Page last updated: 2024-12-04

5-carboxamidotryptamine

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Description

5-carboxamidotryptamine: agonist of 5-HT receptor; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID1809
CHEMBL ID18840
CHEBI ID48292
SCHEMBL ID2677791
MeSH IDM0136157

Synonyms (51)

Synonym
gtpl4
3-(2-aminoethyl-1h-indole-5-carboxamide
1h-indole-5-carboxamide, 3-(2-aminoethyl)-
PDSP2_000762
lopac-c-117
NCGC00015182-01
NCGC00024598-01 ,
tocris-0458
BIOMOL-NT_000109
LOPAC0_000352
PDSP1_000774
BPBIO1_001405
chembl18840 ,
[3h]-5-carboxamide tryptamine
[3h]-5-carboxamidotryptamine
[3h]-5-ct
bdbm21392
[3h]-5-carboxyamidotryptamine
5-carboxamidotryptamine
NCGC00024598-03
NCGC00024598-02
5-carboxamide tryptamine
5-ct
5-carboxyamidotryptamine
CHEBI:48292 ,
74885-09-9
3-(2-aminoethyl)-1h-indole-5-carboxamide
NCGC00015182-05
L000077
A22556
CCG-204447
NCGC00015182-03
NCGC00015182-04
NCGC00015182-02
91h76044o0 ,
unii-91h76044o0
WKZLNEWVIAGNAW-UHFFFAOYSA-N
3-(2-amino-ethyl)-1h-indole-5-carboxylic acid amide
SCHEMBL2677791
AKOS027380025
Q4639580
3-(2-aminoethyl)-1h-indole-5-carboxylic acid amide
3-(2-aminoethyl)-1h-indole-5-carboximidic acid
DTXSID60996379
BRD-K92382976-103-01-8
SDCCGSBI-0050340.P002
NCGC00015182-09
3-(2-amino-ethyl)-1h-indole-5-carboxylicacidamide
PD051007
3-(2-azanylethyl)-1h-indole-5-carboxamide
8k3 ,

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" The objective of this work was to identify potent and selective 5-HT1D receptor agonists with high oral bioavailability and low central nervous system penetration."( Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.
Baker, R; Beer, MS; Davey, WB; Guiblin, AR; Jelley, RA; Reeve, AJ; Routledge, H; Sternfeld, F; Street, LJ; Watt, AP, 1995
)
0.29

Dosage Studied

ExcerptRelevanceReference
" In membrane preparations, 8-OH-DPAT dose-response curve was shifted leftwards when the receptor concentration became higher whereas the corresponding shift was smaller for 5-HT and absent for 5-CT."( Differential coupling of 5-HT1A receptors occupied by 5-HT or 8-OH-DPAT to adenylyl cyclase.
Bockaert, J; Varrault, A, 1992
)
0.28
" pretreatment (25 min) with morphine sulfate, 8-OH-DPAT, buspirone and 5-CT shifted the morphine sulfate dose-response curve 3- to 5-fold to the right."( Differential roles of 5-hydroxytryptamine1A and 5-hydroxytryptamine1B receptor subtypes in modulating spinal nociceptive transmission in mice.
Alhaider, AA; Wilcox, GL, 1993
)
0.29
" The dose-response curve obtained with the 5-HT1 receptor agonist, 5-carboxamidotryptamine (5-CT), was biphasic in arteries with endothelium; removal of the endothelium eliminated the first phase of the contraction."( Endothelial thromboxane production plays a role in the contraction caused by 5-hydroxytryptamine in rat basilar arteries.
Descombes, JJ; Devys, M; Laubie, M; Verbeuren, TJ, 1993
)
0.52
" Dose-response relationships were established for 5-HT in experiments in which each mouse was treated with a single dose of 5-HT without antagonist or after LY53857."( Serotonin-induced pulmonary responses are mediated by the 5-HT2 receptor in the mouse.
Cohen, ML; Drazen, JM; Martin, TR, 1994
)
0.29
"2 mumol/kg), GR-127,935 right-shifted the dose-response curve of sumatriptan."( The 5-HT1D receptor antagonist GR-127,935 prevents inhibitory effects of sumatriptan but not CP-122,288 and 5-CT on neurogenic plasma extravasation within guinea pig dura mater.
Cutrer, FM; Moskowitz, MA; Waeber, C; Yu, XJ, 1997
)
0.3
"0 nmol kg-1), produced significant rightward displacements of the dose-response curve for 5-CT in methoxamine-infused pithed animals pretreated with ketanserin (0."( Role of 5-ht7 receptors in the long-lasting hypotensive response induced by 5-hydroxytryptamine in the rat.
TerrĂ³n, JA, 1997
)
0.3
"05) and suppressed the dose-response curve for the 2C agonist."( Pharmacological characterization of serotonergic receptor activity in the hypoglossal nucleus.
Fenik, P; Veasey, SC, 2003
)
0.32
"2 microg) and higher doses (2 and 5 microg) of SB-269970-A were less effective, indicating a bell-shaped dose-response curve."( 5-HT7 receptor subtype as a mediator of the serotonergic regulation of luteinizing hormone release in the zona incerta.
Abu-Amara, M; Aldairy, C; Hagan, JJ; Siddiqui, A; Wilson, C, 2004
)
0.32
" The novel 5-HT7R antagonist 1-8 exhibited an antidepressant effect at a dose of 25mg/kg in the forced swimming test in mice and showed a U-shaped dose-response curve which typically appears in 5-HT7R antagonists such as SB-269970 and lurasidone."( Novel N-biphenyl-2-ylmethyl 2-methoxyphenylpiperazinylalkanamides as 5-HT7R antagonists for the treatment of depression.
Cho, H; Choo, H; Choo, IH; Keum, G; Kim, Y; Lee, K; Park, WK; Rhim, H; Tae, J, 2014
)
0.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
tryptaminesTryptamine and its substitution derivatives.
[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 (21)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency12.58930.025120.237639.8107AID886
Chain B, HADH2 proteinHomo sapiens (human)Potency12.58930.025120.237639.8107AID886
thyroid stimulating hormone receptorHomo sapiens (human)Potency6.30960.001318.074339.8107AID926; AID938
arylsulfatase AHomo sapiens (human)Potency2.68551.069113.955137.9330AID720538
D(1A) dopamine receptorHomo sapiens (human)Potency0.00410.02245.944922.3872AID488982
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency19.95260.00106.000935.4813AID943
[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)Ki0.00040.00010.532610.0000AID1570285; AID1798075; AID3830; AID3925
D(2) dopamine receptorHomo sapiens (human)Ki0.00050.00000.651810.0000AID1798075
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.00050.00010.601710.0000AID1798075
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.00030.00010.739610.0000AID4411
5-hydroxytryptamine receptor 1BHomo sapiens (human)Ki0.00130.00010.54859.2100AID4276
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki5.01190.00000.385510.0000AID5422
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki1.56590.00010.954910.0000AID4747; AID5650
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.00500.00031.29679.2440AID4699
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.00040.00000.14803.1800AID1798075; AID282108; AID296883; AID308128; AID391745; AID6650; AID6652; AID6666
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki0.00170.00030.380610.0000AID1384577; AID1739139; AID282108; AID6587; AID6611; AID6612; AID6678; AID776869
5-hydroxytryptamine receptor 5AHomo sapiens (human)Ki0.02000.00080.94335.1600AID6479; AID6480
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.86000.00020.522910.0000AID6514; AID6536
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)Ki0.00050.00050.00180.0035AID391745
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.00090.00000.437510.0000AID6587
5-hydroxytryptamine receptor 1DSus scrofa (pig)IC50 (µMol)0.00400.00030.64963.7153AID4857; AID4864
[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)Kd0.00040.00010.95285.0119AID438555
5-hydroxytryptamine receptor 7Homo sapiens (human)EC50 (µMol)0.00510.00060.03560.0832AID1704743
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (170)

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 internalization5-hydroxytryptamine receptor 1BHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of gamma-aminobutyric acid secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of serotonin secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of synaptic transmission, GABAergic5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to cocaine5-hydroxytryptamine receptor 1BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 1BHomo sapiens (human)
drinking behavior5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to ethanol5-hydroxytryptamine receptor 1BHomo sapiens (human)
bone remodeling5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to mineralocorticoid5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to alkaloid5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to xenobiotic stimulus5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 1BHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentration5-hydroxytryptamine receptor 1BHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferation5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of synaptic vesicle exocytosis5-hydroxytryptamine receptor 1BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1BHomo sapiens (human)
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
smooth muscle contraction5-hydroxytryptamine receptor 7Homo sapiens (human)
circadian rhythm5-hydroxytryptamine receptor 7Homo sapiens (human)
blood circulation5-hydroxytryptamine receptor 7Homo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 7Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 5AHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 5AHomo sapiens (human)
hippocampus development5-hydroxytryptamine receptor 5AHomo sapiens (human)
response to estradiol5-hydroxytryptamine receptor 5AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 5AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 5AHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 5AHomo sapiens (human)
cerebral cortex cell migration5-hydroxytryptamine receptor 6Homo sapiens (human)
positive regulation of TOR signaling5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 6Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (20)

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)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1BHomo sapiens (human)
voltage-gated calcium channel activity involved in regulation of presynaptic cytosolic calcium levels5-hydroxytryptamine receptor 1BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1BHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 7Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 5AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 5AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 5AHomo sapiens (human)
histamine receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
protein binding5-hydroxytryptamine receptor 6Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (34)

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)
endoplasmic reticulum5-hydroxytryptamine receptor 1BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
calyx of Held5-hydroxytryptamine receptor 1BHomo sapiens (human)
serotonergic synapse5-hydroxytryptamine receptor 1BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 1BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
trans-Golgi network membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
synapse5-hydroxytryptamine receptor 7Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 7Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 5AHomo sapiens (human)
perikaryon5-hydroxytryptamine receptor 5AHomo sapiens (human)
postsynaptic specialization membrane5-hydroxytryptamine receptor 5AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 5AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 5AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
cilium5-hydroxytryptamine receptor 6Homo sapiens (human)
synapse5-hydroxytryptamine receptor 6Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 6Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (165)

Assay IDTitleYearJournalArticle
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.
