Page last updated: 2024-12-04

2-methyl-5-ht

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

Description

2-methyl-5-HT: M-receptor agonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID1574
CHEMBL ID266591
CHEBI ID31085
SCHEMBL ID399028
MeSH IDM0133298

Synonyms (53)

Synonym
gtpl218
2-me-5-ht
1h-indol-5-ol, 3-(2-aminoethyl)-2-methyl-
NCGC00024652-01
tocris-0558
NCGC00015628-01
lopac-m-109
BPBIO1_001361
LOPAC0_000813
PDSP1_001520
PDSP2_001504
2-methyl-5-hydroxytryptamine
2-me 5-ht
2-me-5ht
NCGC00024652-03
BIOMOL-NT_000098
NCGC00024652-02
CHEBI:31085 ,
2-methyl-5-ht
3-(2-aminoethyl)-2-methyl-1h-indol-5-ol
2-methylserotonin
78263-90-8
NCGC00015628-05
L000061
CHEMBL266591 ,
5-ht,2-me
bdbm50014406
CCG-204897
NCGC00015628-02
NCGC00015628-03
NCGC00015628-04
d77z9hjt2u ,
unii-d77z9hjt2u
2-methylserotonin.hcl
AKOS016362704
DTXSID80228927
SCHEMBL399028
AC-30467
Y11118
NS-01775
3-(2-amino-ethyl)-2-methyl-1h-indol-5-ol
Q4596904
mfcd00152134
2-methyl-5-hydroxytryptamine; 2-methylserotonin;2-me-5-ht
BRD-K64137799-003-01-7
SDCCGSBI-0050790.P002
SB38745
CS-0015425
HY-19358
EN300-325733
PD048535
3-(2-azanylethyl)-2-methyl-1h-indol-5-ol
indol-5-ol, 3-(2-aminoethyl)-2-methyl-

Research Excerpts

Dosage Studied

GR38032F (10 micrograms/kg) caused a significant rightward shift in the 2-methyl-5-HT dose-response curve. Treatment with either ketanserin or bunazosin had no antagonistic effect.

