Compounds > vestipitant
Page last updated: 2024-11-11

vestipitant

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

Cross-References

ID SourceID
PubMed CID9832383
CHEMBL ID522987
SCHEMBL ID2485871
MeSH IDM0528765

Synonyms (21)

Synonym
gw597599
gw-597599
CHEMBL522987
vestipitant
bdbm50413891
vestipitant [inn]
334476-46-9
s052toi9bi ,
unii-s052toi9bi
1-piperazinecarboxamide, n-((1r)-1-(3,5-bis(trifluoromethyl)phenyl)ethyl)-2-(4-fluoro-2-methylphenyl)-n-methyl-, (2s)-
(2s)-n-[(1r)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl]-2-(4-fluoro-2-methylphenyl)-n-methylpiperazine-1-carboxamide
gtpl5757
vestipitant [who-dd]
1-piperazinecarboxamide, n-(1-(3,5-bis(trifluoromethyl)phenyl)ethyl)-2-(4-fluoro-2-methylphenyl)-n-methyl-
2-(s)-(4-fluoro-2-methyl-phenyl)-piperazine-1 carboxylic acid [1-(r)-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-methyl-amide
2(s)-(4-fluoro-2-methyl-phenyl)-piperazine-1-carboxylic acid [1-(r)-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-methyl-amide
2-(s)-(4-fluoro-2-methyl-phenyl)-piperazine-1-carboxylic acid [1-(r)-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-methyl-amide
SCHEMBL2485871
DTXSID50187092
DB11949
Q12747348

Research Excerpts

Overview

Vestipitant is a neurokinin 1 (NK-1) receptor antagonist that is effective for prophylaxis. Its efficacy for treating established PONV is unknown.

ExcerptReferenceRelevance
"Vestipitant is a neurokinin 1 (NK-1) receptor antagonist that is effective for prophylaxis, but its efficacy for treating established PONV is unknown."( Comparison of vestipitant with ondansetron for the treatment of breakthrough postoperative nausea and vomiting after failed prophylaxis with ondansetron.
Brigandi, RA; Dalby, PL; Eberhart, LH; Johnson, BM; Kranke, P; Noble, R; Novikova, E; Russ, SF; Thompson, JP, 2015)		1.5
"Vestipitant (1) is a novel NK1 antagonist currently under investigation for the treatment of CNS disorders and emesis. "( Application of LC-NMR and HR-NMR to the characterization of biphenyl impurities in the synthetic route development for vestipitant, a novel NK1 antagonist.
Costa, L; Guercio, G; Marchioro, C; Martini, L; Provera, S; Turco, L, 2010)		2.01
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Substance-P receptorHomo sapiens (human)IC50 (µMol)0.00030.00000.09526.8130AID779964
Substance-P receptorHomo sapiens (human)Ki0.00020.00000.79368.7470AID350133; AID453198; AID576859
[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)
Substance-P receptorHomo sapiens (human)Kd0.00000.00000.00540.0166AID350144
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (38)