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.
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.
AID282112Agonist activity at 5-carboxamidotryptamine desensitized 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents.
AID6480Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
AID1571104Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 100 uM after 48 hrs by MTT assay relative to control2018MedChemComm, Nov-01, Volume: 9, Issue:11
Search for a 5-CT alternative.
AID4864Displacement of radioligand [3H]5-HT binding to 5-hydroxytryptamine 1D receptor in pig caudate membrane1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
Synthesis and serotonergic activity of 5-(oxadiazolyl)tryptamines: potent agonists for 5-HT1D receptors.
AID1704743Agonist activity at human 5HT7 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
AID5422Binding affinity against 5-hydroxytryptamine 2A receptor human cloned receptors in HEK 293 cells using [3H]ketanserin as radioligand2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
A novel ergot alkaloid as a 5-HT(1A) inhibitor produced by Dicyma sp.
AID282113Activity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileum2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents.
AID1571100Cytotoxicity against HEK293 cells assessed as cell viability at 100 uM after 48 hrs by MTT assay relative to control2018MedChemComm, Nov-01, Volume: 9, Issue:11
Search for a 5-CT alternative.
AID6671Agonistic activity against rat 5-HT7 adenyl cyclase expressed by HEK293 cells2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Characterization of the 5-HT(7) receptor. Determination of the pharmacophore for 5-HT(7) receptor agonism and CoMFA-based modeling of the agonist binding site.
AID6514Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
AID4699Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Central serotonin receptors as targets for drug research.
AID5452The compound was tested for binding affinity against 5-HT2A receptor1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Computer-aided design and synthesis of 5-substituted tryptamines and their pharmacology at the 5-HT1D receptor: discovery of compounds with potential anti-migraine properties.
AID1570294Competitive antagonist activity at human D2S receptor expressed in CHOK1 cells assessed as quinpirole mediated inhibition of forskolin induced cAMP accumulation by measuring parallel rightward shifts of quinpirole concentration-response curves incubated f
AID1704742Agonist activity at human 5HT7 receptor expressed in CHO-K1 cells at 10 uM by calcium 4 dye based FLIPR assay relative to control
AID308128Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells2007Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15
Bivalent ligand approach on 4-[2-(3-methoxyphenyl)ethyl]-1-(2-methoxyphenyl)piperazine: synthesis and binding affinities for 5-HT(7) and 5-HT(1A) receptors.
AID4867The compound was tested for intrinsic activity against 5-HT1D receptor1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Computer-aided design and synthesis of 5-substituted tryptamines and their pharmacology at the 5-HT1D receptor: discovery of compounds with potential anti-migraine properties.
AID391749Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction relative to 5-carboxamidotryptamine2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III.
AID1570293Antagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assay
AID1571093Retention time of the compound in rat liver microsomes in presence of NADPH generating system by UPLC analysis2018MedChemComm, Nov-01, Volume: 9, Issue:11
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AID1570291Agonist activity at human 5HT1A receptor expressed in HEK293 cell membranes assessed as maximal inhibition of forskolin induced cAMP production incubated for 24 hrs followed by forskolin addition by HTRF assay relative to control
AID6536Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
A novel ergot alkaloid as a 5-HT(1A) inhibitor produced by Dicyma sp.
AID4747Evaluated for the binding affinity to porcine choroid plexus at 5-hydroxytryptamine 2C receptor binding site by using [3H]-MES as a radioligand.1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Central serotonin receptors as targets for drug research.
AID6587Displacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptor2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
AID296883Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.
AID6611Binding affinity against 5-hydroxytryptamine 7 human receptors2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
A novel ergot alkaloid as a 5-HT(1A) inhibitor produced by Dicyma sp.
AID5126Binding affinity for 5-hydroxytryptamine 2 receptor was determined1993Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13
(+/-) 3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: a conformationally restricted analogue of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor.