ExcerptRelevanceReference
" The 5-HT2 receptor antagonist ketanserin (1 microM) caused a clear rightward shift of the dose-response curve to 5-HT on the guinea-pig ganglion, but not on the mouse or rat ganglion."( Evidence that the 5-HT3 receptors of the rat, mouse and guinea-pig superior cervical ganglion may be different.
Cheshire, SH; Gilbert, MJ; Newberry, NR, 1991
)
0.28
" In the presence of 100 microM 2-Me5-HT, the upper part of the 5-HT dose-response curve was shifted to the right but reached the same maximum value as in the absence of 2-Me5-HT."( The agonist properties of m-chlorophenylbiguanide and 2-methyl-5-hydroxytryptamine on 5-HT3 receptors in N1E-115 neuroblastoma cells.
Lummis, SC; Martin, IL; Sepúlveda, MI, 1991
)
0.28
" GR38032F (10 micrograms/kg) caused a significant rightward shift in the 2-methyl-5-HT dose-response curve."( Effect of 5-hydroxytryptamine on external carotid nerve activity and its blockade by GR38032F in anesthetized rats.
Abe, M; Ikeda, T; Saito, H; Togashi, H; Yoshioka, M, 1991
)
0.51
" On the other hand, 2-methyl-5-HT produced only a vasoconstriction, and the dose-response curve was shifted to the right in parallel by treatment with either ketanserin or bunazosin, although methysergide and granisetron had no antagonistic effect."( 2-Methyl-5-HT-induced vasoconstrictions mediated via alpha 1-adrenoceptors in rabbit common carotid arteries.
Chiba, S; Fujiwara, T, 1994
)
2.05
" The NK1 antagonist (+/-)-CP96345 was found to cause, at a maximally tolerated dose of 9 mumol/kg, an approximate 10-fold rightward shift of the dose-response curves for selective NK1 agonists substance P (SP), [Sar9,Met(O2)11]SP and Ac-[Arg6,Sar9,Met(O2)11]SP6-11 without altering responses to selective NK2 agonists neurokinin A (NKA), [Nle10]NKA4-10 or [beta-Ala8]NKA4-10."( Differential blockade by tachykinin NK1 and NK2 receptor antagonists of bronchoconstriction induced by direct-acting agonists and the indirect-acting mimetics capsaicin, serotonin and 2-methyl-serotonin in the anesthetized guinea pig.
Buckner, CK; Campbell, J; Dea, D; Krell, RD; Lengel, D; Liberati, N; Miller, S; Shenvi, A; Stinson-Fisher, C, 1993
)
0.29
") dosing to rats."( Pharmacological characterization of FK1052, a dihydropyridoindole derivative, as a new serotonin 3 and 4 dual receptor antagonist.
Kadowaki, M; Kohsaka, M; Mori, J; Nagakura, Y; Tokoro, K; Tomoi, M, 1993
)
0.29
" Moreover, increasing doses of carbidopa significantly shifted the inhibitory dose-response effect of delta-9-THC in protecting shrews from 5-HTP-induced emesis to the left."( Central and peripheral mechanisms contribute to the antiemetic actions of delta-9-tetrahydrocannabinol against 5-hydroxytryptophan-induced emesis.
Darmani, NA; Johnson, JC, 2004
)
0.32
" The antiemetic dose-response curves of tropisetron against both emetogens were U-shaped probably because larger doses of this antagonist behave as a partial agonist."( Synergistic antiemetic interactions between serotonergic 5-HT3 and tachykininergic NK1-receptor antagonists in the least shrew (Cryptotis parva).
Alkam, T; Amos, B; Chebolu, S; Darmani, NA, 2011
)
0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
serotonergic agonistAn agent that has an affinity for serotonin receptors and is able to mimic the effects of serotonin by stimulating the physiologic activity at the cell receptors. Serotonin agonists are used as antidepressants, anxiolytics, and in the treatment of migraine disorders.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (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 (46)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency35.48130.004023.8416100.0000AID485290
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency11.19360.140911.194039.8107AID2451
Chain A, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID893
phosphopantetheinyl transferaseBacillus subtilisPotency56.23410.141337.9142100.0000AID1490
GLS proteinHomo sapiens (human)Potency1.58490.35487.935539.8107AID624146
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency37.68580.035520.977089.1251AID504332
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency29.88160.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency7.94330.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency39.81070.00636.904339.8107AID883
chromobox protein homolog 1Homo sapiens (human)Potency50.11870.006026.168889.1251AID488953
mitogen-activated protein kinase 1Homo sapiens (human)Potency0.19950.039816.784239.8107AID995
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency15.84890.031610.279239.8107AID884; AID885
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency39.81070.00638.235039.8107AID883
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
[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 2CRattus norvegicus (Norway rat)Ki5.32500.00020.667710.0000AID4758; AID5248
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki10.00000.00010.601710.0000AID5248
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki1.85590.00010.739610.0000AID4043; AID4411
5-hydroxytryptamine receptor 3AMus musculus (house mouse)Ki1.43000.00130.23781.4300AID6008
5-hydroxytryptamine receptor 1DHomo sapiens (human)Ki1.22000.00010.808710.0000AID4539
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.52000.00031.29679.2440AID4697
5-hydroxytryptamine receptor 1EHomo sapiens (human)Ki10.00000.09304.770110.0000AID4950
5-hydroxytryptamine receptor 5AMus musculus (house mouse)Ki10.00000.00203.98248.7000AID6492
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki10.00000.00020.590910.0000AID5248
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki1.25800.00030.380610.0000AID6678
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)IC50 (µMol)0.77900.00021.13514.6000AID6069
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Ki0.87780.00020.484110.0000AID6041; AID6297
5-hydroxytryptamine receptor 3AHomo sapiens (human)Ki1.20000.00000.74119.9000AID6365
5-hydroxytryptamine receptor 5AHomo sapiens (human)Ki10.00000.00080.94335.1600AID6479
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.16400.00020.522910.0000AID6513; AID6518; AID6575
5-hydroxytryptamine receptor 3BMus musculus (house mouse)Ki1.43000.00130.26351.4300AID6008
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)IC50 (µMol)0.77900.00041.17424.6000AID6069
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Ki0.87780.00020.502310.0000AID6041; AID6297
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (25)

Processvia Protein(s)Taxonomy
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1DHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 1DHomo sapiens (human)
regulation of locomotion5-hydroxytryptamine receptor 1DHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 1DHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1DHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1DHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1DHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1DHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1EHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1EHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1EHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1EHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1EHomo 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)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3AHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3AHomo 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 (11)

