Page last updated: 2024-12-11

sr 142801

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

Description

SR 142801: SR 142806 is the (R)-enantiomer; structure given in first source; neurokinin-3 receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9808948
CHEMBL ID299377
SCHEMBL ID5679271
MeSH IDM0241765

Synonyms (12)

Synonym
bdbm50051290
n-(1-{3-[1-benzoyl-3-(3,4-dichloro-phenyl)-piperidin-3-yl]-propyl}-4-phenyl-piperidin-4-yl)-n-methyl-acetamide
sr 142801
CHEMBL299377 ,
L001511
FT-0689956
SCHEMBL5679271
sr-142801; sr142801; sr 142801
BCP27643
DTXSID70870070
n-(1-{3-[1-benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]propyl}-4-phenylpiperidin-4-yl)-n-methylacetamide
172734-92-8

Research Excerpts

Overview

SR 142801 was shown to be a potent uncompetitive antagonist of the senktide-induced formation of [3H]inositol monophosphate in slices from the guinea-pig ileum.

ExcerptReferenceRelevance
"SR 142801 was shown to be a potent uncompetitive antagonist of the senktide-induced formation of [3H]inositol monophosphate in slices from the guinea-pig ileum (apparent KB = 3.2 nM, 51% reduction of the maximal response), a functional test for tachykinin NK3 receptors."( Potency and selectivity of the tachykinin NK3 receptor antagonist SR 142801.
Beaujouan, JC; Glowinski, J; Saffroy, M; Torrens, Y, 1997
)
1.26

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic evaluation of SB 223412 in rat and dog indicated low plasma clearance, oral bioavailability and high and sustained plasma concentrations after 4 to 8 mg/kg oral dosages."( Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.
Brawner, ME; Elshourbagy, NA; Foley, JJ; Giardina, GA; Griswold, DE; Hay, DW; Martin, LD; Medhurst, AD; Potts, W; Sarau, HM; Schmidt, DB; Webb, EF, 1997
)
0.3

Bioavailability

ExcerptReferenceRelevance
" Pharmacokinetic evaluation of SB 223412 in rat and dog indicated low plasma clearance, oral bioavailability and high and sustained plasma concentrations after 4 to 8 mg/kg oral dosages."( Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.
Brawner, ME; Elshourbagy, NA; Foley, JJ; Giardina, GA; Griswold, DE; Hay, DW; Martin, LD; Medhurst, AD; Potts, W; Sarau, HM; Schmidt, DB; Webb, EF, 1997
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (124)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's49 (39.52)18.2507
2000's62 (50.00)29.6817
2010's12 (9.68)24.3611
2020's1 (0.81)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 9.42

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 Index9.42 (24.57)
Research Supply Index4.87 (2.92)
Research Growth Index4.28 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (9.42)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (1.57%)5.53%
Reviews3 (2.36%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other122 (96.06%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (3)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase 2A Randomized, Double-Blind, Placebo-Controlled, Dose-Ranging Study to Evaluate the Efficacy, Safety and Pharmacokinetics (PK) of ACER-801 for Treatment of Moderate to Severe Vasomotor Symptoms (VMS) Associated With Menopause [NCT05325775]Phase 1/Phase 249 participants (Actual)Interventional2022-03-30Completed
Pilot of Osanetant to Reduce Severity of Hot Flashes in Men With Adenocarcinoma of the Prostate (POSH-MAP) [NCT05647447]Early Phase 110 participants (Anticipated)Interventional2023-01-03Recruiting
Pilot of Osanetant to Reduce Testosterone in Men With Adenocarcinoma of the Prostate (PORT-MAP) [NCT05607342]Early Phase 110 participants (Anticipated)Interventional2023-01-03Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]