AID1571106Mutagenicity in Salmonella typhimurium TA100 assessed as revertant colonies at 10 uM by Ames test2018MedChemComm, Nov-01, Volume: 9, Issue:11
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AID4411Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Binding of arylpiperazines, (aryloxy)propanolamines, and tetrahydropyridylindoles to the 5-HT1A receptor: contribution of the molecular lipophilicity potential to three-dimensional quantitative structure-affinity relationship models.
AID1281956Agonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as increase in cAMP level at 10 uM after 15 mins by HTRF assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Rational design in search for 5-phenylhydantoin selective 5-HT7R antagonists. Molecular modeling, synthesis and biological evaluation.
AID1571089Drug metabolism in human liver microsomes measured after 120 mins in presence of NADPH generating system by UPLC analysis2018MedChemComm, Nov-01, Volume: 9, Issue:11
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AID1571096Inhibition of CYP2D6 (unknown origin) assessed as residual activity at 10 uM using beetle D-luciferin as substrate by CYP450-Glo assay relative to control2018MedChemComm, Nov-01, Volume: 9, Issue:11
Search for a 5-CT alternative.
AID4869The compound was tested for binding affinity against 5-HT1D receptor1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Computer-aided design and synthesis of 5-substituted tryptamines and their pharmacology at the 5-HT1D receptor: discovery of compounds with potential anti-migraine properties.
AID1595179Agonist activity at 5-HT7 receptor (unknown origin) expressed in N1E-115 cells assessed as intracellular cAMP response amplitude by confocal laser scanning microscopy
AID3889Agonist efficacy on 5-hydroxytryptamine 1A receptor subtype1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors.
AID1570292Antagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as maximal inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assay relative to control
AID4857Binding activity against 5-hydroxytryptamine 1D receptor from pig caudate membrane using [3H]5-HT as radioligand1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.
AID4096Evaluated for the binding affinity to hippocampus striatal membranes at 5-hydroxytryptamine 1A receptor binding site by using [3H]-8-OH- DPAT as a radioligand.1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Central serotonin receptors as targets for drug research.
AID1570285Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cell membranes measured after 120 mins
AID1571091Drug metabolism in mouse liver microsomes measured after 120 mins in presence of NADPH generating system by UPLC analysis2018MedChemComm, Nov-01, Volume: 9, Issue:11
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AID1571103Hepatotoxicity against human HepG2 cells assessed as ATP level at 100 uM after 3 hrs by CellTiter-Glo luminescent cell viability assay relative to control2018MedChemComm, Nov-01, Volume: 9, Issue:11
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AID391748Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III.
AID391745Displacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cells2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III.
AID6662Maximal relaxation effect induced by 3 uM compound on substance P stimulated guinea pig ileum with 5-hydroxytryptamine 7 receptor nondesensitization2003Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4
Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones as 5-HT(7) receptor ligands.
AID6663Maximal relaxation effect induced by 3 uM compound on substance P stimulated guinea pig ileum with 5-hydroxytryptamine receptor desensitization2003Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4
Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones as 5-HT(7) receptor ligands.
AID6678Binding affinity of compound towards rodent 5-hydroxytryptamine 7 receptor2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
AID1384577Binding affinity to 5-HT7 receptor (unknown origin)2018Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
Structure-Activity Relationships and Therapeutic Potentials of 5-HT
AID1571105Hepatotoxicity against human HepG2 cells assessed as cell viability at 100 uM after 48 hrs by MTT assay relative to control2018MedChemComm, Nov-01, Volume: 9, Issue:11
Search for a 5-CT alternative.
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.
AID4455Binding affinity for 5-hydroxytryptamine 1A receptor was determined1993Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13
(+/-) 3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: a conformationally restricted analogue of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor.
AID1739139Displacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 60 mins by radioligand binding assay2020European journal of medicinal chemistry, Aug-01, Volume: 199Privileged scaffold-based design to identify a novel drug-like 5-HT
AID391758Agonist activity at human cloned 5HT1A receptor expressed in human HeLa cell membrane assessed as stimulation of [35S]GTPgammaS binding2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents.
AID1595155Effect on cAMP response in mouse N1E-115 cells at 10 uM by confocal laser scanning microscopy
AID6612Binding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligand2002Journal of medicinal chemistry, May-23, Volume: 45, Issue:11
2a-[4-(Tetrahydropyridoindol-2-yl)butyl]tetrahydrobenzindole derivatives: new selective antagonists of the 5-hydroxytryptamine7 receptor.
AID282111Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents.
AID1571095Inhibition of CYP3A4 (unknown origin) assessed as residual activity at 10 uM using beetle D-luciferin as substrate by CYP450-Glo assay relative to control2018MedChemComm, Nov-01, Volume: 9, Issue:11
Search for a 5-CT alternative.
