The compound you described, **1-[(3,4-dimethoxyphenyl)-[1-(thiophen-2-ylmethyl)-5-tetrazolyl]methyl]-4-phenylpiperazine**, is a **selective antagonist** for **histamine H4 receptors**.
Here's why it's important for research:
* **Histamine H4 receptors (H4R)** are a relatively new target in pharmacology, discovered in the late 1990s. They are found in various immune cells like mast cells, eosinophils, and neutrophils, and play a role in various inflammatory and allergic conditions.
* **H4R antagonists** like this compound have the potential to be useful in treating:
* **Allergic diseases:** such as asthma, allergic rhinitis, and atopic dermatitis, by modulating the immune response.
* **Inflammatory diseases:** such as inflammatory bowel disease (IBD) and rheumatoid arthritis, by reducing inflammation.
* **Other conditions:** such as pain, sleep disorders, and neurodegenerative diseases.
**Research on this compound and other H4R antagonists aims to:**
* **Understand the role of H4R in various disease processes:** by studying the effects of these compounds in different models of disease.
* **Develop new drugs for the treatment of these diseases:** by optimizing the efficacy and safety of H4R antagonists.
**Note:** It's important to remember that this compound is still under research and has not been approved for any medical use.
**Further research on this compound and other H4R antagonists is ongoing, and it holds promise for the development of new therapies for a range of diseases.**
ID Source | ID |
---|---|
PubMed CID | 655875 |
CHEMBL ID | 1594858 |
CHEBI ID | 116449 |
Synonym |
---|
OPREA1_813685 |
MLS000882455 |
smr000005056 |
MLS000032507 |
1-[(3,4-dimethoxy-phenyl)-(1-thiophen-2-ylmethyl-1h-tetrazol-5-yl)-methyl]-4-phenyl-piperazine |
CHEBI:116449 |
AKOS000791539 |
1-[(3,4-dimethoxyphenyl)-[1-(thiophen-2-ylmethyl)tetrazol-5-yl]methyl]-4-phenylpiperazine |
AKOS024310344 |
HMS2342H10 |
CHEMBL1594858 |
Q27199334 |
1-[(3,4-dimethoxyphenyl)-[1-(thiophen-2-ylmethyl)-5-tetrazolyl]methyl]-4-phenylpiperazine |
Class | Description |
---|---|
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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 28.1838 | 0.0447 | 17.8581 | 100.0000 | AID485341 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 23.1093 | 0.0041 | 10.8903 | 31.5287 | AID504467 |
TDP1 protein | Homo sapiens (human) | Potency | 35.4813 | 0.0008 | 11.3822 | 44.6684 | AID686978 |
TSHR protein | Homo sapiens (human) | Potency | 16.9441 | 0.3381 | 19.0466 | 37.9330 | AID602292 |
thioredoxin glutathione reductase | Schistosoma mansoni | Potency | 44.6684 | 0.1000 | 22.9075 | 100.0000 | AID485364 |
apical membrane antigen 1, AMA1 | Plasmodium falciparum 3D7 | Potency | 25.1189 | 0.7079 | 12.1943 | 39.8107 | AID720542 |
aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 1.9953 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 12.5893 | 0.0013 | 18.0743 | 39.8107 | AID926; AID938 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 28.1838 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 12.5893 | 0.0158 | 12.3113 | 615.5000 | AID1461 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 1 (20.00) | 29.6817 |
2010's | 3 (60.00) | 24.3611 |
2020's | 1 (20.00) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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.
| This Compound (12.56) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 0 (0.00%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 5 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |