-methyleneaporphine: synthesis, structure, and interactions with G-protein coupled receptors.
AID172335in vivo antagonist activity was measured as flat body posture (FBP) in a behavioral response test in reserpinized rats at 3 mg/kg(sc) dose1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists.
AID188182The effect on the accumulation of 5-HTP in rat brain(limbic), by subcutaneous administration at a dose of 10(umol/kg)1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
(S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: a putative 5-HT1A-receptor antagonist.
AID4171Effect on 5-hydroxytryptamine 1A receptor mediated inhibition of VIP-stimulated cAMP production at dose of 0.1 uM + 1 uM 5-HT.1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Derivatives of (R)- and (S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: synthesis and interactions with 5-HT1A receptors.
AID4324Displacement of [3H]8-OH-DPAT from rat hippocampal 5-hydroxytryptamine 1A receptor1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
N-[2-[(substituted chroman-8-yl)oxy]ethyl]-4-(4-methoxyphenyl)butylamines: synthesis and wide range of antagonism at the human 5-HT1A receptor.
AID37325Binding affinity was evaluated against Alpha-1 adrenergic receptor on rat cortex using [3H]prazosin as radioligand1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists.
AID188185The effect on the accumulation of 5-HTP in rat brain(striatum), by subcutaneous administration at a dose of 32(umol/kg)1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
(S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: a putative 5-HT1A-receptor antagonist.
AID172337in vivo antagonist activity was measured as forepaw treading(FT) in a behavioral response test in reserpinized rats at 1 mg/kg(sc) dose1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists.
AID4017Binding affinity towards 5-hydroxytryptamine 1A receptor sites in cortical membranes using [3H]8-OH-DPAT as radioligand1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
(S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: a putative 5-HT1A-receptor antagonist.
AID181616Antagonistic effect on 5-HT syndrome or behavior of rat at the dose of 32 umol/kg with saline1993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
Derivatives of 2-(dipropylamino)tetralin: effect of the C8-substituent on the interaction with 5-HT1A receptors.
AID181618Antagonistic effect on 5-HT syndrome or behavior of rat induced by (R)-8-hydroxy-DPAT at the dose of 32 and 1.0 umol/kg1993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
Derivatives of 2-(dipropylamino)tetralin: effect of the C8-substituent on the interaction with 5-HT1A receptors.
AID228853Effect on 5-hydroxytryptamine 1A receptor mediated inhibition of VIP-stimulated cAMP production at dose of 1 uM1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Derivatives of (R)- and (S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: synthesis and interactions with 5-HT1A receptors.
AID4025Binding affinity was evaluated against 5-hydroxytryptamine 1A receptor on rat hippocampus using [3H]8-OH-DPAT as radioligand1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists.
AID36440In vitro radioligand binding assay on adrenaline Alpha-1 adrenergic receptor of rat cortex using [3H]- prazosin1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
N-[2-[(substituted chroman-8-yl)oxy]ethyl]-4-(4-methoxyphenyl)butylamines: synthesis and wide range of antagonism at the human 5-HT1A receptor.
AID172334in vivo antagonist activity was measured as flat body posture (FBP) in a behavioral response test in reserpinized rats at 1 mg/kg(sc) dose1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists.
AID172339in vivo antagonist activity was measured as forepaw treading(FT) in a behavioral response test in reserpinized rats upon subcutaneous administration1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists.
AID4179Effect on 5-hydroxytryptamine 1A receptor mediated inhibition of VIP-stimulated cAMP production at dose of 1 uM+ 3 uM 5-HT.1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Derivatives of (R)- and (S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: synthesis and interactions with 5-HT1A receptors.
AID4169Effect against 5-hydroxytryptamine 1A receptor mediated inhibition of VIP-stimulated cAMP production at 0.1 uM dose1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Derivatives of (R)- and (S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: synthesis and interactions with 5-HT1A receptors.