Processvia Protein(s)Taxonomy
aggressive behaviorSubstance-P receptorHomo sapiens (human)
positive regulation of leukocyte migrationSubstance-P receptorHomo sapiens (human)
angiotensin-mediated drinking behaviorSubstance-P receptorHomo sapiens (human)
inflammatory responseSubstance-P receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwaySubstance-P receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationSubstance-P receptorHomo sapiens (human)
tachykinin receptor signaling pathwaySubstance-P receptorHomo sapiens (human)
long-term memorySubstance-P receptorHomo sapiens (human)
associative learningSubstance-P receptorHomo sapiens (human)
detection of abiotic stimulusSubstance-P receptorHomo sapiens (human)
response to ozoneSubstance-P receptorHomo sapiens (human)
positive regulation of epithelial cell migrationSubstance-P receptorHomo sapiens (human)
response to auditory stimulusSubstance-P receptorHomo sapiens (human)
regulation of smooth muscle cell migrationSubstance-P receptorHomo sapiens (human)
positive regulation of synaptic transmission, cholinergicSubstance-P receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicSubstance-P receptorHomo sapiens (human)
response to estradiolSubstance-P receptorHomo sapiens (human)
response to progesteroneSubstance-P receptorHomo sapiens (human)
response to nicotineSubstance-P receptorHomo sapiens (human)
operant conditioningSubstance-P receptorHomo sapiens (human)
sperm ejaculationSubstance-P receptorHomo sapiens (human)
eating behaviorSubstance-P receptorHomo sapiens (human)
positive regulation of vascular permeabilitySubstance-P receptorHomo sapiens (human)
response to ethanolSubstance-P receptorHomo sapiens (human)
positive regulation of action potentialSubstance-P receptorHomo sapiens (human)
positive regulation of blood pressureSubstance-P receptorHomo sapiens (human)
positive regulation of ossificationSubstance-P receptorHomo sapiens (human)
positive regulation of vasoconstrictionSubstance-P receptorHomo sapiens (human)
positive regulation of hormone secretionSubstance-P receptorHomo sapiens (human)
behavioral response to painSubstance-P receptorHomo sapiens (human)
regulation of smooth muscle cell proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of lymphocyte proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of epithelial cell proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of stress fiber assemblySubstance-P receptorHomo sapiens (human)
response to electrical stimulusSubstance-P receptorHomo sapiens (human)
smooth muscle contraction involved in micturitionSubstance-P receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionSubstance-P receptorHomo sapiens (human)
positive regulation of flagellated sperm motilitySubstance-P receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Processvia Protein(s)Taxonomy
tachykinin receptor activitySubstance-P receptorHomo sapiens (human)
protein bindingSubstance-P receptorHomo sapiens (human)
substance P receptor activitySubstance-P receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
plasma membraneSubstance-P receptorHomo sapiens (human)
cell surfaceSubstance-P receptorHomo sapiens (human)
dendriteSubstance-P receptorHomo sapiens (human)
sperm flagellumSubstance-P receptorHomo sapiens (human)
cell bodySubstance-P receptorHomo sapiens (human)
sperm headSubstance-P receptorHomo sapiens (human)
sperm midpieceSubstance-P receptorHomo sapiens (human)
plasma membraneSubstance-P receptorHomo sapiens (human)
sperm midpieceSubstance-P receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (28)