AID296887Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.
AID6666Binding affinity at rat 5-hydroxytryptamine 7 receptor.2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Characterization of the 5-HT(7) receptor. Determination of the pharmacophore for 5-HT(7) receptor agonism and CoMFA-based modeling of the agonist binding site.
AID4883Binding affinity for 5-hydroxytryptamine 1D receptor was determined1993Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13
(+/-) 3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: a conformationally restricted analogue of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor.
AID438555Binding affinity to 5HT1A receptor2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Physical binding pocket induction for affinity prediction.
AID1571097Inhibition of CYP2C9 (unknown origin) assessed as residual activity at 25 uM using beetle D-luciferin as substrate by CYP450-Glo assay relative to control2018MedChemComm, Nov-01, Volume: 9, Issue:11
Search for a 5-CT alternative.
AID5650Binding affinity against 5-hydroxytryptamine 2C receptor human cloned receptors in HEK 293 cells using [3H]mesulergine as radioligand2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
A novel ergot alkaloid as a 5-HT(1A) inhibitor produced by Dicyma sp.
AID63231Binding affinity against human Dopamine receptor D2 in CHO cells using [125I]iodosulpiride; Not determined2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
A novel ergot alkaloid as a 5-HT(1A) inhibitor produced by Dicyma sp.
AID282116Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum at 3 uM2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents.
AID3925Binding affinity against 5-hydroxytryptamine 1A human cloned receptors in HEK293 cells using [3H]8-OH-DPAT as radioligand2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
A novel ergot alkaloid as a 5-HT(1A) inhibitor produced by Dicyma sp.
AID6650Binding affinity to the rat 5-hydroxytryptamine 7 receptor2003Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4
Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones as 5-HT(7) receptor ligands.
AID3898Negative logarithm of concentration required to obtain 50% maximal stimulation of [35S]GTP gamma-S binding to human cloned 5-HT1A receptors of cell membranes from HeLa cells1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) 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.
AID1187938Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as cAMP accumulation at 12.5 uM incubated for 10 mins by fluorescence assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Novel N-biphenyl-2-ylmethyl 2-methoxyphenylpiperazinylalkanamides as 5-HT7R antagonists for the treatment of depression.
AID3891Maximum binding affinity was evaluated as ([35S]GTP binding on 5-hydroxytryptamine 1A serotonergic receptors.1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes.
AID282108Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents.
AID1571088Inhibition of recombinant human membrane bound Pgp assessed as basal ATP consumption at 100 uM after 40 mins by Pgp-Glo luminescence assay relative to control2018MedChemComm, Nov-01, Volume: 9, Issue:11
Search for a 5-CT alternative.
AID773788Displacement of [3H]-5-CT from 5-HT7 receptor in Sprague-Dawley rat hypothalamus after 120 mins2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
New serotonin 5-HT1A receptor agonists endowed with antinociceptive activity in vivo.
AID1571087Permeability of the compound by PAMPA2018MedChemComm, Nov-01, Volume: 9, Issue:11
Search for a 5-CT alternative.
AID6479Binding affinity towards human 5-hydroxytryptamine 5A receptor2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
AID4276Binding affinity against human 5-hydroxytryptamine 1B receptor cloned receptors in CHO cells2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
A novel ergot alkaloid as a 5-HT(1A) inhibitor produced by Dicyma sp.
AID391759Agonist activity at human cloned 5HT1A receptor expressed in HeLa cell membrane assessed as stimulation of [35S]GTPgammaS binding relative to 5-hydroxytryptamine2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents.
AID1571090Drug metabolism in rat liver microsomes measured after 120 mins in presence of NADPH generating system by UPLC analysis2018MedChemComm, Nov-01, Volume: 9, Issue:11
Search for a 5-CT alternative.
AID1595154Agonist activity at 5-HT7 receptor (unknown origin) expressed in N1E-115 cells assessed as intracellular cAMP response time by confocal laser scanning microscopy
AID4778Binding affinity for 5-hydroxytryptamine 1C receptor was determined1993Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13
(+/-) 3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: a conformationally restricted analogue of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor.
AID776869Displacement of [3H]-5-CT from human recombinant 5-HT7 receptor expressed in CHO-K1 cells after 120 mins2013European journal of medicinal chemistry, Nov, Volume: 69Development of 3,4-dihydroisoquinolin-1(2H)-one derivatives for the Positron Emission Tomography (PET) imaging of σ₂ receptors.
AID5089In vitro binding affinity to 5-hydroxytryptamine 2 receptor of rat cerebral cortex membranes using [3H]ketanserin as the radioligand2002Journal of medicinal chemistry, May-23, Volume: 45, Issue:11
2a-[4-(Tetrahydropyridoindol-2-yl)butyl]tetrahydrobenzindole derivatives: new selective antagonists of the 5-hydroxytryptamine7 receptor.