AID65750In vitro radioligand binding assay on Dopamine receptor D2 of rat striatum using [3H]- spiperone1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
N-[2-[(substituted chroman-8-yl)oxy]ethyl]-4-(4-methoxyphenyl)butylamines: synthesis and wide range of antagonism at the human 5-HT1A receptor.
AID6652Binding affinity against Rat 5-hydroxytryptamine 7 receptor using [3H]5-HT2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Derivatives of (R)-1,11-methyleneaporphine: synthesis, structure, and interactions with G-protein coupled receptors.
AID3830Binding affinity was measured on cloned Human 5-hydroxytryptamine 1A receptor which is labeled by [3H]8-OH-DPAT2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Derivatives of (R)-1,11-methyleneaporphine: synthesis, structure, and interactions with G-protein coupled receptors.
AID4023Binding affinity against rat hippocampal 5-hydroxytryptamine 1A (5-HT1A) receptor determined using [3H]8-OH-DPAT as radioligand1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Derivatives of (R)- and (S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: synthesis and interactions with 5-HT1A receptors.
AID57538The effect on the accumulation of DOPA in rat brain(striatum), by subcutaneous administration at a dose of 10(umol/kg)1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
(S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: a putative 5-HT1A-receptor antagonist.
AID233876Selectivity for 5-HT1A receptor of rat hippocampus and alpha-1 adrenergic receptor of rat cortex.1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists.
AID438555Binding affinity to 5HT1A receptor2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Physical binding pocket induction for affinity prediction.
AID228140Binding affinity (Ki) ratio of D2 receptor of rat striatum and 5-HT1A receptor of rat hippocampus1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists.
AID4018Binding affinity towards 5-hydroxytryptamine 1A receptor sites, in rat striatum membranes using [3H]- sandoz 205-501 as radioligand1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
(S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: a putative 5-HT1A-receptor antagonist.
AID4173Effect on 5-hydroxytryptamine 1A receptor mediated inhibition of VIP-stimulated cAMP production at dose of 10 uM1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Derivatives of (R)- and (S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: synthesis and interactions with 5-HT1A receptors.
AID3567Antagonist activity was measured against CHO cells expressing the human 5-hydroxytryptamine 1A receptor in a forskolin stimulated adenylate cyclase (FSC) assay1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists.
AID190307Antagonistic effect on body temperature of rat induced by (R)-1 at the dose of 32 umol/kg with saline1993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
Derivatives of 2-(dipropylamino)tetralin: effect of the C8-substituent on the interaction with 5-HT1A receptors.
AID172338in vivo antagonist activity was measured as forepaw treading(FT) in a behavioral response test in reserpinized rats at 3 mg/kg(sc) dose1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists.
AID190306Antagonistic effect on body temperature of rat induced by (R)-1 at the dose of 32 and 1.0 umol/kg of compound (R)-11993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
Derivatives of 2-(dipropylamino)tetralin: effect of the C8-substituent on the interaction with 5-HT1A receptors.
AID57536The effect on the accumulation of DOPA in rat brain(limbic), by subcutaneous administration at a dose of 10(umol/kg)1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
(S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: a putative 5-HT1A-receptor antagonist.
AID172336in vivo antagonist activity was measured as flat body posture (FBP) in a behavioral response test in reserpinized rats upon subcutaneous administration1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists.
AID63956Binding affinity was evaluated against Dopamine receptor D2 on rat striatum using [3H]spiperone as radioligand; ND = Not determined1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists.
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.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
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.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
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.
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.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
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.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
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.
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.
AID624215Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1A1998European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3
Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study.
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)1998European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3
Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (51)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's33 (64.71)18.2507
2000's8 (15.69)29.6817
2010's5 (9.80)24.3611
2020's5 (9.80)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.12

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 Index18.12 (24.57)
Research Supply Index3.97 (2.92)
Research Growth Index4.46 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.12)

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%
Other52 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]