Page last updated: 2024-12-06

mesulergine

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

Description

Mesulergine is a serotonin antagonist that was synthesized in the 1950s. It has been investigated for its potential therapeutic effects in a variety of conditions, including migraine headaches, anxiety, and depression. Its pharmacological profile is characterized by its affinity for various serotonin receptors, particularly 5-HT2A and 5-HT2C receptors. Research on mesulergine has explored its anti-migraine properties, its effects on anxiety and mood, and its potential use as a treatment for other conditions. However, its clinical development has been limited due to its potential side effects. Studies have focused on understanding its mechanism of action, its interaction with other drugs, and its overall safety profile.'

mesulergine: RN given refers to parent cpd; CU 32-085 is synonymous to mono-HCl; metabolized into dopaminergic agonists; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

mesulergine : A member of the class of ergot alkaloids that is known to act on serotonin and dopamine receptors. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID68848
CHEMBL ID_10959
CHEMBL ID12314
CHEBI ID73378
SCHEMBL ID292175
MeSH IDM0099260

Synonyms (46)

Synonym
AB01275438-01
BRD-K91336023-001-01-4
(6ar,9s,10ar)-9-(dimethylsulfamoylamino)-4,7-dimethyl-6,6a,8,9,10,10a-hexahydroindolo[4,3-fg]quinoline
gtpl206
BPBIO1_001398
NCGC00163168-01
mesulergine [inn]
n'-(1,6-dimethylergolin-8alpha-yl)-n,n-dimethylsulfamide
mesulerginum [inn-latin]
mesulergina [inn-spanish]
mesulergine
3-(1,6-dimethyl-8alpha-ergolinyl)-1,1-dimethylsulfamid
cq 32085
BIOMOL-NT_000077
HMS2089G12
chembl_10959
2n-[4,7-dimethyl-(6ar,9s,10ar)-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinolin-9-yl]-2-dimethylaminosulfonamide
1h-imidazo[4,5-c]pyridine derivative
n''-4,7-dimethyl-4,6,6a,7,8,9,10,10a-octahydro-indolo[4,3-fg]quinolin-9-yl)-n''-,n''-dimethyl-sulphonediamine
4,7-dimethyl-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinolin-9-amine-sulfonamide
4,7-dimethyl-(6ar,9s,10ar)-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinolin-9-amino-n,n-dimethyl sulfonamide
chembl12314 ,
bdbm50024204
9-n,n-dimethylsulfamide-4,7-dimethyl-4,6,6a,7,8,9,10,10a-octahydro-indolo[4,3-fg]quinoline
NCGC00163168-02
tox21_112023
dtxcid1026324
cas-64795-35-3
dtxsid3046324 ,
mesulergina
unii-sml95fk06i
sml95fk06i ,
mesulerginum
64795-35-3
n'-[(8alpha)-1,6-dimethylergolin-8-yl]-n,n-dimethylsulfuric diamide
chebi:73378 ,
SCHEMBL292175
tox21_112023_1
NCGC00163168-03
n'-(1,6-dimethylergolin-8.alpha.-yl)-n,n-dimethylsulfamide
mesulergine [who-dd]
{[(2r,4s,7r)-6,11-dimethyl-6,11-diazatetracyclo[7.6.1.0{2,7}.0{12,16}]hexadeca-1(16),9,12,14-tetraen-4-yl]sulfamoyl}dimethylamine
SR-05000001430-1
sr-05000001430
Q6822173
sulfamide, n'-[(8.alpha.)-1,6-dimethylergolin-8-yl]-n,n-dimethyl-

Research Excerpts

Overview

Mesulergine (Cu32-085) is an active semisynthetic ergot alkaloid with unusual biphasic antagonistic-agonistic effect on dopamine turnover.