AID3894Agonist efficacy was evaluated as ([35S]GTP binding on 5-hydroxytryptamine 1A serotonergic receptors.1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes.
AID1346903Rat 5-HT2B receptor (5-Hydroxytryptamine receptors)1993Molecular pharmacology, Mar, Volume: 43, Issue:3
Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor.
AID624216Agonists at Human 5-Hydroxytryptamine receptor 5-HT2C2004Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.
AID624220Agonists at Mouse 5-Hydroxytryptamine receptor 5-HT1B1992Proceedings of the National Academy of Sciences of the United States of America, Apr-01, Volume: 89, Issue:7
Mouse 5HT1B serotonin receptor: cloning, functional expression, and localization in motor control centers.
AID1345068Human 5-HT5A receptor (5-Hydroxytryptamine receptors)1994FEBS letters, Dec-05, Volume: 355, Issue:3
Cloning and characterisation of the human 5-HT5A serotonin receptor.
AID1345291Human 5-HT7 receptor (5-Hydroxytryptamine receptors)2001Naunyn-Schmiedeberg's archives of pharmacology, Jun, Volume: 363, Issue:6
The cloned human 5-HT7 receptor splice variants: a comparative characterization of their pharmacology, function and distribution.
AID1346739Human 5-HT1F receptor (5-Hydroxytryptamine receptors)1993Proceedings of the National Academy of Sciences of the United States of America, Jan-15, Volume: 90, Issue:2
Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase.
AID624227Agonists at Rat 5-Hydroxytryptamine receptor 5-HT1F1993Proceedings of the National Academy of Sciences of the United States of America, Mar-15, Volume: 90, Issue:6
Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes.
AID1346603Human 5-ht1e receptor (5-Hydroxytryptamine receptors)1992Proceedings of the National Academy of Sciences of the United States of America, Jun-15, Volume: 89, Issue:12
Molecular cloning of a serotonin receptor from human brain (5HT1E): a fifth 5HT1-like subtype.
AID1346783Rat 5-HT1F receptor (5-Hydroxytryptamine receptors)1993Proceedings of the National Academy of Sciences of the United States of America, Mar-15, Volume: 90, Issue:6
Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes.
AID1346302Mouse 5-HT1B receptor (5-Hydroxytryptamine receptors)1992Proceedings of the National Academy of Sciences of the United States of America, Apr-01, Volume: 89, Issue:7
Mouse 5HT1B serotonin receptor: cloning, functional expression, and localization in motor control centers.
AID624212Agonists at Human 5-Hydroxytryptamine receptor 5-ht5a2001European journal of pharmacology, Apr-27, Volume: 418, Issue:3
Human 5-HT(5) receptors: the 5-HT(5A) receptor is functional but the 5-HT(5B) receptor was lost during mammalian evolution.
AID1345170Human 5-HT6 receptor (5-Hydroxytryptamine receptors)1996Journal of neurochemistry, Jan, Volume: 66, Issue:1
Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
AID624230Agonists at Human 5-Hydroxytryptamine receptor 5-ht1e1996Journal of neurochemistry, Nov, Volume: 67, Issue:5
Two amino acid differences in the sixth transmembrane domain are partially responsible for the pharmacological differences between the 5-HT1D beta and 5-HT1E 5-hydroxytryptamine receptors.
AID1346528Human 5-HT1D receptor (5-Hydroxytryptamine receptors)1991Molecular pharmacology, Aug, Volume: 40, Issue:2
Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.
AID1346867Human 5-HT2B receptor (5-Hydroxytryptamine receptors)2004Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)1997Naunyn-Schmiedeberg's archives of pharmacology, Jun, Volume: 355, Issue:6
Agonist activity of antimigraine drugs at recombinant human 5-HT1A receptors: potential implications for prophylactic and acute therapy.
AID624216Agonists at Human 5-Hydroxytryptamine receptor 5-HT2C2000Synapse (New York, N.Y.), Feb, Volume: 35, Issue:2
Agonist high and low affinity state ratios predict drug intrinsic activity and a revised ternary complex mechanism at serotonin 5-HT(2A) and 5-HT(2C) receptors.
AID1346528Human 5-HT1D receptor (5-Hydroxytryptamine receptors)1992Proceedings of the National Academy of Sciences of the United States of America, Apr-15, Volume: 89, Issue:8
Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
AID1346903Rat 5-HT2B receptor (5-Hydroxytryptamine receptors)1994Molecular pharmacology, Aug, Volume: 46, Issue:2
Molecular cloning, functional expression, and mRNA tissue distribution of the human 5-hydroxytryptamine2B receptor.
