Page last updated: 2024-12-09

1-(2,5-dimethoxyphenyl)sulfonyl-4-(phenylmethyl)piperazine

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

1-(2,5-dimethoxyphenyl)sulfonyl-4-(phenylmethyl)piperazine, also known as **WAY-100635**, is a **selective antagonist** of the **5-HT1A receptor**.

**What are 5-HT1A receptors?**

5-HT1A receptors are a type of serotonin receptor found in the brain. They play a role in regulating mood, anxiety, sleep, appetite, and other functions.

**What is a selective antagonist?**

An antagonist is a drug that blocks the action of a neurotransmitter, in this case, serotonin. A selective antagonist specifically targets a particular receptor type, like the 5-HT1A receptor in the case of WAY-100635.

**Why is WAY-100635 important for research?**

WAY-100635 has been a valuable tool for researchers studying the role of 5-HT1A receptors in various conditions, including:

* **Anxiety and depression:** By blocking the 5-HT1A receptor, WAY-100635 can help researchers understand how these receptors contribute to anxiety and depression.
* **Sleep disorders:** 5-HT1A receptors are involved in sleep regulation. WAY-100635 has been used to study the role of these receptors in sleep disorders like insomnia.
* **Neurological disorders:** 5-HT1A receptors are also implicated in neurological disorders like Parkinson's disease and Alzheimer's disease. WAY-100635 has helped researchers investigate the potential therapeutic benefits of targeting these receptors in these conditions.

**Other important uses of WAY-100635:**

* **Pharmacology research:** WAY-100635 is used to investigate the mechanisms of action of other drugs that target the 5-HT1A receptor.
* **Drug development:** WAY-100635 has served as a template for developing new drugs that target the 5-HT1A receptor for the treatment of various mental and neurological conditions.

Overall, WAY-100635 has been an important tool for understanding the role of the 5-HT1A receptor in various biological processes and for developing potential new treatments for a variety of disorders.

Cross-References

ID SourceID
PubMed CID1106577
CHEMBL ID1603822
CHEBI ID111356

Synonyms (25)

Synonym
MS-10549
1-benzyl-4-(2,5-dimethoxy-benzenesulfonyl)-piperazine
OPREA1_744562
OPREA1_056099
smr000515389
MLS001211423
CHEBI:111356
AKOS000595449
1-benzyl-4-(2,5-dimethoxyphenyl)sulfonylpiperazine
HMS2823M11
F0376-0330
1-benzyl-4-((2,5-dimethoxyphenyl)sulfonyl)piperazine
332021-08-6
1-((2,5-dimethoxyphenyl)sulfonyl)-4-benzylpiperazine
AB00096634-01
Z45509673
1-benzyl-4-(2,5-dimethoxybenzenesulfonyl)piperazine
cambridge id 5784415
CHEMBL1603822
1-(2,5-dimethoxyphenyl)sulfonyl-4-(phenylmethyl)piperazine
Q27191012
mfcd01173058
1-[(2,5-dimethoxyphenyl)sulfonyl]-4-(phenylmethyl)piperazine
DTXSID501183541
piperazine, 1-[(2,5-dimethoxyphenyl)sulfonyl]-4-(phenylmethyl)-
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
sulfonamideAn amide of a sulfonic acid RS(=O)2NR'2.
[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)
TDP1 proteinHomo sapiens (human)Potency18.35640.000811.382244.6684AID686978
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency31.62280.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency31.62280.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency31.62280.15855.287912.5893AID540303
Guanine nucleotide-binding protein GHomo sapiens (human)Potency28.18381.995325.532750.1187AID624287
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (5)

Processvia Protein(s)Taxonomy
negative regulation of inflammatory response to antigenic stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
renal water homeostasisGuanine nucleotide-binding protein GHomo sapiens (human)
G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein GHomo sapiens (human)
regulation of insulin secretionGuanine nucleotide-binding protein GHomo sapiens (human)
cellular response to glucagon stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (2)

Processvia Protein(s)Taxonomy
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (15)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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 (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]