Processvia Protein(s)Taxonomy
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1DHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1DHomo sapiens (human)
G protein-coupled receptor activity5-hydroxytryptamine receptor 1EHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1EHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1EHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1EHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1EHomo 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)
protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3AHomo 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 (12)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membrane5-hydroxytryptamine receptor 1DHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1DHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1DHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1DHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1EHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1EHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1EHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1EHomo 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 3AHomo sapiens (human)
cleavage furrow5-hydroxytryptamine receptor 3AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3AHomo 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)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (67)

Assay IDTitleYearJournalArticle
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
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.
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.
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.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
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.
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.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
AID4043Binding affinity was determined against 5-hydroxytryptamine 1A receptor was determined in male Sprague-Dawley rat brain.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
5-HT1 and 5-HT2 binding profiles of the serotonergic agents alpha-methylserotonin and 2-methylserotonin.
AID6279Compound was evaluated for the displacement of [3H]Q-ICS-205-930 from 5-HT3 recognition sites in rat brain membranes1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Novel 5-HT3 antagonists: indol-3-ylspiro(azabicycloalkane-3,5'(4'H)-oxazoles).
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).
AID185248Percent inhibition of serotonin-induced B-J reflex (Bezold-Jarisch reflex)in the right femoral vein of rat at a dose of 10 ug/kg1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists.
AID1325190Antibacterial activity against Bacillus subtilis 168 after 16 to 18 hrs by micro-dilution method2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
5-Alkyloxytryptamines are membrane-targeting, broad-spectrum antibiotics.
AID375333Agonist activity at 5HT3 receptor in spontaneously beating guinea pig right atrium assessed as positive chronotropic potency2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships.
AID5248Binding affinity was determined against 5-hydroxytryptamine 2 receptor from male Sprague-Dawley rat brain.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
5-HT1 and 5-HT2 binding profiles of the serotonergic agents alpha-methylserotonin and 2-methylserotonin.
AID6297The compound was tested for the binding affinity against 5-hydroxytryptamine 3 receptor using [3H]zacopride as radioligand.1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Pyrroloquinoxaline derivatives as high-affinity and selective 5-HT(3) receptor agonists: synthesis, further structure-activity relationships, and biological studies.
AID5937Compound was evaluated for the displacement of [3H]-Q-ICS 205-930 binding to 5-hydroxytryptamine 3 receptor in rat brain membranes1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Novel 5-HT3 antagonists. Indole oxadiazoles.
AID6329Intrinsic activity towards CNS 5-hydroxytryptamine 3 receptor was determined; A: agonist2002Bioorganic & medicinal chemistry letters, Oct-07, Volume: 12, Issue:19
Electrostatic potential surfaces of 5-HT(3)R agonists suggest accessory cation-pi site adjacent to agonist binding domain.
AID6518Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.
AID1325188Antibacterial activity against Escherichia coli BW25113 after 16 to 18 hrs by micro-dilution method2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
5-Alkyloxytryptamines are membrane-targeting, broad-spectrum antibiotics.
AID4758Binding affinity was determined against 5-hydroxytryptamine 1C receptor was determined in male Sprague-Dawley rat brain.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
5-HT1 and 5-HT2 binding profiles of the serotonergic agents alpha-methylserotonin and 2-methylserotonin.
AID6324Intrinsic activity towards 5-hydroxytryptamine 3 receptor was determined by Benzold-Jarisch reflex (peripheral assay); A: agonist2002Bioorganic & medicinal chemistry letters, Oct-07, Volume: 12, Issue:19
Electrostatic potential surfaces of 5-HT(3)R agonists suggest accessory cation-pi site adjacent to agonist binding domain.
AID6575Binding affinity towards 5-hydroxytryptamine 6 receptor2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
AID1325197Antibacterial activity against Acinetobacter baumannii after 16 to 18 hrs by micro-dilution method2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
5-Alkyloxytryptamines are membrane-targeting, broad-spectrum antibiotics.
AID6492Binding affinity towards mouse 5-hydroxytryptamine 5A 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).