Assay IDTitleYearJournalArticle
AID350140Antagonist activity at human recombinant NK1 receptor expressed in CHO cells assessed as inhibition of substance P-induced cytosolic calcium release at 3 nM after 60 mins by FLIPR2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID453199Anxiolytic-like activity in po or sc dosed gerbils assessed as inhibition of GR-73632-induced foot tapping administered 1 hr before GR-73632 challenge measured2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK(1) receptor antagonists.
AID350135Inhibition of GR-73632-induced foot tapping in po dosed Mongolian gerbil assessed as duration of repetitive hind foot tapping administered 1 hr before GR-73632 challenge2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID350148Bioavailability in rat2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID350139Inhibition of GR-73632-induced foot tapping in po dosed Mongolian gerbil assessed as duration of repetitive hind foot tapping administered 1 hr before GR-73632 challenge measured after 4 hrs2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID350141Antagonist activity at human recombinant NK1 receptor expressed in CHO cells assessed as inhibition of substance P-induced cytosolic calcium release at 5 nM after 60 mins by FLIPR2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID350146Chemical stability assessed as half life2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID350144Binding affinity to human recombinant NK1 receptor expressed in CHO cells assessed as dissociation constant2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID350151Plasma clearance in dog2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID577009Inhibition of GR73632-induced foot tapping in orally dosed Mongolian gerbil after 1 hr2011Journal of medicinal chemistry, Feb-24, Volume: 54, Issue:4
Discovery and biological characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a new potent and selective neurokinin 1 (NK1) receptor antagonist clini
AID350145Binding affinity to human recombinant NK1 receptor expressed in CHO cells assessed as association constant2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID350154Ratio of drug level in brain to plasma in rat at 1 mg/kg, iv after 5 mins2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID779964Antagonist activity at NK1 receptor (unknown origin)2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.
AID350153Half life in dog2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID350142Antagonist activity at human recombinant NK1 receptor expressed in CHO cells assessed as inhibition of substance P-induced cytosolic calcium release at 10 nM after 60 mins by FLIPR2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID350138Inhibition of GR-73632-induced foot tapping in po dosed Mongolian gerbil assessed as duration of repetitive hind foot tapping administered 1 hr before GR-73632 challenge measured after 2 hrs2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID350152Half life in rat2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID350136Inhibition of GR-73632-induced foot tapping in po dosed Mongolian gerbil assessed as duration of repetitive hind foot tapping administered 1 hr before GR-73632 challenge measured after 8 hrs2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID350134Antagonist activity at human recombinant NK1 receptor expressed in CHO cells assessed as inhibition of substance P-induced cytosolic calcium release after 30 mins by FLIPR2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID350147Receptor occupancy at human recombinant NK1 receptor expressed in CHO cells assessed as half life of occupancy2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID576859Displacement of [3H]SP from human NK1 receptor expressed in CHO cells by liquid scintillation counting2011Journal of medicinal chemistry, Feb-24, Volume: 54, Issue:4
Discovery and biological characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a new potent and selective neurokinin 1 (NK1) receptor antagonist clini
AID350149Bioavailability in dog2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID350137Inhibition of GR-73632-induced foot tapping in po dosed Mongolian gerbil assessed as duration of repetitive hind foot tapping administered 1 hr before GR-73632 challenge measured after 1 hr2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID350150Plasma clearance in rat2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID453198Displacement of [3H]substance P from human NK1 receptor expressed in CHO cells2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK(1) receptor antagonists.
AID350133Displacement of [3H]substance P from human recombinant NK1 receptor expressed in CHO cells2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
AID1346346Human NK1 receptor (Tachykinin receptors)2008European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology, Oct, Volume: 18, Issue:10
Cellular and behavioural profile of the novel, selective neurokinin1 receptor antagonist, vestipitant: a comparison to other agents.
AID1346346Human NK1 receptor (Tachykinin receptors)2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (13)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (15.38)29.6817
2010's11 (84.62)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 23.40

