Page last updated: 2024-11-12

vabicaserin

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

Description

vabicaserin: an antipsychotic agent and 5-HT2C receptor agonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11521822
CHEMBL ID2110670
SCHEMBL ID2980790
MeSH IDM0555539

Synonyms (23)

Synonym
vabicaserin
cyclopenta(4,5)pyrido(3,2,1-jk)(1,4)benzodiazepine, 4,5,6,7,9,9a,10,11,12,12a-decahydro-, (9ar,12as)-rel-(-)-
620948-93-8
vabicaserin [inn]
CHEMBL2110670
unii-wd9550hpnl
887258-95-9
(-)-(9ar*,12as*)-4,5,6,7,9,9a,10,11,12,12a-decahydrocyclopenta(4,5)pyrido(3,2,1-jk)(1,4)benzodiazepine
wd9550hpnl ,
cyclopenta(4,5)pyrido(3,2,1-jk)(1,4)benzodiazepine, 1,2,3,4,6,6a,7,8,9,9a-decahydro-, (6ar,9as)-
SCHEMBL2980790
vabicaserin [who-dd]
(-)-(9ar*,12as*)-4,5,6,7,9,9a,10,11,12,12a-decahydrocyclopenta(4,5)pyrido(3,2,1- jk)(1,4)benzodiazepine
bdbm50076216
DB12071
Q7907856
(-)-vabicaserin
(9ar,12as)-4,5,6,7,9,9a,10,11,12,12a-decahydrocyclopenta[c][1,4]diazepino[6,7,1-ij]quinoline
cis-4,5,6,7,9,9a,10,11,12,12a-decahydrocyclopenta[c][1,4]diazepino[6,7,1-ij]quinoline
A936771
(9ar,12as)-4,5,6,7,9,9a,10,11,12,12a-decahydrocyclopenta[4,5]pyrido[3,2,1-jk][1,4]benzodiazepine
DTXSID601336565
cyclopenta[4,5]pyrido[3,2,1-jk][1,4]benzodiazepine, 4,5,6,7,9,9a,10,11,12,12a-decahydro-, (9ar,12as)-

Research Excerpts

Overview

Vabicaserin is a potent 5-hydroxytryptamine(2C) agonist that is currently being developed for the treatment of the psychotic symptoms of schizophrenia.

ExcerptReferenceRelevance
"Vabicaserin is a potent 5-hydroxtryptamine 2C full agonist with therapeutic potential for a wide array of psychiatric disorders. "( Species differences in the formation of vabicaserin carbamoyl glucuronide.
Burghart, P; Chandrasekaran, A; DeMaio, W; Hultin, T; Jordan, R; Li, H; Moore, R; Poola, N; Scatina, J; Tong, Z, 2010
)
2.07
"Vabicaserin is a potent 5-hydroxytryptamine(2C) agonist that is currently being developed for the treatment of the psychotic symptoms of schizophrenia. "( Metabolism of vabicaserin in mice, rats, dogs, monkeys, and humans.
Chandrasekaran, A; DeMaio, W; Espina, R; Jordan, R; Lu, W; Scatina, J; Tong, Z, 2010
)
2.16
[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)
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.00300.00010.954910.0000AID1075710
[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 2CHomo sapiens (human)EC50 (µMol)0.00800.00010.10082.4500AID1075711; AID1199723
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 2CHomo sapiens (human)K0.00550.00300.00730.0100AID1855127; AID1855128
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (19)

Processvia Protein(s)Taxonomy
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (6)

Assay IDTitleYearJournalArticle
AID1855127Binding affinity to 5-HT2C (unknown origin)2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
AID1075710Displacement of [125I]DOI from human 5-HT2C receptor2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
Imaging evaluation of 5HT2C agonists, [(11)C]WAY-163909 and [(11)C]vabicaserin, formed by Pictet-Spengler cyclization.
AID1199723Agonist activity at 5HT2C receptor (unknown origin) relative to control2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents.
AID1855128Agonist activity at 5-HT2C receptor (unknown origin)2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
AID1075711Agonist activity at human 5-HT2C receptor assessed as stimulation of Ca2+ mobilization2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
Imaging evaluation of 5HT2C agonists, [(11)C]WAY-163909 and [(11)C]vabicaserin, formed by Pictet-Spengler cyclization.
AID1199724Agonist activity at 5HT2B receptor (unknown origin) relative to control2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's9 (81.82)24.3611
2020's2 (18.18)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 24.06

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 Index24.06 (24.57)
Research Supply Index2.64 (2.92)
Research Growth Index5.06 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (24.06)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (18.18%)5.53%
Reviews3 (27.27%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (54.55%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]