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)1998Naunyn-Schmiedeberg's archives of pharmacology, Mar, Volume: 357, Issue:3
Labelling of recombinant human and native rat serotonin 5-HT1A receptors by a novel, selective radioligand, [3H]-S 15535: definition of its binding profile using agonists, antagonists and inverse agonists.
AID624212Agonists at Human 5-Hydroxytryptamine receptor 5-ht5a1994FEBS letters, Dec-05, Volume: 355, Issue:3
Cloning and characterisation of the human 5-HT5A serotonin receptor.
AID624230Agonists at Human 5-Hydroxytryptamine receptor 5-ht1e2004European journal of pharmacology, Jan-26, Volume: 484, Issue:2-3
Molecular cloning and pharmacological characterization of the guinea pig 5-HT1E receptor.
AID1345061Mouse 5-HT5A receptor (5-Hydroxytryptamine receptors)1995FEBS letters, Dec-27, Volume: 377, Issue:3
Expression of functional mouse 5-HT5A serotonin receptor in the methylotrophic yeast Pichia pastoris: pharmacological characterization and localization.
AID624210Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A1992The Biochemical journal, Aug-01, Volume: 285 ( Pt 3)High-level stable expression of recombinant 5-HT1A 5-hydroxytryptamine receptors in Chinese hamster ovary cells.
AID1345154Rat 5-HT6 receptor (5-Hydroxytryptamine receptors)
AID1345068Human 5-HT5A receptor (5-Hydroxytryptamine receptors)2001European journal of pharmacology, Apr-27, Volume: 418, Issue:3
Human 5-HT(5) receptors: the 5-HT(5A) receptor is functional but the 5-HT(5B) receptor was lost during mammalian evolution.
AID1345154Rat 5-HT6 receptor (5-Hydroxytryptamine receptors)1998Journal of neurochemistry, Nov, Volume: 71, Issue:5
Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
AID1345061Mouse 5-HT5A receptor (5-Hydroxytryptamine receptors)2001European journal of pharmacology, Apr-27, Volume: 418, Issue:3
Human 5-HT(5) receptors: the 5-HT(5A) receptor is functional but the 5-HT(5B) receptor was lost during mammalian evolution.
AID624210Agonists 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.
AID1345235Rat 5-HT7 receptor (5-Hydroxytryptamine receptors)1993The Journal of biological chemistry, Aug-25, Volume: 268, Issue:24
Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
AID624219Agonists at Human 5-Hydroxytryptamine receptor 5-HT2B1994Molecular pharmacology, Aug, Volume: 46, Issue:2
Molecular cloning, functional expression, and mRNA tissue distribution of the human 5-hydroxytryptamine2B receptor.
AID624230Agonists at Human 5-Hydroxytryptamine receptor 5-ht1e1993Proceedings of the National Academy of Sciences of the United States of America, Jan-15, Volume: 90, Issue:2
Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase.
AID1345154Rat 5-HT6 receptor (5-Hydroxytryptamine receptors)1993Molecular pharmacology, Mar, Volume: 43, Issue:3
Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
AID1346893Human 5-HT2C receptor (5-Hydroxytryptamine receptors)2004Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.
AID1345291Human 5-HT7 receptor (5-Hydroxytryptamine receptors)1993The Journal of biological chemistry, Nov-05, Volume: 268, Issue:31
Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
AID1345235Rat 5-HT7 receptor (5-Hydroxytryptamine receptors)1993Proceedings of the National Academy of Sciences of the United States of America, Sep-15, Volume: 90, Issue:18
Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
AID624219Agonists at Human 5-Hydroxytryptamine receptor 5-HT2B2004Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.
AID1345215Mouse 5-HT7 receptor (5-Hydroxytryptamine receptors)1993Molecular pharmacology, Aug, Volume: 44, Issue:2
Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
AID624210Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A1997Naunyn-Schmiedeberg's archives of pharmacology, Jun, Volume: 355, Issue:6
Agonist activity of antimigraine drugs at recombinant human 5-HT1A receptors: potential implications for prophylactic and acute therapy.
AID624210Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A1998Naunyn-Schmiedeberg's archives of pharmacology, Mar, Volume: 357, Issue:3
Labelling of recombinant human and native rat serotonin 5-HT1A receptors by a novel, selective radioligand, [3H]-S 15535: definition of its binding profile using agonists, antagonists and inverse agonists.
AID1346528Human 5-HT1D receptor (5-Hydroxytryptamine receptors)1996Molecular pharmacology, Dec, Volume: 50, Issue:6
Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamin
AID1345061Mouse 5-HT5A receptor (5-Hydroxytryptamine receptors)1993Molecular pharmacology, Mar, Volume: 43, Issue:3
Mouse 5-hydroxytryptamine5A and 5-hydroxytryptamine5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization.