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 Index23.40 (24.57)
Research Supply Index2.89 (2.92)
Research Growth Index4.65 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.40)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (30.77%)5.53%
Reviews1 (7.69%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (61.54%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (9)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase I, Randomized, Placebo-Controlled, Parallel-Group, Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of a Single Intravenous Dose of the Captisol™ Formulation of Vestipitant (GW597599) in Healthy Adult Subjects [NCT01290133]Phase 155 participants (Actual)Interventional2011-05-31Completed
Vestipitant and Vofopitant 2 Day PSG Study for Insomnia [NCT00606697]Phase 251 participants (Actual)Interventional2007-12-19Completed
A 28-Day, Polysomnographic and Subjective Assessment of Vestipitant (15mg/Day) for the Treatment of Primary Insomnia in Adult Outpatients [NCT00992160]Phase 2161 participants (Actual)Interventional2009-05-31Completed
Phase II Multicenter, Dose Ranging Study on the Safety and Antiemetic Efficacy of One Day Intraveous Dosing of GW597599 Administered With Ondansetron HCL in a Female Subjects Undergoing Surgical Procedures of High Emetogenic Risk [NCT00600990]Phase 2624 participants (Actual)Interventional2004-12-31Completed
A Randomised, Double-Blind, Parallel-Group, Placebo-Controlled Fixed Dose Study Comparing the Efficacy and Safety of GW597599/Paroxetine Combination or Paroxetine Monotherapy to Placebo in Patients With Social Anxiety Disorder (SAD) [NCT00403962]Phase 2204 participants Interventional2004-11-30Completed
Randomised, Double-blind, Placebo Controlled, Cross-over Study Comparing the Effects of Both Single Dose and Repeated Dosing Treatment for 14 Days of Vestipitant or Vestipitant / Paroxetine Combination in an Enriched Population of Subjects With Tinnitus & [NCT00394056]Phase 226 participants (Actual)Interventional2006-12-31Completed
An 8-Week, Randomized, Double-Blind, Placebo-Controlled, Multicenter, Fixed-Dose Study Comparing the Efficacy and Safety of GW597599B or Paroxetine to Placebo in Moderately to Severely Depressed Patients With Major Depressive Disorder [NCT00048204]Phase 2372 participants (Actual)Interventional2002-11-04Completed
A Double-blind, Triple Dummy, Placebo-controlled, Randomised, Parallel Group Positron Emission Tomography Study to Investigate the Effects of a 8 Week Administration of GW597599 and Paroxetine Either Alone or in Combination on Regional Cerebral Blood Flow [NCT00343707]Phase 272 participants (Actual)Interventional2004-11-30Completed
A Multicenter, Randomized, Single-blind, Active-controlled, Parallel Group, Phase II Study to Evaluate the Efficacy, Safety, and Tolerability of a Single Intravenous (6 mg, 12 mg, 18 mg, 24 mg or 36 mg) Dose of the Neurokinin-1 Receptor Antagonist, Vestip [NCT01507194]Phase 2131 participants (Actual)Interventional2012-02-29Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
alprazolam
Alprazolam: A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238). alprazolam : A member of the class of triazolobenzodiazepines that is 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine carrying methyl, phenyl and chloro substituents at positions 1, 6 and 8 respectively. Alprazolam is only found in individuals that have taken this drug.		3.4811organochlorine compound;
triazolobenzodiazepine		anticonvulsant;
anxiolytic drug;
GABA agonist;
muscle relaxant;
sedative;
xenobiotic
diazepam
Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5.		2.06101,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
environmental contaminant;
sedative;
xenobiotic
ondansetron
Ondansetron: A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.		9.4111carbazoles
diphenyl
diphenyl: RN given refers to unlabeled cpd; structure		2.0510aromatic fungicide;
benzenes;
biphenyls		antifungal agrochemical;
antimicrobial food preservative
phenylpiperazine
phenylpiperazine: RN given refers to parent cpd		2.0510
fluorobenzenes
Fluorobenzenes: Derivatives of BENZENE that contain FLUORINE.. monofluorobenzene : The simplest member of the class of monofluorobenzenes that is benzene carrying a single fluoro substituent.. fluorobenzenes : Any fluoroarene that is a benzene or a substituted benzene carrying at least one fluoro group.		8.91114monofluorobenzenesNMR chemical shift reference compound
substance p
[no description available]		2.0410peptideneurokinin-1 receptor agonist;
neurotransmitter;
vasodilator agent
paroxetine
Paroxetine: A serotonin uptake inhibitor that is effective in the treatment of depression.. paroxetine : A benzodioxole that consists of piperidine bearing 1,3-benzodioxol-5-yloxy)methyl and 4-fluorophenyl substituents at positions 3 and 4 respectively; the (3S,4R)-diastereomer. Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (Ki = 0.05 nM). Ki values are 1.1, 350 and 1100 nM for inhibition of [3H]-5-HT, [3H]-l-NA and [3H]-DA uptake respectively. Displays minimal affinity for alpha1-, alpha2- or beta-adrenoceptors, 5-HT2A, 5-HT1A, D2 or H1 receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (Ki = 42 nM). Antidepressant and anxiolytic in vivo.		9.3711aromatic ether;
