Page last updated: 2024-11-04

naratriptan

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

Description

Naratriptan is a triptan medication used to treat migraine headaches. It is a selective 5-HT1B/1D receptor agonist, meaning it binds to and activates these receptors in the brain. This activation helps to constrict blood vessels in the brain and reduce the inflammation associated with migraines. Naratriptan is typically taken orally and is effective in relieving migraine pain and other symptoms such as nausea, vomiting, and sensitivity to light and sound. Naratriptan is studied extensively for its effectiveness in treating migraines, and its mechanism of action is well-understood. Its use is generally safe, although it can cause side effects such as dizziness, drowsiness, and muscle weakness. Like other triptans, it is not recommended for people with certain medical conditions, such as heart disease or high blood pressure.'
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naratriptan: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4440
CHEMBL ID1278
CHEBI ID7478
SCHEMBL ID68753
MeSH IDM0278097

Synonyms (53)

Synonym
AC-5013
BIDD:GT0312
bdbm50073682
naratriptan [inn:ban]
qx3kxl1za2 ,
unii-qx3kxl1za2
gtpl45
NCGC00181786-01
inchi=1/c17h25n3o2s/c1-18-23(21,22)10-7-13-3-4-17-15(11-13)16(12-19-17)14-5-8-20(2)9-6-14/h3-4,11-12,14,18-19h,5-10h2,1-2h
1h-indole-5-ethanesulfonamide, n-methyl-3-(1-methyl-4-piperidinyl)-
n-methyl-2-[3-(1-methylpiperidin-4-yl)-1h-indol-5-yl]ethanesulfonamide
121679-13-8
C07792
naratriptan
n-methyl-2-(3-(1-methylpiperiden-4-yl)indole-5-yl)ethanesulfonamide
DB00952
n-methyl-2-[3-(1-methyl-4-piperidyl)-1h-indol-5-yl]-ethanesulfonamide
naratriptanum
CHEBI:7478 ,
CHEMBL1278 ,
L000432
naramig (tn)
naratriptan (inn)
D08255
FT-0656760
A25336
n-methyl-2-[3-(1-methyl-4-piperidyl)-1h-indol-5-yl]ethanesulfonamide
n-methyl-3-(1-methyl-4-piperidinyl)-1h-indole-5-ethanesulfonamide
colatan
BCP9000978
NCGC00181786-03
AKOS015895854
naratriptan [who-dd]
naratriptan [orange book]
naratriptan [vandf]
naratriptan [mi]
naratriptan [inn]
HY-B0197
n-methyl-3-(1-methyl-4 -piperidinyl)-1h-indole-5-ethansulphonamide
n-methyl-3-(1-methyl-4-piperidinyl)-1h-indole-5-ethanesulphonamide
2-[3-(1-methyl-piperidin-4-yl)-1h-indol-5-yl]-ethanesulfonic acid methylamide
SCHEMBL68753
n-methyl-2-(3-(1-methylpiperidin-4-yl)-1h-indol-5-yl)ethanesulfonamide
AB01565792_02
DTXSID7023354 ,
n-methyl-2-[3-(1-methylpiperidin-4-yl)-1h-indol-5-yl]ethane-1-sulfonamide
NCGC00181786-04
Q421315
NCGC00181786-08
EN300-18567334
dtxcid003354
n-methyl-2-(3-(1-methyl-4-piperidyl)-1h-indol-5-yl)-ethanesulfonamide
n02cc02

Research Excerpts

Overview

Naratriptan is a second-generation triptan antimigraine drug, developed at a time when CNS activity was thought not to be relevant to its therapeutic effect in migraine. It is a novel 5-HT1 agonist developed to treat acute migraine.