AID1345291Human 5-HT7 receptor (5-Hydroxytryptamine receptors)1997British journal of pharmacology, Sep, Volume: 122, Issue:1
Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)1992The Biochemical journal, Aug-01, Volume: 285 ( Pt 3)High-level stable expression of recombinant 5-HT1A 5-hydroxytryptamine receptors in Chinese hamster ovary cells.
AID1346264Human 5-HT1B receptor (5-Hydroxytryptamine receptors)1992Proceedings of the National Academy of Sciences of the United States of America, Apr-15, Volume: 89, Issue:8
Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
AID624233Agonists at Human 5-Hydroxytryptamine receptor 5-HT1F
AID624240Agonists at Rat 5-Hydroxytryptamine receptor 5-HT2B1993Molecular pharmacology, Mar, Volume: 43, Issue:3
Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor.
AID624233Agonists at Human 5-Hydroxytryptamine receptor 5-HT1F1993Proceedings of the National Academy of Sciences of the United States of America, Jan-15, Volume: 90, Issue:2
Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase.
AID1346264Human 5-HT1B receptor (5-Hydroxytryptamine receptors)1996Journal of neurochemistry, Nov, Volume: 67, Issue:5
Two amino acid differences in the sixth transmembrane domain are partially responsible for the pharmacological differences between the 5-HT1D beta and 5-HT1E 5-hydroxytryptamine receptors.
AID1345069Rat 5-HT5A receptor (5-Hydroxytryptamine receptors)1993Proceedings of the National Academy of Sciences of the United States of America, Apr-15, Volume: 90, Issue:8
Two members of a distinct subfamily of 5-hydroxytryptamine receptors differentially expressed in rat brain.
AID1346867Human 5-HT2B receptor (5-Hydroxytryptamine receptors)1994Molecular pharmacology, Aug, Volume: 46, Issue:2
Molecular cloning, functional expression, and mRNA tissue distribution of the human 5-hydroxytryptamine2B receptor.
AID1346893Human 5-HT2C receptor (5-Hydroxytryptamine receptors)2000Synapse (New York, N.Y.), Feb, Volume: 35, Issue:2
Agonist high and low affinity state ratios predict drug intrinsic activity and a revised ternary complex mechanism at serotonin 5-HT(2A) and 5-HT(2C) receptors.
AID624240Agonists at Rat 5-Hydroxytryptamine receptor 5-HT2B1994Molecular pharmacology, Aug, Volume: 46, Issue:2
Molecular cloning, functional expression, and mRNA tissue distribution of the human 5-hydroxytryptamine2B receptor.
AID624235Agonists at Human 5-Hydroxytryptamine receptor 5-HT2A2004Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.
AID1346603Human 5-ht1e receptor (5-Hydroxytryptamine receptors)2004European journal of pharmacology, Jan-26, Volume: 484, Issue:2-3
Molecular cloning and pharmacological characterization of the guinea pig 5-HT1E receptor.
AID1346603Human 5-ht1e receptor (5-Hydroxytryptamine receptors)1993Proceedings of the National Academy of Sciences of the United States of America, Jan-15, Volume: 90, Issue:2
Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase.
AID1345291Human 5-HT7 receptor (5-Hydroxytryptamine receptors)1998British journal of pharmacology, Jul, Volume: 124, Issue:6
Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719.
AID1346739Human 5-HT1F receptor (5-Hydroxytryptamine receptors)
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.
AID1346603Human 5-ht1e receptor (5-Hydroxytryptamine receptors)1996Journal of neurochemistry, Nov, Volume: 67, Issue:5
Two amino acid differences in the sixth transmembrane domain are partially responsible for the pharmacological differences between the 5-HT1D beta and 5-HT1E 5-hydroxytryptamine receptors.
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)2004Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.
AID624230Agonists at Human 5-Hydroxytryptamine receptor 5-ht1e1992Proceedings of the National Academy of Sciences of the United States of America, Jun-15, Volume: 89, Issue:12
Molecular cloning of a serotonin receptor from human brain (5HT1E): a fifth 5HT1-like subtype.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1798075Radioligand Labeled Binding Assay from Article 10.1021/jm070487n: \\Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.\\2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (383)

TimeframeStudies, This Drug (%)All Drugs %
pre-199036 (9.40)18.7374
1990's203 (53.00)18.2507
2000's101 (26.37)29.6817
2010's35 (9.14)24.3611
2020's8 (2.09)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.31

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 Index18.31 (24.57)
Research Supply Index5.98 (2.92)
Research Growth Index4.99 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.31)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (0.26%)5.53%
Reviews3 (0.77%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other388 (98.98%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]