benzodioxoles;
organofluorine compound;
piperidines		antidepressant;
anxiolytic drug;
hepatotoxic agent;
P450 inhibitor;
serotonin uptake inhibitor
cp 96345
CP 96345: structure given in first source; potent nonpeptide antagonist of the substance P (NK1) receptor; CP 96344 is enantiomer of CP 96345		2.0810
(2-methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine
(2-methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine: structure given in first source		2.0810
l 733060
3-((3,5-bis(trifluoromethyl)phenyl)methyloxy)-2-phenylpiperidine: RN given refers to (2S-cis)-isomer; L-733,061 is pharmacologically inactive; structure in first source		2.4720piperidines
betadex
beta-Cyclodextrins: Cyclic GLUCANS consisting of seven (7) glucopyranose units linked by 1,4-glycosidic bonds.		2.1310cyclodextrin
netupitant
netupitant: orally active neurokinin-1 receptor antagonist. netupitant : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2-[3,5-bis(trifluoromethyl)phenyl]-2-methylpropanoic acid with the secondary amino group of N-methyl-4-(2-methylphenyl)-6-(4-methylpiperazin-1-yl)pyridin-3-amine; an antiemetic used in combination with palonosetron hydrochloride (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy.		2.0810aminopyridine;
monocarboxylic acid amide;
N-alkylpiperazine;
N-arylpiperazine;
organofluorine compound;
toluenes		antiemetic;
neurokinin-1 receptor antagonist
vofopitant
[no description available]		3.8621
orvepitant
[no description available]		2.0810
casopitant
[no description available]		3.8730piperidines
piperidines
Piperidines: A family of hexahydropyridines.		8.91114
aprepitant
Aprepitant: A morpholine neurokinin-1 (NK1) receptor antagonist that is used in the management of nausea and vomiting caused by DRUG THERAPY, and for the prevention of POSTOPERATIVE NAUSEA AND VOMITING.. aprepitant : A morpholine-based antiemetic, which is or the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors.		2.0810(trifluoromethyl)benzenes;
cyclic acetal;
morpholines;
triazoles		antidepressant;
antiemetic;
neurokinin-1 receptor antagonist;
peripheral nervous system drug;
substance P receptor antagonist
ConditionIndicatedRelationship StrengthStudiesTrials
Depression, Endogenous
[description not available]		02.0610
Depressive Disorder
An affective disorder manifested by either a dysphoric mood or loss of interest or pleasure in usual activities. The mood disturbance is prominent and relatively persistent.		14.0610
Depression, Involutional
Form of depression in those MIDDLE AGE with feelings of ANXIETY.		0310
Chronic Insomnia
[description not available]		04.7921
Depressive Disorder, Major
Disorder in which five (or more) of the following symptoms have been present during the same 2-week period and represent a change from previous functioning; at least one of the symptoms is either (1) depressed mood or (2) loss of interest or pleasure. Symptoms include: depressed mood most of the day, nearly every daily; markedly diminished interest or pleasure in activities most of the day, nearly every day; significant weight loss when not dieting or weight gain; Insomnia or hypersomnia nearly every day; psychomotor agitation or retardation nearly every day; fatigue or loss of energy nearly every day; feelings of worthlessness or excessive or inappropriate guilt; diminished ability to think or concentrate, or indecisiveness, nearly every day; or recurrent thoughts of death, recurrent suicidal ideation without a specific plan, or a suicide attempt. (DSM-5)		1510
Sleep Initiation and Maintenance Disorders
Disorders characterized by impairment of the ability to initiate or maintain sleep. This may occur as a primary disorder or in association with another medical or psychiatric condition.		04.7921
Anxiety Neuroses
[description not available]		03.4811
Anxiety
Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.		03.4811
Anxiety Disorders
Persistent and disabling ANXIETY.		03.4811
Emesis, Postoperative
[description not available]		04.4111
Postoperative Nausea and Vomiting
Emesis and queasiness occurring after anesthesia.		111.4111
Pulsatile Tinnitus
[description not available]		04.3711
Tinnitus
A nonspecific symptom of hearing disorder characterized by the sensation of buzzing, ringing, clicking, pulsations, and other noises in the ear. Objective tinnitus refers to noises generated from within the ear or adjacent structures that can be heard by other individuals. The term subjective tinnitus is used when the sound is audible only to the affected individual. Tinnitus may occur as a manifestation of COCHLEAR DISEASES; VESTIBULOCOCHLEAR NERVE DISEASES; INTRACRANIAL HYPERTENSION; CRANIOCEREBRAL TRAUMA; and other conditions.		111.3711