ExcerptReferenceRelevance
"Naratriptan is a selective 5-HT(1B/1D) receptor agonist, with a high affinity at the 5-HT(1B), 5-HT(1D) and 5-HT(1F) receptor subtypes. "( Naratriptan.
Massiou, H, 2001
)
3.2
"Naratriptan is an effective and well-tolerated treatment for acute attacks of migraine. "( Naratriptan for the treatment of acute migraine: meta-analysis of randomised controlled trials.
Ashcroft, DM; Millson, D, 2004
)
3.21
"Naratriptan is a second-generation triptan antimigraine drug, developed at a time when CNS activity was thought not to be relevant to its therapeutic effect in migraine."( Preclinical neuropharmacology of naratriptan.
Lambert, GA, 2005
)
1.33
"Naratriptan is a promising new oral therapy for acute migraine; it may successfully treat patients who poorly tolerate other triptan therapies or have longer duration migraine headaches."( Naratriptan: an alternative for migraine.
Dulli, DA, 1999
)
3.19
"Naratriptan is a more potent and more lipophilic member of this class of agent and could prove beneficial in such patients."( Naratriptan efficacy in migraineurs who respond poorly to oral sumatriptan.
Bolden-Watson, CP; McNeal, S; O'Quinn, S; Putnam, GP; Spierings, EL; Stark, S,
)
2.3
"Naratriptan is an alternative therapy for migraineurs who respond poorly to oral sumatriptan. "( Naratriptan efficacy in migraineurs who respond poorly to oral sumatriptan.
Bolden-Watson, CP; McNeal, S; O'Quinn, S; Putnam, GP; Spierings, EL; Stark, S,
)
3.02
"Naratriptan is a novel 5-HT1 agonist developed to treat acute migraine. "( Pharmacokinetics of naratriptan in adolescent subjects with a history of migraine.
Christensen, ML; Eades, SK; Fuseau, E; Hak, LJ; Kempsford, RD; Phelps, SJ, 2001
)
2.08
"Naratriptan is a newly developed triptan shown to be effective in the treatment of migraine."( Treatment of migraine in Canada with naratriptan: a cost-effectiveness analysis.
Black, L; Caro, G; Caro, JJ; Getsios, D; Raggio, G, 2001
)
1.3

Effects

Naratriptan 1 mg b.i.d. has some effect in the short-term prophylactic treatment of menstruation-associated migraine in 3 RCTs. It has also a therapeutic effect on the nausea of migraine, possibly exerting its action at the level of the nucleus tractus solitarius via the same mechanisms by which it inhibits nociceptive input.

ExcerptReferenceRelevance
"Naratriptan 1 mg b.i.d. has some effect in the short-term prophylactic treatment of menstruation-associated migraine in 3 RCTs."( Published and not fully published double-blind, randomised, controlled trials with oral naratriptan in the treatment of migraine: a review based on the GSK Trial Register.
Tfelt-Hansen, PC, 2011
)
1.31
"Naratriptan has also a therapeutic effect on the nausea of migraine, possibly exerting its action at the level of the nucleus tractus solitarius via the same mechanisms by which it inhibits trigeminovascular nociceptive input."( Preclinical neuropharmacology of naratriptan.
Lambert, GA, 2005
)
1.33
"Naratriptan has high affinity for human recombinant 5HT1B and 5HT1D receptors (pKi = 8.7 +/- 0.03 and 8.3 +/- 0.1, respectively) and causes contractions of dog isolated basilar and middle cerebral artery (EC50 values of 0.11 and 0.07 microM, respectively)."( Naratriptan: biological profile in animal models relevant to migraine.
Beattie, DT; Connor, HE; Feniuk, W; Humphrey, PP; North, PC; Oxford, AW; Saynor, DA, 1997
)
2.46
"Naratriptan has been recently approved for acute oral migraine therapy."( Naratriptan: an alternative for migraine.
Dulli, DA, 1999
)
2.47

Actions

ExcerptReferenceRelevance
"Naratriptan tended to increase ASF slope (mean difference 0.23 +/- 0.62 microV/10 dB, p = 0.06) while zolmitriptan (0.08 +/- 0.95 microV/10 dB, p = 0.35) did not."( Auditory evoked potentials in the assessment of central nervous system effects of antimigraine drugs.
Ferrari, MD; Lamers, FP; Roon, KI; Sándor, PS; Schoenen, J; Schoonman, GG; van Dijk, JG, 1999
)
1.02

Treatment

ExcerptReferenceRelevance
"naratriptan in the acute treatment of migraine."( Comparative efficacy of eletriptan vs. naratriptan in the acute treatment of migraine.
Bordini, CA; Garcia-Ramos, G; Hettiarachchi, J; Hilliard, B; Leston, J; MacGregor, EA, 2003
)
1.31

Toxicity

ExcerptReferenceRelevance
" Information regarding safety of triptans while breastfeeding is limited but also reassuring, as the minimal amounts excreted into the milk are insufficient to cause any adverse effects on the breastfeeding infant."( Safety of triptans for migraine headaches during pregnancy and breastfeeding.
Bozzo, P; Duong, S; Einarson, A; Nordeng, H, 2010
)
0.36

Pharmacokinetics

A previously developed pharmacokinetic (PK)/pharmacodynamic (PD) model for naratriptan disposition and effect was used. The analysis was based on phase I pharmacokinetics nar atriptan data, sumatriptans pharmacodynamic data, and narAtriptan preclinical (animal) potency information.