ExcerptReferenceRelevance
"Mesulergine (Cu32-085) is an active semisynthetic ergot alkaloid with unusual biphasic antagonistic-agonistic effect on dopamine (DA) turnover in the rat striatum. "( The effect of mesulergine on prolactin secretion and anterior pituitary cells morphology in diethylstilboestrol-treated female Wistar rats.
Pisarek, H; Stepien, H, 1992
)
2.09

Actions

ExcerptReferenceRelevance
"Mesulergine displays approximately 50-fold higher affinity for the rat 5-HT2 receptor than for the human receptor. "( Site-directed mutagenesis of a single residue changes the binding properties of the serotonin 5-HT2 receptor from a human to a rat pharmacology.
Adham, N; Branchek, TA; Hartig, PR; Kao, HT; Olsen, MA; Weinshank, RL, 1992
)
1.73

Treatment

ExcerptReferenceRelevance
"Pretreatment with mesulergine (200 microg/kg) did not change the inhibition of DA release induced by apomorphine (100 microg/kg), whereas it prevented the reduction of DOPAC outflow induced by apomorphine (100 microg/kg)."( Selective blockade of serotonin2C/2B receptors enhances dopamine release in the rat nucleus accumbens.
Di Giovanni, G; Di Mascio, M; Di Matteo, V; Esposito, E, 1998
)
0.62

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

A dose-response relationship was evident, however, between mesulergine and PRL secretion during both the 8 A. and 8 B trials. The patients developed symptoms from nine months to four years after starting treatment with bromocriptine that varied in dosage from 22 to 50 mg daily.

ExcerptRelevanceReference
" The patients developed symptoms from nine months to four years after starting treatment with bromocriptine that varied in dosage from 22 to 50 mg daily, while the patient receiving mesulergine was taking 6 mg daily."( Pleuropulmonary disease during bromocriptine treatment of Parkinson's disease.
Churg, A; Fleetham, JA; McElvaney, NG; Wilcox, PG, 1988
)
0.47
" Participants were divided into two groups, and over a nine-week period, mesulergine dosage was increased to a maximum of either 10 or 20 mg daily."( Mesulergine (CU32-085) in the treatment of Parkinson's disease.
Glaeske, C; Pfeiffer, RF; Wilken, K, 1985
)
1.94
" The daily dosage was increased slowly to 7 mg over 9 weeks, held constant for 8 weeks, then replaced by placebo for 4 weeks."( Initial treatment of parkinsonism with 8-alpha-amino-ergoline.
Hietanen, M; Huttunen, J; Teräväinen, H, 1985
)
0.27
" The effects of CU 32-085 and bromocriptine on dose-response curves to sympathomimetic agents (adrenaline, noradrenaline, methoxamine and clonidine), intravenously administered, were also studied."( Hypotensive action and alpha-adrenolytic properties of a new dopaminergic agonist, CU 32-085, in the rat.
Esplugues, J; Morales-Olivas, FJ; Palop, V; Rubio, E, 1984
)
0.27
" To test the hypothesis that the 5-HT1C properties of these drugs are involved instead, dose-response and time-course studies of 5-HT1C and 5-HT2 receptors were performed using several different radioligands in rat brain after making neonatal 5,7-DHT lesions by intraperitoneal injection."( High and low affinity 5-HT2 and 5-HT1C binding sites: responses to neonatal 5,7-DHT lesions in rat brain.
Gregory, CM; Pranzatelli, MR, 1993
)
0.29
" In acute dose-response studies, injection of a single dose of DOI did not result in a significant change in any receptor parameters."( Novel regulation of 5-HT1C receptors: down-regulation induced both by 5-HT1C/2 receptor agonists and antagonists.
Murthy, JN; Pranzatelli, MR; Tailor, PT, 1993
)
0.29
" Drugs that produced a significant decrease in myoclonus compared with the control were studied in a dose-response study with six doses across a range from the original dose studied to 10% of that dose."( Animal model of posthypoxic myoclonus: effects of serotonergic antagonists.
Carvey, PM; Goetz, CG; Leurgans, S; Ling, ZD; Pappert, EJ; Raman, R; Vu, TQ, 1999
)
0.3
" Dose-response studies showed that all doses of methiothepin mesylate and the three highest doses of mesulergine hydrochloride inhibited myoclonus effectively."( Animal model of posthypoxic myoclonus: effects of serotonergic antagonists.
