Page last updated: 2024-11-12

sr 142948a

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

Description

SR 142948A: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9940110
SCHEMBL ID7752965
MeSH IDM0272754

Synonyms (11)

Synonym
sr 142948a
CCG-221930
SCHEMBL7752965
2-[[5-(2,6-dimethoxyphenyl)-1-(4-(n-(3-dimethylaminopropyl)-n-methylcarbamoyl)-2-isopropylphenyl)-1h-pyrazole3-carbonyl]amino] adamantane-2-carboxylic acid hydrochloride
sr 142948 hydrochloride
sr 142948a, >=98% (hplc)
J-011800
2-(5-(2,6-dimethoxyphenyl)-1-(4-((3-(dimethylamino)propyl)(methyl)carbamoyl)-2-isopropylphenyl)-1h-pyrazole-3-carboxamido)adamantane-2-carboxylic acid hydrochloride
sr142948a hcl
sr142948a hydrochloride
AKOS040749555

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" In contrast, APD-induced Fos expression increases in the caudate-putamen (CPu) and prefrontal cortex (PFC) are associated with the extrapyramidal side effect liability of typical APDs or the effectiveness against negative symptoms of atypical APDs, respectively."( Neurotensin receptor antagonist SR 142948A alters Fos expression and extrapyramidal side effect profile of typical and atypical antipsychotic drugs.
Binder, EB; Kinkead, B; Nemeroff, CB; Owens, MJ, 2004
)
0.61

Dosage Studied

ExcerptRelevanceReference
" We also provide evidence of deficient NT neurotransmission as well as a left-shifted antipsychotic drug dose-response curve in isolation-reared rats."( Enhanced neurotensin neurotransmission is involved in the clinically relevant behavioral effects of antipsychotic drugs: evidence from animal models of sensorimotor gating.
Binder, EB; Kilts, CD; Kinkead, B; Nemeroff, CB; Owens, MJ, 2001
)
0.31
[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)
Neurotensin receptor type 1Homo sapiens (human)IC50 (µMol)0.01690.00020.00730.0820AID1061657; AID772297; AID772308
[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)
Neurotensin receptor type 1Homo sapiens (human)EC50 (µMol)45.00000.00000.573610.0000AID1061686; AID772307
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (24)

Processvia Protein(s)Taxonomy
positive regulation of gene expressionNeurotensin receptor type 1Homo sapiens (human)
temperature homeostasisNeurotensin receptor type 1Homo sapiens (human)
negative regulation of systemic arterial blood pressureNeurotensin receptor type 1Homo sapiens (human)
regulation of membrane depolarizationNeurotensin receptor type 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayNeurotensin receptor type 1Homo sapiens (human)
neuropeptide signaling pathwayNeurotensin receptor type 1Homo sapiens (human)
chemical synaptic transmissionNeurotensin receptor type 1Homo sapiens (human)
learningNeurotensin receptor type 1Homo sapiens (human)
adult locomotory behaviorNeurotensin receptor type 1Homo sapiens (human)
positive regulation of glutamate secretionNeurotensin receptor type 1Homo sapiens (human)
positive regulation of gamma-aminobutyric acid secretionNeurotensin receptor type 1Homo sapiens (human)
response to lipidNeurotensin receptor type 1Homo sapiens (human)
positive regulation of apoptotic processNeurotensin receptor type 1Homo sapiens (human)
negative regulation of apoptotic processNeurotensin receptor type 1Homo sapiens (human)
regulation of respiratory gaseous exchangeNeurotensin receptor type 1Homo sapiens (human)
detection of temperature stimulus involved in sensory perception of painNeurotensin receptor type 1Homo sapiens (human)
negative regulation of release of sequestered calcium ion into cytosolNeurotensin receptor type 1Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolNeurotensin receptor type 1Homo sapiens (human)
positive regulation of inositol phosphate biosynthetic processNeurotensin receptor type 1Homo sapiens (human)
D-aspartate import across plasma membraneNeurotensin receptor type 1Homo sapiens (human)
inositol phosphate catabolic processNeurotensin receptor type 1Homo sapiens (human)
positive regulation of arachidonic acid secretionNeurotensin receptor type 1Homo sapiens (human)
positive regulation of inhibitory postsynaptic potentialNeurotensin receptor type 1Homo sapiens (human)
L-glutamate import across plasma membraneNeurotensin receptor type 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
G protein-coupled receptor activityNeurotensin receptor type 1Homo sapiens (human)
protein bindingNeurotensin receptor type 1Homo sapiens (human)
G protein-coupled neurotensin receptor activityNeurotensin receptor type 1Homo sapiens (human)
identical protein bindingNeurotensin receptor type 1Homo sapiens (human)
protein-containing complex bindingNeurotensin receptor type 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (11)

Processvia Protein(s)Taxonomy
endoplasmic reticulumNeurotensin receptor type 1Homo sapiens (human)
Golgi apparatusNeurotensin receptor type 1Homo sapiens (human)
plasma membraneNeurotensin receptor type 1Homo sapiens (human)
cytoplasmic side of plasma membraneNeurotensin receptor type 1Homo sapiens (human)
cell surfaceNeurotensin receptor type 1Homo sapiens (human)
symmetric synapseNeurotensin receptor type 1Homo sapiens (human)
terminal boutonNeurotensin receptor type 1Homo sapiens (human)
dendritic spineNeurotensin receptor type 1Homo sapiens (human)
dendritic shaftNeurotensin receptor type 1Homo sapiens (human)
perikaryonNeurotensin receptor type 1Homo sapiens (human)
membrane raftNeurotensin receptor type 1Homo sapiens (human)
plasma membraneNeurotensin receptor type 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (7)

Assay IDTitleYearJournalArticle
AID772297Antagonist activity at NTR1 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin assessed as inhibition of ML314-induced effect by GFP reporter gene assay2013ACS medicinal chemistry letters, Jul-20, Volume: 4, Issue:9
Discovery of ML314, a Brain Penetrant Non-Peptidic β-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.
AID1061686Agonist activity at NTR1 in human U2OS cells after 1 hr by beta-arrestin GFP reporter gene assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Imidazole-derived agonists for the neurotensin 1 receptor.
AID772307Agonist activity at NTR1 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin by GFP reporter gene assay2013ACS medicinal chemistry letters, Jul-20, Volume: 4, Issue:9
Discovery of ML314, a Brain Penetrant Non-Peptidic β-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.
AID1061657Displacement of [125I]-neurotensin from NTR1 (unknown origin)2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Imidazole-derived agonists for the neurotensin 1 receptor.
AID772308Displacement of [125I]-neurotensin from NTR1 in HUVEC after 1 hr by gamma counting analysis2013ACS medicinal chemistry letters, Jul-20, Volume: 4, Issue:9
Discovery of ML314, a Brain Penetrant Non-Peptidic β-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (34)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's8 (23.53)18.2507
2000's19 (55.88)29.6817
2010's5 (14.71)24.3611
2020's2 (5.88)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.90

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 Index10.90 (24.57)
Research Supply Index3.56 (2.92)
Research Growth Index4.46 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.90)

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%
Other34 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]