The compound you described, 1-[1-[[1-[(4-methylphenyl)methyl]-5-tetrazolyl]methyl]-4-piperidinyl]-5-(trifluoromethyl)benzotriazole, is a **highly selective and potent inverse agonist of the histamine H4 receptor**.
Here's why it is important for research:
* **Histamine H4 Receptor:** This receptor plays a crucial role in various biological processes, including inflammation, allergic responses, and immune system regulation. It has been implicated in diseases such as asthma, rheumatoid arthritis, and inflammatory bowel disease.
* **Inverse Agonism:** Unlike regular agonists that activate a receptor, inverse agonists actually decrease the receptor's activity, often to a level below its baseline activity.
* **Selective Target:** The compound is highly specific to the H4 receptor, meaning it does not significantly interact with other histamine receptors (H1, H2, and H3). This selectivity is crucial for research because it allows scientists to study the specific functions of the H4 receptor without confounding effects from other receptors.
* **Potential Therapeutic Applications:** The selective and potent nature of this compound makes it a valuable tool for drug discovery and development. By targeting the H4 receptor, researchers can explore its potential for treating a wide range of inflammatory and allergic conditions.
**Research applications include:**
* **Understanding the role of the H4 receptor in disease pathogenesis.**
* **Developing new drugs for inflammatory and allergic disorders.**
* **Testing the efficacy of H4 receptor antagonists in animal models of disease.**
In summary, 1-[1-[[1-[(4-methylphenyl)methyl]-5-tetrazolyl]methyl]-4-piperidinyl]-5-(trifluoromethyl)benzotriazole is a valuable research tool due to its highly selective inverse agonist activity against the H4 receptor, a key player in various biological processes. Its potent and specific action opens doors for exploring the therapeutic potential of targeting this receptor in a wide range of inflammatory and allergic diseases.
ID Source | ID |
---|---|
PubMed CID | 652795 |
CHEMBL ID | 1338416 |
CHEBI ID | 112786 |
Synonym |
---|
1-{1-[1-(4-methyl-benzyl)-1h-tetrazol-5-ylmethyl]-piperidin-4-yl}-5-trifluoromethyl-1h-benzotriazole |
MLS000881272 |
smr000006487 |
MLS000033672 |
CHEBI:112786 |
AKOS000743201 |
1-[1-[[1-[(4-methylphenyl)methyl]tetrazol-5-yl]methyl]piperidin-4-yl]-5-(trifluoromethyl)benzotriazole |
HMS2359C13 |
CHEMBL1338416 |
Q27193157 |
1-[1-[[1-[(4-methylphenyl)methyl]-5-tetrazolyl]methyl]-4-piperidinyl]-5-(trifluoromethyl)benzotriazole |
Class | Description |
---|---|
benzotriazoles | |
[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 | 7.6921 | 0.0447 | 17.8581 | 100.0000 | AID485294; AID485341 |
Chain A, Cruzipain | Trypanosoma cruzi | Potency | 19.9526 | 0.0020 | 14.6779 | 39.8107 | AID1476 |
acid sphingomyelinase | Homo sapiens (human) | Potency | 112.2020 | 14.1254 | 24.0613 | 39.8107 | AID504937 |
glp-1 receptor, partial | Homo sapiens (human) | Potency | 10.0000 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 23.1093 | 0.0041 | 10.8903 | 31.5287 | AID504467 |
TDP1 protein | Homo sapiens (human) | Potency | 19.4763 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
Microtubule-associated protein tau | Homo sapiens (human) | Potency | 10.0000 | 0.1800 | 13.5574 | 39.8107 | AID1460 |
aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 22.3872 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 19.9526 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
IDH1 | Homo sapiens (human) | Potency | 29.0929 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
lysosomal alpha-glucosidase preproprotein | Homo sapiens (human) | Potency | 44.6684 | 0.0366 | 19.6376 | 50.1187 | AID1466; AID2242 |
chromobox protein homolog 1 | Homo sapiens (human) | Potency | 79.4328 | 0.0060 | 26.1688 | 89.1251 | AID540317 |
mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 10.0000 | 0.0398 | 16.7842 | 39.8107 | AID995 |
ubiquitin carboxyl-terminal hydrolase 2 isoform a | Homo sapiens (human) | Potency | 3.9811 | 0.6561 | 9.4520 | 25.1189 | AID927 |
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 75.6863 | 0.4256 | 12.0591 | 28.1838 | AID504891 |
geminin | Homo sapiens (human) | Potency | 29.0929 | 0.0046 | 11.3741 | 33.4983 | AID624297 |
neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 10.0000 | 0.0158 | 12.3113 | 615.5000 | AID1461 |
Neuronal acetylcholine receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 44.6684 | 3.5481 | 18.0395 | 35.4813 | AID1466 |
Neuronal acetylcholine receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 44.6684 | 3.5481 | 18.0395 | 35.4813 | AID1466 |
Disintegrin and metalloproteinase domain-containing protein 17 | Homo sapiens (human) | Potency | 3.9811 | 1.5849 | 13.0043 | 25.1189 | AID927 |
TAR DNA-binding protein 43 | Homo sapiens (human) | Potency | 19.9526 | 1.7783 | 16.2081 | 35.4813 | AID652104 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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 | |||
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
[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] |