Carvey, PM; Goetz, CG; Leurgans, S; Ling, ZD; Pappert, EJ; Raman, R; Vu, TQ, 1999
)
0.52
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
antiparkinson drugA drug used in the treatment of Parkinson's disease.
dopamine agonistA drug that binds to and activates dopamine receptors.
serotonergic antagonistDrugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or serotonergic agonists.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
ergot alkaloid
sulfamidesCompounds where two amino groups are bound to an SO2 unit.
[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 (31)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
acetylcholinesteraseHomo sapiens (human)Potency9.77170.002541.796015,848.9004AID1347398
RAR-related orphan receptor gammaMus musculus (house mouse)Potency0.18830.006038.004119,952.5996AID1159521
GLS proteinHomo sapiens (human)Potency22.38720.35487.935539.8107AID624170
TDP1 proteinHomo sapiens (human)Potency29.85540.000811.382244.6684AID686978
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency35.48130.011212.4002100.0000AID1030
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency18.02120.001022.650876.6163AID1224838; AID1224839
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency12.58930.01237.983543.2770AID1346984
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency23.71010.003041.611522,387.1992AID1159552
retinoid X nuclear receptor alphaHomo sapiens (human)Potency23.91450.000817.505159.3239AID1159527
pregnane X nuclear receptorHomo sapiens (human)Potency25.94690.005428.02631,258.9301AID1346982; AID1346985
cytochrome P450 2D6Homo sapiens (human)Potency2.18760.00108.379861.1304AID1645840
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency31.62280.035520.977089.1251AID504332
aryl hydrocarbon receptorHomo sapiens (human)Potency13.33320.000723.06741,258.9301AID743085
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency10.00000.10009.191631.6228AID1346983
[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)Ki0.00220.00020.667710.0000AID1278109; AID1297677; AID1365270; AID442989; AID5270; AID5273; AID5712; AID5743; AID5757; AID599611; AID633918
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.00300.00010.601710.0000AID5270; AID5273
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.00190.00010.949010.0000AID1278109; AID442989
Endothelin receptor type BRattus norvegicus (Norway rat)Ki0.00790.00630.05750.3710AID6685
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.00190.00000.575110.0000AID1278109; AID442989
Endothelin receptor type BHomo sapiens (human)Ki0.00790.00010.05430.3710AID6670; AID6685
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC50 (µMol)0.00190.00011.03029.0000AID255315
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.00140.00010.954910.0000AID1154617; AID4747; AID5855
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki13.00000.00031.29679.2440AID4699
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.00300.00020.590910.0000AID5270; AID5273
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.00790.00000.14803.1800AID6670
5-hydroxytryptamine receptor 7Homo sapiens (human)IC50 (µMol)0.20500.00050.45464.7640AID1186029; AID415374
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki0.00790.00030.380610.0000AID6685
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)IC50 (µMol)0.00210.00021.13514.6000AID6072
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC50 (µMol)0.00520.00011.18738.9125AID1597292
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.00280.00030.769310.0000AID1597292
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.00190.00000.965010.0000AID1278109; AID442989
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.77610.00020.522910.0000AID1154620
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)IC50 (µMol)0.00210.00041.17424.6000AID6072
[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)Kd0.15850.00010.95285.0119AID438555
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 7Homo sapiens (human)Kb0.01100.00010.00200.0110AID1186030
5-hydroxytryptamine receptor 7Homo sapiens (human)Kbapp0.01600.01600.01600.0160AID1141733
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (104)

