Page last updated: 2024-11-10

rs 102221

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 CID3693566
CHEMBL ID88402
CHEBI ID93519
SCHEMBL ID7107338
MeSH IDM0280355

Synonyms (33)

Synonym
CHEMBL88402
rs-102221
BRD-K87048468-003-01-9
gtpl187
n-[5-[5-(2,4-dioxo-1,3,8-triazaspiro[4.5]decan-8-yl)pentanoyl]-2,4-dimethoxyphenyl]-4-(trifluoromethyl)benzenesulfonamide
rs-102,221
PDSP2_001617
PDSP1_001633
BPBIO1_000243
tocris-1050
NCGC00024967-01
BIOMOL-NT_000133
rs102221
NCGC00024967-02
L000523
bdbm85098
n-[5-[5-(2,4-dioxo-1,3,8-triazaspiro[4.5]decan-8-yl)-1-oxopentyl]-2,4-dimethoxyphenyl]-4-(trifluoromethyl)benzenesulfonamide
n-{5-[5-(2,4-dioxo -1,3,8-triazaspiro[4.5]dec-8-yl)pentanoyl]-2,4-dimethoxyphenyl}-4-trifluoromethylbenzenesulfonamide
SCHEMBL7107338
185376-97-0
CHEBI:93519
n-{5-[5-(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)pentanoyl] -2,4-dimethoxyphenyl}-4-(trifluoromethyl)benzenesulfonamide
rs 102221 hcl
BCP03496
rs102221 hcl
n-(5-(5-(2,4-dioxo-1,3,8-triazaspiro[4.5]decan-8-yl)pentanoyl)-2,4-dimethoxyphenyl)-4-(trifluoromethyl)benzenesulfonamide
Q7277678
n-(2,4-dimethoxy-5-(5-(4-oxidanyl-2-oxidanylidene-1,3,8-triazaspiro(4.5)dec-3-en-8-yl)pentanoyl)phenyl)-4-(trifluoromethyl)benzenesulfonamide
48d22qr8gy ,
n-{5-[5-(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)pentanoyl]-2,4-dimethoxyphenyl}-4-(trifluoromethyl)benzenesulfonamide
DTXSID801028164
n-[5-[5-(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)-1-oxopentyl]-2,4-dimethoxyphenyl]-4-(trifluoromethyl)benzenesulfonamide
benzenesulfonamide, n-[5-[5-(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)-1-oxopentyl]-2,4-dimethoxyphenyl]-4-(trifluoromethyl)-

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
", ip) indicate that the liver is the primary site of biotransformation of the compound, suggesting that both 22a and its metabolite(s) are active, compensating probably low bioavailability of the parent molecule."( Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Bednarski, M; Gunia-Krzyżak, A; Marona, H; Nitek, W; Pękala, E; Powroźnik, B; Słoczyńska, K; Walczak, M; Waszkielewicz, AM; Żesławska, E, 2016
)
0.43

Dosage Studied

ExcerptRelevanceReference
" Consistent with its action as a 5-HT2C receptor antagonist, daily dosing with RS-102221 (2 mg/kg intraperitoneal) increased food-intake and weight-gain in rats."( RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist.
Bonhaus, DW; Dawson, MW; DeSouza, A; Eglen, RM; Flippin, LA; Fontana, DJ; McNeeley, PM; Rocha, CL; Szczepanski, K; Taylor, M; Trinh, J; Weinhardt, KK,
)
0.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic ketoneA ketone in which the carbonyl group is attached to an aromatic ring.
[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 (28)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
15-lipoxygenase, partialHomo sapiens (human)Potency15.84890.012610.691788.5700AID887
USP1 protein, partialHomo sapiens (human)Potency56.23410.031637.5844354.8130AID504865
TDP1 proteinHomo sapiens (human)Potency10.76680.000811.382244.6684AID686978; AID686979
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency7.94330.031610.279239.8107AID884; AID885
lethal factor (plasmid)Bacillus anthracis str. A2012Potency12.58930.020010.786931.6228AID912
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00150.00021.874210.0000AID1285659
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00150.00021.270410.0000AID1285659
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC50 (µMol)0.00390.00011.03029.0000AID1285659; AID1336358; AID346455; AID751850; AID752214
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.00150.00010.954910.0000AID1152684; AID1196330; AID346455; AID751850
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00150.00001.819410.0000AID1285659
Small conductance calcium-activated potassium channel protein 2Rattus norvegicus (Norway rat)IC50 (µMol)0.00150.00151.22696.8000AID1285659
Small conductance calcium-activated potassium channel protein 3Rattus norvegicus (Norway rat)IC50 (µMol)0.00150.00151.68587.0000AID1285659
Small conductance calcium-activated potassium channel protein 1Rattus norvegicus (Norway rat)IC50 (µMol)0.00150.00151.22696.8000AID1285659
[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 membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (22)

Assay IDTitleYearJournalArticle
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.
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.
AID624222Antagonists at Rat 5-Hydroxytryptamine receptor 5-HT2A
AID1346867Human 5-HT2B receptor (5-Hydroxytryptamine receptors)
AID1346893Human 5-HT2C receptor (5-Hydroxytryptamine receptors)2004Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.
AID1346919Rat 5-HT2A receptor (5-Hydroxytryptamine receptors)
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)2004Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.
AID624223Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A
AID1346867Human 5-HT2B receptor (5-Hydroxytryptamine receptors)2004Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)
AID1346868Rat 5-HT2C receptor (5-Hydroxytryptamine receptors)
AID624218Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2B2004Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.
AID624218Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2B
AID624223Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A2004Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.
AID1346893Human 5-HT2C receptor (5-Hydroxytryptamine receptors)
AID1336358Displacement of [3H]mesulergine from human recombinant 5HT2C receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
AID751850Binding affinity to human 5-HT2C receptor by radioligand displacement assay2013European journal of medicinal chemistry, May, Volume: 63Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
AID1196330Displacement of [3H]mesulergine from human 5-HT2C receptor expressed in HEK-293 cells2015European journal of medicinal chemistry, Mar-06, Volume: 92Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.
AID1285659Displacement of [3H]mesuleregine from human recombinant 5-HT2C receptor expressed in HEK293 cells2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
AID1152684Displacement of [3H]mesulergine from human recombinant 5-HT2C receptor expressed in HEK293 cells2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia.
AID346455Displacement of radiolabeled RS 102221 from human 5HT2C receptor2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.
AID752214Binding affinity to human 5-HT2C receptor by radioligand displacement assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (20.00)29.6817
2010's6 (60.00)24.3611
2020's2 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.73

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 Index17.73 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index5.03 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.73)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]