Page last updated: 2024-11-07

sr 140333

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

Description

SR 140333: SR-140603 is the (R)-antipode of SR-140333; a neurokinin-1 receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID108166
CHEMBL ID38763
SCHEMBL ID1650319
MeSH IDM0226243

Synonyms (25)

Synonym
1-azoniabicyclo(2.2.2)octane, 1-(2-(3-(3,4-dichlorophenyl)-1-((3-(1-methylethoxy)phenyl)acetyl)-3-piperidinyl)ethyl)-4-phenyl-, chloride, (s)-
sr 140,333
153050-21-6
1-(2-(3-(3,4-dichlorophenyl)-1-(3-isopropoxyphenylacetyl)piperidin-3-yl)ethyl)-4-phenyl-1-azabicyclo(2.2.2)octane chloride
sr 140333
sr-140,333
CHEMBL38763 ,
nolpitantium chloride
22o6xi63e0 ,
sr 140333a
unii-22o6xi63e0
1-azoniabicyclo(2.2.2)octane, 1-(2-((3s)-3-(3,4-dichlorophenyl)-1-(2-(3-(1-methylethoxy)phenyl)acetyl)-3-piperidinyl)ethyl)-4-phenyl-, chloride (1:1)
sr-140333a
SCHEMBL1650319
1-[2-[(3s)-3-(3,4-dichlorophenyl)-1-[2-[3-(1-methylethoxy)phenyl]acetyl]-3-piperidinyl]ethyl]-4-phenyl-1-azoniabicyclo[2.2.2]octane chloride
AKOS024457927
(s)1-(2-[3-(3,4-dichlorophenyl)-1-(3-isopropoxyphenylacetyl)piperidin-3-yl] ethyl)-4-phenyl-1-azoniabicyclo [2.2.2]octane chloride
1-{2-[3-(3,4-dichlorophenyl)-1-({3-[(propan-2-yl)oxy]phenyl}acetyl)piperidin-3-yl]ethyl}-4-phenyl-1-azabicyclo[2.2.2]octan-1-ium chloride
DTXSID60934670
1-[(3s)-3-(3,4-dichlorophenyl)-3-[2-(4-phenyl-1-azoniabicyclo[2.2.2]octan-1-yl)ethyl]piperidin-1-yl]-2-(3-propan-2-yloxyphenyl)ethanone;chloride
Q27253664
CS-0028928
HY-108479
(s)-1-(2-(3-(3,4-dichlorophenyl)-1-(2-(3-isopropoxyphenyl)acetyl)piperidin-3-yl)ethyl)-4-phenylquinuclidin-1-ium chloride
1-{2-[(3s)-3-(3,4-dichlorophenyl)-1-{2-[3-(propan-2-yloxy)phenyl]acetyl}piperidin-3-yl]ethyl}-4-phenyl-1-azabicyclo[2.2.2]octan-1-ium chloride

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"5-fold higher than in wild-type mice, suggesting increased bioavailability of SP."( Neutral endopeptidase (EC 3.4.24.11) terminates colitis by degrading substance P.
Barbara, G; Bunnett, NW; Collins, SM; Figini, M; Geppetti, P; Gerard, C; Gerard, N; Grady, EF; Qiu, B; Sturiale, S, 1999
)
0.3
" Although SR 140 333 increased the absorption rate from the jejunum in animals infused intra-arterially with 5-HT, 5-HT itself did not cause a significant reduction in absorption."( Effects of tachykinins and 5-hydroxytryptamine on intestinal secretion.
Coupar, IM; Di Iulio, JL, 2003
)
0.32

Dosage Studied

ExcerptRelevanceReference
" Airway hyperresponsiveness was evidenced by significant shifts to the left of dose-response curves for intravenous acetylcholine (ACh) without a change in maximum responses to ACh."( The tachykinin NK2 receptor antagonist SR 48968 inhibits citric acid-induced airway hyperresponsiveness in guinea pigs.
Advenier, C; Emonds-Alt, X; Girard, V; Yavo, JC, 1996
)
0.29
[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 receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.00000.00002.751810.0000AID145488
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (1)

Assay IDTitleYearJournalArticle
AID145488Neurokinin (NK1) receptor antagonistic activity was evaluated.1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Synthesis and NK1 receptor antagonistic activity of (+/-)-1-acyl-3-(3,4- dichlorophenyl)-3-[2-(spiro-substituted piperidin-1'-yl)ethyl]piperidines.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (228)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's98 (42.98)18.2507
2000's114 (50.00)29.6817
2010's15 (6.58)24.3611
2020's1 (0.44)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 8.79

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

MetricThis Compound (vs All)
Research Demand Index8.79 (24.57)
Research Supply Index5.47 (2.92)
Research Growth Index4.25 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (8.79)

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%
Other236 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]