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)
negative regulation of transcription by RNA polymerase IIEndothelin receptor type BHomo sapiens (human)
neural crest cell migrationEndothelin receptor type BHomo sapiens (human)
positive regulation of protein phosphorylationEndothelin receptor type BHomo sapiens (human)
renin secretion into blood streamEndothelin receptor type BHomo sapiens (human)
regulation of heart rateEndothelin receptor type BHomo sapiens (human)
regulation of pHEndothelin receptor type BHomo sapiens (human)
cell surface receptor signaling pathwayEndothelin receptor type BHomo sapiens (human)
negative regulation of adenylate cyclase activityEndothelin receptor type BHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayEndothelin receptor type BHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationEndothelin receptor type BHomo sapiens (human)
nervous system developmentEndothelin receptor type BHomo sapiens (human)
peripheral nervous system developmentEndothelin receptor type BHomo sapiens (human)
posterior midgut developmentEndothelin receptor type BHomo sapiens (human)
positive regulation of cell population proliferationEndothelin receptor type BHomo sapiens (human)
gene expressionEndothelin receptor type BHomo sapiens (human)
negative regulation of neuron maturationEndothelin receptor type BHomo sapiens (human)
response to organic cyclic compoundEndothelin receptor type BHomo sapiens (human)
vein smooth muscle contractionEndothelin receptor type BHomo sapiens (human)
calcium-mediated signalingEndothelin receptor type BHomo sapiens (human)
cGMP-mediated signalingEndothelin receptor type BHomo sapiens (human)
heparin metabolic processEndothelin receptor type BHomo sapiens (human)
melanocyte differentiationEndothelin receptor type BHomo sapiens (human)
regulation of fever generationEndothelin receptor type BHomo sapiens (human)
aldosterone metabolic processEndothelin receptor type BHomo sapiens (human)
enteric smooth muscle cell differentiationEndothelin receptor type BHomo sapiens (human)
positive regulation of urine volumeEndothelin receptor type BHomo sapiens (human)
renal sodium excretionEndothelin receptor type BHomo sapiens (human)
epithelial fluid transportEndothelin receptor type BHomo sapiens (human)
vasoconstrictionEndothelin receptor type BHomo sapiens (human)
vasodilationEndothelin receptor type BHomo sapiens (human)
negative regulation of apoptotic processEndothelin receptor type BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionEndothelin receptor type BHomo sapiens (human)
macrophage chemotaxisEndothelin receptor type BHomo sapiens (human)
response to painEndothelin receptor type BHomo sapiens (human)
enteric nervous system developmentEndothelin receptor type BHomo sapiens (human)
regulation of epithelial cell proliferationEndothelin receptor type BHomo sapiens (human)
negative regulation of protein metabolic processEndothelin receptor type BHomo sapiens (human)
canonical Wnt signaling pathwayEndothelin receptor type BHomo sapiens (human)
positive regulation of penile erectionEndothelin receptor type BHomo sapiens (human)
establishment of endothelial barrierEndothelin receptor type BHomo sapiens (human)
renal sodium ion absorptionEndothelin receptor type BHomo sapiens (human)
calcium ion transmembrane transportEndothelin receptor type BHomo sapiens (human)
cellular response to lipopolysaccharideEndothelin receptor type BHomo sapiens (human)
protein transmembrane transportEndothelin receptor type BHomo sapiens (human)
podocyte differentiationEndothelin receptor type BHomo sapiens (human)
endothelin receptor signaling pathwayEndothelin receptor type BHomo sapiens (human)
renal albumin absorptionEndothelin receptor type BHomo sapiens (human)
neuroblast migrationEndothelin receptor type BHomo sapiens (human)
chordate pharynx developmentEndothelin receptor type BHomo sapiens (human)
response to sodium phosphateEndothelin receptor type BHomo sapiens (human)
response to endothelinEndothelin receptor type BHomo sapiens (human)
developmental pigmentationEndothelin receptor type BHomo 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)
neural crest cell migration5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cytokine production5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of endothelial cell proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 2BHomo sapiens (human)
heart morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
cardiac muscle hypertrophy5-hydroxytryptamine receptor 2BHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
neural crest cell differentiation5-hydroxytryptamine receptor 2BHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphorylation5-hydroxytryptamine receptor 2BHomo sapiens (human)
calcium-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 2BHomo sapiens (human)
negative regulation of apoptotic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of MAP kinase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
embryonic morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of nitric-oxide synthase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell division5-hydroxytryptamine receptor 2BHomo sapiens (human)
ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2BHomo 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 (14)

