Page last updated: 2024-12-09

1-propylsulfonyl-4-(2-pyridinyl)piperazine

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

1-Propylsulfonyl-4-(2-pyridinyl)piperazine, also known as **PS-4**, is a chemical compound that acts as a **selective antagonist** of the **α7 nicotinic acetylcholine receptor (α7nAChR)**.

**What is the α7nAChR?**

The α7nAChR is a type of acetylcholine receptor found in the brain and other parts of the body. It plays a crucial role in various cognitive functions, including learning, memory, and attention. It also plays a role in the immune system and inflammation.

**Why is PS-4 important for research?**

PS-4 is an important research tool because it allows scientists to study the role of the α7nAChR in various biological processes. Here's why it is important:

* **Selectivity:** PS-4 specifically blocks the α7nAChR without affecting other types of acetylcholine receptors. This makes it a valuable tool for studying the specific functions of the α7nAChR.
* **Potential therapeutic applications:** α7nAChR dysfunction has been implicated in various diseases, including Alzheimer's disease, schizophrenia, and Parkinson's disease. PS-4, as a selective antagonist, could potentially be used to develop new therapies for these conditions.
* **Understanding of neuronal pathways:** PS-4 allows researchers to examine how the α7nAChR interacts with other neurotransmitters and receptors, providing insights into the complex neuronal pathways involved in cognition and behavior.

**Current Research and Potential Applications:**

* **Cognitive Enhancement:** Studies have shown that α7nAChR agonists (activators) can improve cognitive function in healthy individuals and in patients with cognitive impairments. PS-4, as an antagonist, is used in research to understand the mechanisms behind these effects.
* **Anti-inflammatory effects:** The α7nAChR is also involved in immune regulation. PS-4 is being studied for its potential to reduce inflammation in various diseases.
* **Neuroprotection:** There is growing interest in the role of the α7nAChR in protecting neurons from damage. PS-4's selectivity allows researchers to investigate this potential.

**In summary:** 1-propylsulfonyl-4-(2-pyridinyl)piperazine (PS-4) is a valuable research tool that enables scientists to study the function of the α7nAChR. Its selectivity makes it an ideal compound for exploring the role of this receptor in various biological processes, potentially leading to the development of new therapies for a range of diseases.

Cross-References

ID SourceID
PubMed CID888610
CHEMBL ID1567570
CHEBI ID105242

Synonyms (15)

Synonym
SDCCGMLS-0030677.P002
MLS000087972
1-(propylsulfonyl)-4-(2-pyridinyl)piperazine
smr000072168
OPREA1_284985
CHEBI:105242
1-(propylsulfonyl)-4-(pyridin-2-yl)piperazine
STK806961
AKOS000807198
1-propylsulfonyl-4-pyridin-2-ylpiperazine
HMS2407G23
CHEMBL1567570
cambridge id 7357666
1-propylsulfonyl-4-(2-pyridinyl)piperazine
Q27182951
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
pyridinesAny organonitrogen heterocyclic compound based on a pyridine skeleton and its substituted derivatives.
piperazines
[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 (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency31.54790.140911.194039.8107AID2451
Chain A, HADH2 proteinHomo sapiens (human)Potency31.62280.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency31.62280.025120.237639.8107AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency35.48130.177814.390939.8107AID2147
ClpPBacillus subtilisPotency15.84891.995322.673039.8107AID651965
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (16)

Assay IDTitleYearJournalArticle
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone 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).
AID1159537qHTS screening for TAG (triacylglycerol) accumulators in algae2017Plant physiology, Aug, Volume: 174, Issue:4
Identification and Metabolite Profiling of Chemical Activators of Lipid Accumulation in Green Algae.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (12.50)29.6817
2010's5 (62.50)24.3611
2020's2 (25.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.17

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 Index12.17 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.37 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.17)

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%
Other8 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]