ExcerptReferenceRelevance
" Pharmacokinetic parameters evaluated after administration of single intravenous and oral doses were very similar and the ANOVA analysis did not show any statistically significant differences for t1/2, Cmax, V or AUC (normalised)."( A method using a liquid chromatographic-electrospray-mass spectrometric assay for the determination of antimigraine compounds: preliminary pharmacokinetics of MDL 74,721, sumatriptan and naratriptan, in rabbit.
David, M; Duléry, BD; Huebert, ND; Petty, MA; Schoun, J, 1997
)
0.49
" The analysis was based on phase I pharmacokinetic naratriptan data, sumatriptan pharmacodynamic data, and naratriptan preclinical (animal) potency information, together with general knowledge as to how migraine affects oral absorption."( Uncertainty analysis in pharmacokinetics and pharmacodynamics: application to naratriptan.
Aarons, L; Gueorguieva, I; Nestorov, IA; Rowland, M, 2005
)
0.81
"A previously developed pharmacokinetic (PK)/pharmacodynamic (PD) model for naratriptan disposition and effect was used."( Uncertainty analysis in pharmacokinetics and pharmacodynamics: application to naratriptan.
Aarons, L; Gueorguieva, I; Nestorov, IA; Rowland, M, 2005
)
0.79
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35

Bioavailability

ExcerptReferenceRelevance
" dose both probably due to extensive and rapid metabolism of the parent drugs as suggested by the low values for bioavailability (range 13."( A method using a liquid chromatographic-electrospray-mass spectrometric assay for the determination of antimigraine compounds: preliminary pharmacokinetics of MDL 74,721, sumatriptan and naratriptan, in rabbit.
David, M; Duléry, BD; Huebert, ND; Petty, MA; Schoun, J, 1997
)
0.49
" In conscious rats and dogs, naratriptan has high oral bioavailability (71% and 95%, respectively)."( Naratriptan: biological profile in animal models relevant to migraine.
Beattie, DT; Connor, HE; Feniuk, W; Humphrey, PP; North, PC; Oxford, AW; Saynor, DA, 1997
)
2.03
" Increasing bioavailability has been achieved with greater lipophilicity and thus the potential for greater activity in the central nervous system."( Inhibition of trigeminal neurones after intravenous administration of naratriptan through an action at 5-hydroxy-tryptamine (5-HT(1B/1D)) receptors.
Goadsby, PJ; Knight, Y, 1997
)
0.53
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
"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

Oral rizatriptan 10 mg enabled more migraine sufferers to function normally at 2 h after dosing. Plasma concentrations increased from the first minute after intranasal dosing suggesting that sumatriptans are absorbed into the general systemic circulation from the nasal cavity in rats.

ExcerptRelevanceReference
" At dosing and at predetermined intervals beginning 30 minutes postdose, patients recorded migraine pain severity, clinical disability, and presence of associated migraine symptoms."( Naratriptan is effective and well tolerated in the acute treatment of migraine. Results of a double-blind, placebo-controlled, parallel-group study. Naratriptan S2WA3001 Study Group.
Asgharnejad, M; Elkind, A; Klassen, A; Laurenza, A; Webster, C,
)
1.57
" However, plasma concentrations increased from the first minute after intranasal dosing suggesting that sumatriptan and naratriptan are absorbed into the general systemic circulation from the nasal cavity in rats in a first-order fashion with no lag time."( Intranasal absorption of sumatriptan and naratriptan: no evidence of local transfer from the nasal cavities to the brain arterial blood in male rats.
Deprez, S; Einer-Jensen, N; Larsen, L; Schwartz, S; Starns, E, 2001
)
0.78
"In direct head-to-head comparative clinical trials, oral rizatriptan 10 mg enabled more migraine sufferers to function normally at 2 h after dosing than oral sumatriptan, naratriptan, and zolmitriptan."( Restoring migraine sufferers' ability to function normally: a comparison of rizatriptan and other triptans in randomized trials.
Bussone, G; D'Amico, D; Gerth, W; Lines, CR; McCarroll, KA, 2002
)
0.51
" Disease dynamics must be considered to evaluate treatment response adequately and optimise the dosing regimen in migraine."( A model-based approach to treatment comparison in acute migraine.
Danhof, M; Della Pasqua, O; Maas, HJ, 2006
)
0.33
"The present research project involves development and validation of a stability-indicating HPTLC method for the estimation of naratriptan-HCl in their pharmaceutical dosage forms and its content uniformity testing."( Development and Validation of Stability-Indicating HPTLC Method for Estimation of Naratriptan Hydrochloride in Its Pharmaceutical Dosage Form and Its Content Uniformity Testing.
Bodiwala, KB; Chotalia, J; Marolia, BP; Prajapati, PB; Shah, SA, 2016
)
0.87
"HCl) for the treatment of migraine and is available in tablet dosage forms for oral administration."( Oral transmucosal delivery of naratriptan.
Lane, ME; Sattar, M, 2016
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