AID375330Agonist activity at 5HT3 receptor in voltage-stimulated guinea pig left atrium assessed as positive inotropic potency2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships.
AID6008The binding affinity was measured for 5-hydroxytryptamine 3 receptor on NG 108-15 cell line of mouse neuroblastoma-glioma cells in presence of [3H]5 radioligand (in vitro)1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
Synthesis, in vitro binding profile, and central nervous system penetrability of the highly potent 5-HT3 receptor antagonist [3H]-4-(2-methoxyphenyl)-2-[4(5)-methyl-5(4)-imidazolylmethyl]thiazole.
AID4539Binding affinity was determined against 5-hydroxytryptamine 1D receptor in bovine caudate homogenate1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
5-HT1 and 5-HT2 binding profiles of the serotonergic agents alpha-methylserotonin and 2-methylserotonin.
AID4697Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
5-HT1 and 5-HT2 binding profiles of the serotonergic agents alpha-methylserotonin and 2-methylserotonin.
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).
AID189515Ability of compounds to relax oesophagus expressed as equipotent concentration ratio (ECR) where ECR = IC40 test agonist / IC40 5-HT1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Synthesis of 2-piperazinylbenzothiazole and 2-piperazinylbenzoxazole derivatives with 5-HT3 antagonist and 5-HT4 agonist properties.
AID4950Binding affinity was determined against 5-hydroxytryptamine 1E receptor in human cortical homogenate1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
5-HT1 and 5-HT2 binding profiles of the serotonergic agents alpha-methylserotonin and 2-methylserotonin.
AID191058Percent response to 100 ug/kg serotonin was determined as blockade of serotonin-induced bradycardia in anesthetized rat1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists.
AID185252Percent inhibition of serotonin-induced B-J reflex (Bezold-Jarisch reflex)in the right femoral vein of rat at a dose of 50 ug/kg1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists.
AID1325200Antibacterial activity against Staphylococcus aureus after 16 to 18 hrs by micro-dilution method2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
5-Alkyloxytryptamines are membrane-targeting, broad-spectrum antibiotics.
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.
AID6041In vitro displacement of [3H]ICS-205-930 from 5-hydroxytryptamine 3 receptor in cultured NG-108-15 rat glioma cells1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists.
AID15661The compound was evaluated for the value in rat isolated esophageal tunica muscularis mucose1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Synthesis of 2-piperazinylbenzothiazole and 2-piperazinylbenzoxazole derivatives with 5-HT3 antagonist and 5-HT4 agonist properties.
AID1325189Antibacterial activity against tolC-deficient Escherichia coli BW25113 after 16 to 18 hrs by micro-dilution method2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
5-Alkyloxytryptamines are membrane-targeting, broad-spectrum antibiotics.
AID6513Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo 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).
AID186653The compound was evaluated for the intrinsic activity in rat isolated esophageal tunica muscularis mucose1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Synthesis of 2-piperazinylbenzothiazole and 2-piperazinylbenzoxazole derivatives with 5-HT3 antagonist and 5-HT4 agonist properties.
AID375335Intrinsic activity at 5HT3 receptor in spontaneously beating guinea pig right atrium assessed as positive chronotropic potency relative to serotonin2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships.
AID375332Intrinsic activity at 5HT3 receptor in voltage-stimulated guinea pig left atrium assessed as positive inotropic potency relative to serotonin2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships.
AID6365Compound was evaluated for its binding affinity towards 5-hydroxytryptamine 3 receptor2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.
AID6069Inhibition of [3H]BRL-43694 binding to 5-hydroxytryptamine 3 receptor of rat cortical homogenate.1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.
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.
AID1345154Rat 5-HT6 receptor (5-Hydroxytryptamine receptors)
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.
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.
AID1346903Rat 5-HT2B receptor (5-Hydroxytryptamine receptors)1993Molecular 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.
AID624240Agonists at Rat 5-Hydroxytryptamine receptor 5-HT2B1993Molecular pharmacology, Mar, Volume: 43, Issue:3
Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor.
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.
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
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.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (214)

TimeframeStudies, This Drug (%)All Drugs %
pre-199012 (5.61)18.7374
1990's142 (66.36)18.2507
2000's43 (20.09)29.6817
2010's12 (5.61)24.3611
2020's5 (2.34)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.00

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

MetricThis Compound (vs All)
Research Demand Index20.00 (24.57)
Research Supply Index5.39 (2.92)
Research Growth Index5.50 (4.65)
Search Engine Demand Index19.78 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (20.00)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (0.46%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other218 (99.54%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]