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)
endothelin receptor activityEndothelin receptor type BHomo sapiens (human)
protein bindingEndothelin receptor type BHomo sapiens (human)
peptide hormone bindingEndothelin receptor type BHomo sapiens (human)
type 1 angiotensin receptor bindingEndothelin receptor type BHomo 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)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
G-protein alpha-subunit binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
GTPase activator activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2BHomo 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 (9)

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)
plasma membraneEndothelin receptor type BHomo sapiens (human)
nuclear membraneEndothelin receptor type BHomo sapiens (human)
plasma membraneEndothelin receptor type BHomo 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)
nucleoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo 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 (96)

Assay IDTitleYearJournalArticle
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative 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.
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.
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.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical 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.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346867Human 5-HT2B receptor (5-Hydroxytryptamine 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.
AID1346867Human 5-HT2B receptor (5-Hydroxytryptamine receptors)1998Naunyn-Schmiedeberg's archives of pharmacology, Jan, Volume: 357, Issue:1
[3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor.
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.
AID624223Antagonists 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.
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.
AID1345154Rat 5-HT6 receptor (5-Hydroxytryptamine receptors)
AID624218Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2B1998Naunyn-Schmiedeberg's archives of pharmacology, Jan, Volume: 357, Issue:1
[3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) 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.
AID1346919Rat 5-HT2A receptor (5-Hydroxytryptamine receptors)1994Molecular pharmacology, Feb, Volume: 45, Issue:2
Species variations in transmembrane region V of the 5-hydroxytryptamine type 2A receptor alter the structure-activity relationship of certain ergolines and tryptamines.
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.
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.
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.
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).
AID1346903Rat 5-HT2B receptor (5-Hydroxytryptamine receptors)1993Molecular pharmacology, Mar, Volume: 43, Issue:3
Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor.
AID1346893Human 5-HT2C receptor (5-Hydroxytryptamine receptors)2003Biochemical pharmacology, Feb-01, Volume: 65, Issue:3
Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes.
AID1346868Rat 5-HT2C receptor (5-Hydroxytryptamine receptors)1997Journal of neurochemistry, Sep, Volume: 69, Issue:3
Activating mutations of the serotonin 5-HT2C receptor.
AID624218Antagonists 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.
AID624223Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A1996Biochemical pharmacology, Jan-12, Volume: 51, Issue:1
Radiolabelling of the human 5-HT2A receptor with an agonist, a partial agonist and an antagonist: effects on apparent agonist affinities.
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.
AID1345154Rat 5-HT6 receptor (5-Hydroxytryptamine receptors)1998Molecular pharmacology, Sep, Volume: 54, Issue:3
The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
AID1345170Human 5-HT6 receptor (5-Hydroxytryptamine receptors)1998Molecular pharmacology, Sep, Volume: 54, Issue:3
The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
AID624228Antagonists at Rat 5-Hydroxytryptamine receptor 5-HT2B1993Molecular pharmacology, Mar, Volume: 43, Issue:3
Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor.
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)1996Biochemical pharmacology, Jan-12, Volume: 51, Issue:1
Radiolabelling of the human 5-HT2A receptor with an agonist, a partial agonist and an antagonist: effects on apparent agonist affinities.
AID624218Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2B
AID624222Antagonists at Rat 5-Hydroxytryptamine receptor 5-HT2A1994Molecular pharmacology, Feb, Volume: 45, Issue:2
Species variations in transmembrane region V of the 5-hydroxytryptamine type 2A receptor alter the structure-activity relationship of certain ergolines and tryptamines.
AID1346893Human 5-HT2C receptor (5-Hydroxytryptamine receptors)
AID1345170Human 5-HT6 receptor (5-Hydroxytryptamine receptors)1997Molecular pharmacology, Sep, Volume: 52, Issue:3
Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor.
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.
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.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID3695Evaluated for binding affinity towards rat cortical membranes at 5-hydroxytryptamine 1 receptor binding site by using [3H]-5-HT as a radioligand.1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Central serotonin receptors as targets for drug research.
AID5855Ability to displace [3H]mesulergine (0.5 nM) from CHO cells of human 5-hydroxytryptamine 2C receptor2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
AID5273Binding affinity to 5-hydroxytryptamine 2 receptor in rat frontal cortical membranes by [3H]- KET displacement.1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Central serotonin receptors as targets for drug research.
AID1154617Displacement of [3H]5-HT from human recombinant 5-HT2C receptor expressed in HEK293 cells2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT₆ and dopamine D₂ receptor ligands.