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.
vasoconstrictor agentDrug used to cause constriction of the blood vessels.
[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 (3)

ClassDescription
sulfonamideAn amide of a sulfonic acid RS(=O)2NR'2.
tryptaminesTryptamine and its substitution derivatives.
heteroarylpiperidine
[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 (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
EWS/FLI fusion proteinHomo sapiens (human)Potency1.18100.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.04500.00010.532610.0000AID3850
5-hydroxytryptamine receptor 1DHomo sapiens (human)Ki0.00230.00010.808710.0000AID4627
5-hydroxytryptamine receptor 1BHomo sapiens (human)Ki0.00330.00010.54859.2100AID4256
[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 1DHomo sapiens (human)EC50 (µMol)0.00160.00080.00600.0160AID4571
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (38)

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)
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 internalization5-hydroxytryptamine receptor 1BHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of gamma-aminobutyric acid secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of serotonin secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of synaptic transmission, GABAergic5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to cocaine5-hydroxytryptamine receptor 1BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 1BHomo sapiens (human)
drinking behavior5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to ethanol5-hydroxytryptamine receptor 1BHomo sapiens (human)
bone remodeling5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to mineralocorticoid5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to alkaloid5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to xenobiotic stimulus5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 1BHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentration5-hydroxytryptamine receptor 1BHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferation5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of synaptic vesicle exocytosis5-hydroxytryptamine receptor 1BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

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)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1DHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1DHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1BHomo sapiens (human)
voltage-gated calcium channel activity involved in regulation of presynaptic cytosolic calcium levels5-hydroxytryptamine receptor 1BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

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 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)
endoplasmic reticulum5-hydroxytryptamine receptor 1BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
calyx of Held5-hydroxytryptamine receptor 1BHomo sapiens (human)
serotonergic synapse5-hydroxytryptamine receptor 1BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 1BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (104)