AID255315Percent inhibition against 5-hydroxytryptamine 2C receptor at 1 uM2005Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID1141733Antagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by Cheng-Prusoff method2014European journal of medicinal chemistry, Jun-10, Volume: 80Towards the development of 5-HT₇ ligands combining serotonin-like and arylpiperazine moieties.
AID5710Ability to displace [3H]mesulergine bound to 5-hydroxytryptamine 2C receptor in rat cortex1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.
AID1297677Displacement of [3H]mesulergine from 5HT2C receptor in Sprague-Dawley rat brain cortex incubated for 15 mins2016European journal of medicinal chemistry, Jun-30, Volume: 1165-HT2 receptor affinity, docking studies and pharmacological evaluation of a series of 1,3-disubstituted thiourea derivatives.
AID6685Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Optimization of the pharmacophore model for 5-HT7R antagonism. Design and synthesis of new naphtholactam and naphthosultam derivatives.
AID1154620Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT₆ and dopamine D₂ receptor ligands.
AID6072Inhibition of radiolabeled [3H]-Zacopride ligand binding to 5-hydroxytryptamine 3 receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.
AID415374Antagonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as inhibition of serotonon-induced increase in cAMP levels by HTRF assay relative to untreated control2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis of new serotonin 5-HT7 receptor ligands. Determinants of 5-HT7/5-HT1A receptor selectivity.
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.
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.
AID5723Binding affinity against 5-hydroxytryptamine 2C receptor of rat cortex1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
AID5270Binding affinity to rat cortical membranes at 5-hydroxytryptamine 2 (5-HT2) receptor using [3H]KET as a radioligand1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Central serotonin receptors as targets for drug research.
AID5712Displacement of [3H]mesulergine (0.5 nM) from rat 5-hydroxytryptamine 2C receptor expressed in SR-3T3 cells2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
AID1597292Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
AID599611Binding affinity to 5HT2C receptor in Sprague-Dawley rat frontal cortical homogenates after 15 mins2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents.
AID5743The compound was tested for their binding affinity towards 5-hydroxytryptamine 2C receptor1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Novel, potent, and selective 5-HT3 receptor antagonists based on the arylpiperazine skeleton: synthesis, structure, biological activity, and comparative molecular field analysis studies.
AID633918Displacement of [3H]mesulergine from Sprague-Dawley rat brain cortex serotonin 5-HT2C receptor after 15 mins by liquid scintillation counting in presence of 5-HT2A blocker, spiperone2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
New potent 5-HT(2A) receptor ligands containing an N'-cyanopicolinamidine nucleus: Synthesis and in vitro pharmacological evaluation.
AID1365270Displacement of [3H]mesulergine from serotonin 5-HT2C receptor in Sprague-Dawley rat brain cortex homogenates incubated for 15 mins by liquid scintillation spectrometry2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
New 5-HT
AID1186030Antagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as dissociation constant after 45 mins by HTRF assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
The extracellular entrance provides selectivity to serotonin 5-HT7 receptor antagonists with antidepressant-like behavior in vivo.
AID1278109Displacement of [3H]mesulergine from 5HT2C receptor in Sprague-Dawley rat brain cortex incubated for 15 mins by liquid scintillation counting analysis2016European journal of medicinal chemistry, Mar-03, Volume: 110Synthesis, in vitro and in vivo pharmacological evaluation of serotoninergic ligands containing an isonicotinic nucleus.
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.
AID438555Binding affinity to 5HT1A receptor2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Physical binding pocket induction for affinity prediction.
AID5240Binding affinity to 5-hydroxytryptamine 2 receptor of rat cortical membranes using [3H]- DOB; ND means no data.1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Central serotonin receptors as targets for drug research.
AID5757The compound was tested for the binding affinity against 5-hydroxytryptamine 2C receptor using [3H]Mesulergine 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.
AID1186029Antagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
The extracellular entrance provides selectivity to serotonin 5-HT7 receptor antagonists with antidepressant-like behavior in vivo.
AID442989Displacement of [3H]mesulergine from 5HT2C in Sprague-Dawley rat brain cortex by liquid scintillation counting2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Efficient microwave combinatorial synthesis of novel indolic arylpiperazine derivatives as serotoninergic ligands.
AID6670Binding affinity towards 5-hydroxytryptamine 7 receptor2000Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10
First pharmacophoric hypothesis for 5-HT7 antagonism.
AID402828Displacement of [3H]ketanserin from 5HT2A receptor in rabbit cerebral cortex membrane1997Journal of natural products, Jun, Volume: 60, Issue:6
Activity of Parthenolide at 5HT2A receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (261)

TimeframeStudies, This Drug (%)All Drugs %
pre-199071 (27.20)18.7374
1990's119 (45.59)18.2507
2000's40 (15.33)29.6817
2010's25 (9.58)24.3611
2020's6 (2.30)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.17

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 Index18.17 (24.57)
Research Supply Index5.62 (2.92)
Research Growth Index4.49 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.17)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials10 (3.77%)5.53%
Reviews7 (2.64%)6.00%
Case Studies1 (0.38%)4.05%
Observational0 (0.00%)0.25%
Other247 (93.21%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]