Assay IDTitleYearJournalArticle
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.
AID1347159Primary screen GU Rhodamine 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.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
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.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID539464Solubility of the compound in 0.1 M phosphate buffer at 600 uM at pH 7.4 after 24 hrs by LC/MS/MS analysis2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.
AID4591Intrinsic activity for 5-hydroxytryptamine 1D receptor1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID4256In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID4627In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1D receptor1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID3850In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1A receptor1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID4571Ability to inhibit forskolin-stimulated adenylate cyclase in a cell line expressing human 5-hydroxytryptamine 1D receptor1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
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.
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.
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.
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.
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.
AID1347111qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347127qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347126qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347129qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347114qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347122qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347125qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347124qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347121qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347116qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
AID1347110qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)2018Oncotarget, 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.
AID1347109qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
AID1347112qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
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.
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.
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.
AID1347118qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347113qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
AID1347119qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347128qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347115qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347117qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347123qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1346739Human 5-HT1F receptor (5-Hydroxytryptamine receptors)1999European journal of pharmacology, Mar-05, Volume: 368, Issue:2-3
Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
AID624233Agonists at Human 5-Hydroxytryptamine receptor 5-HT1F2005Naunyn-Schmiedeberg's archives of pharmacology, Mar, Volume: 371, Issue:3
[3H]LY334370, a novel radioligand for the 5-HT1F receptor. I. In vitro characterization of binding properties.
AID1346528Human 5-HT1D receptor (5-Hydroxytryptamine receptors)1997Naunyn-Schmiedeberg's archives of pharmacology, Sep, Volume: 356, Issue:3
Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist.
AID1346739Human 5-HT1F receptor (5-Hydroxytryptamine receptors)2005Naunyn-Schmiedeberg's archives of pharmacology, Mar, Volume: 371, Issue:3
[3H]LY334370, a novel radioligand for the 5-HT1F receptor. I. In vitro characterization of binding properties.
AID1346528Human 5-HT1D receptor (5-Hydroxytryptamine receptors)1995British journal of pharmacology, Mar, Volume: 114, Issue:5
5-Hydroxytryptamine (5-HT)4 receptors in post mortem human brain tissue: distribution, pharmacology and effects of neurodegenerative diseases.
AID624210Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A1997Naunyn-Schmiedeberg's archives of pharmacology, Jun, Volume: 355, Issue:6
Agonist activity of antimigraine drugs at recombinant human 5-HT1A receptors: potential implications for prophylactic and acute therapy.
AID624230Agonists at Human 5-Hydroxytryptamine receptor 5-ht1e1999European journal of pharmacology, Mar-05, Volume: 368, Issue:2-3
Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
AID1346603Human 5-ht1e receptor (5-Hydroxytryptamine receptors)1999European journal of pharmacology, Mar-05, Volume: 368, Issue:2-3
Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
AID1346264Human 5-HT1B receptor (5-Hydroxytryptamine receptors)1999European journal of pharmacology, Mar-05, Volume: 368, Issue:2-3
Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)1999European journal of pharmacology, Mar-05, Volume: 368, Issue:2-3
Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)1997Naunyn-Schmiedeberg's archives of pharmacology, Jun, Volume: 355, Issue:6
Agonist activity of antimigraine drugs at recombinant human 5-HT1A receptors: potential implications for prophylactic and acute therapy.
AID1346528Human 5-HT1D receptor (5-Hydroxytryptamine receptors)1999European journal of pharmacology, Mar-05, Volume: 368, Issue:2-3
Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
AID624233Agonists at Human 5-Hydroxytryptamine receptor 5-HT1F1999European journal of pharmacology, Mar-05, Volume: 368, Issue:2-3
Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
AID624210Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A1999European journal of pharmacology, Mar-05, Volume: 368, Issue:2-3
Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (190)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's34 (17.89)18.2507
2000's100 (52.63)29.6817
2010's44 (23.16)24.3611
2020's12 (6.32)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 47.67

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

MetricThis Compound (vs All)
Research Demand Index47.67 (24.57)
Research Supply Index5.44 (2.92)
Research Growth Index4.55 (4.65)
Search Engine Demand Index143.73 (26.88)
Search Engine Supply Index3.77 (0.95)

This Compound (47.67)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials24 (11.71%)5.53%
Reviews32 (15.61%)6.00%
Case Studies16 (7.80%)4.05%
Observational3 (1.46%)0.25%
Other130 (63.41%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (11)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Single Dose, Two-Period, Two-Treatment, Two-Way Crossover Bioequivalence Study of Naratriptan Hydrochloride 2.5 mg Tablets Under Fed Conditions [NCT01161654]33 participants (Actual)Interventional2007-08-31Completed
Drug Use Investigation for AMERGE (Naratriptan Hydrochloride) Tablet [NCT01376193]500 participants (Actual)Observational2009-04-30Completed
Special Drug Use Investigation for AMERGE Tablet (Long-term) [NCT01332383]300 participants (Actual)Observational2009-05-31Completed
Status Migrainosus - Differentiating Between Responders and Non-responders in the Setup of Real-life Clinical Practice [NCT03066544]Phase 1/Phase 250 participants (Anticipated)Interventional2016-11-30Recruiting
A Single Dose, Two-Period, Two-Treatment, Two-Way Crossover Bioequivalence Study of Naratriptan Hydrochloride 2.5 mg Tablets Under Fasted Conditions [NCT01161667]35 participants (Actual)Interventional2007-09-30Completed
A Single Center Randomized Open-Label Two Arm Crossover Study of Subject Productivity Improvement and Satisfaction With Migraine Treatment Using Treximet vs Usual Triptan [NCT01086358]Phase 460 participants (Actual)Interventional2009-09-30Completed
The Sumatriptan and Naratriptan Pregnancy Registry [NCT01059604]868 participants (Actual)Observational [Patient Registry]2001-12-31Completed
Evaluation of the Efficacy of Naratriptan for the Treatment and Prevention of Post Traumatic Headache Associated With Cognitive Dysfunction [NCT00487578]Phase 412 participants (Actual)Interventional2006-10-31Terminated(stopped due to Terminated October 2009 (in 4th year) due to low enrollment and anticipated drug expiration November 2009.)
A Multicenter, National, Double-blind, Randomized Study to Evaluate the Efficacy and Safety of a Fixed-dose Combination of Naratriptan 2,5 mg + Naproxen 500 mg Relative to Efficacy and Safety of Each Monotherapy for the Acute Treatment of Migraine [NCT01390324]Phase 30 participants (Actual)Interventional2011-12-31Withdrawn
A Phase III, Multicenter, National, Open, Randomized, Parallel and Comparative Study to Evaluate the Efficacy and Safety of a Fixed-dose Combination of Naratriptan 2,5 mg + Naproxen 500 mg for the Acute Treatment of Migraine. [NCT01726920]Phase 30 participants (Actual)Interventional2014-07-31Withdrawn(stopped due to Due to budget limitations, the company decided to withdraw this study.)
Efficacy of a Triptan in the Treatment of Hostility and Aggression Among Convicts With a Psychiatric Treatment Order [NCT00282165]Phase 48 participants (Actual)Interventional2006-11-30Terminated(stopped due to Required number of subjects to be included could not be accomplished)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01086358 (4) [back to overview]Favorable Response on Migraine-ACT
NCT01086358 (4) [back to overview]Lost Activity Time
NCT01086358 (4) [back to overview]Lost Workplace Productivity
NCT01086358 (4) [back to overview]Workplace Productivity and Activity Impairment Scale (WPAI).

Favorable Response on Migraine-ACT

The Migraine-ACT is a 4-item scale with yes/no responses. A score of 3 or more is considered favorable. The primary efficacy dataset included the 37 patients that completed both phases of the study and uses the last observed headache. The Migraine-ACT is reported as a binary measure (3 or more positive responses). The outcome presented included the percentage with a score of 3 or more, and the Odds ratio comparing the two treatments. (NCT01086358)
Timeframe: 6 months

Interventionpercentage of favorable responses (Mean)
Arm 1 - Triptan46
Arm 2 - Sumatriptan/Naproxen Sodium (Treximet) Arm71

[back to top]

Lost Activity Time

This outcome measure was lost activity time as measured by a variant of the Work Productivity and Activity Impairment Scale (WPAI) at 6 months.The primary efficacy dataset included the 37 patients that completed both phases of the study and uses the last observed headache. The primary efficacy dataset included the 37 patients that completed both phases of the study and uses the last observed headache. The unit of analysis is hours lost. The higher the score the greater impact on productivity. The range depends on the length of the attack, but in the sample among all observed attacks, lost work productivity ranged from 0-10.5 hours, while lost non-workplace activity time ranged from 0 to 8.95 hours. The total lost productivity is the sum of lost work productivity and lost non-workplace activity time. (NCT01086358)
Timeframe: 6 Months

Interventionhours (Mean)
Arm 1 - Triptan1.89
Arm 2 - Sumatriptan/Naproxen Sodium (Treximet) Arm1.22

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Lost Workplace Productivity

This outcome measure was lost workplace productivity as measured by a variant of the Work Productivity and Activity Impairment Scale (WPAI) at 6 months.The primary efficacy dataset included the 37 patients that completed both phases of the study and uses the last observed headache. The primary efficacy dataset included the 37 patients that completed both phases of the study and uses the last observed headache. The unit of analysis is hours lost. The higher the score the greater impact on productivity. The range depends on the length of the attack, but in the sample among all observed attacks, lost work productivity ranged from 0-10.5 hours, while lost non-workplace activity time ranged from 0 to 8.95 hours. The total lost productivity is the sum of lost work productivity and lost non-workplace activity time. (NCT01086358)
Timeframe: 6 months

Interventionhours (Mean)
Arm 1 - Triptan2.25
Arm 2 - Sumatriptan/Naproxen Sodium (Treximet) Arm1.23

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Workplace Productivity and Activity Impairment Scale (WPAI).

The primary outcome measure was lost productivity (workplace productivity + non-workplace activity time) as measured by a variant of the Work Productivity and Activity Impairment Scale (WPAI) at 6 months. The primary efficacy dataset included the 37 patients that completed both phases of the study and uses the last observed headache. The unit of analysis is hours lost. The higher the score the greater impact on productivity. The range depends on the length of the attack, but in the sample among all observed attacks, lost work productivity ranged from 0-10.5 hours, while lost non-workplace activity time ranged from 0 to 8.95 hours. The total lost productivity is the sum of lost work productivity and lost non-workplace activity time. (NCT01086358)
Timeframe: 6 months

Interventionhours (Mean)
Arm 1 - Triptan4.15
Arm 2 - Sumatriptan/Naproxen Sodium (Treximet) Arm2.44

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