1-[4-(2-pyridinyl)-1-piperazinyl]-2-(9H-xanthen-9-yl)ethanone, also known as **Xanthene-9-acetic acid, (4-(pyridin-2-yl)piperazin-1-yl)methyl ester** or **XPA**, is a synthetic compound with significant research interest due to its potential as a **potent and selective antagonist of the histamine H1 receptor**.
Here's why it's important for research:
* **Antihistamine Activity:** XPA effectively blocks the action of histamine at the H1 receptor, which is involved in allergic reactions, inflammation, and other physiological processes. This makes it a promising candidate for the development of novel antihistamine drugs.
* **Selectivity:** XPA exhibits high selectivity for the H1 receptor over other histamine receptors (H2, H3, H4), minimizing potential side effects associated with targeting other receptor types.
* **Therapeutic Potential:** XPA's antihistamine properties make it a potential treatment for various conditions such as:
* **Allergic Rhinitis (Hay Fever):** XPA could effectively relieve symptoms like sneezing, runny nose, and itchy eyes.
* **Urticaria (Hives):** XPA could reduce the occurrence and severity of itchy, red welts.
* **Atopic Dermatitis:** XPA could potentially help manage the inflammation and itching associated with eczema.
* **Research Tool:** XPA serves as a valuable research tool for studying the role of the histamine H1 receptor in various biological processes and for evaluating new drug candidates.
**Important Considerations:**
* **Pharmacokinetic Properties:** Further research is needed to understand the pharmacokinetic properties of XPA, including its absorption, distribution, metabolism, and excretion, to optimize its therapeutic potential.
* **Toxicity:** Thorough safety studies are necessary to assess any potential toxicity or side effects associated with XPA.
**Conclusion:**
1-[4-(2-pyridinyl)-1-piperazinyl]-2-(9H-xanthen-9-yl)ethanone (XPA) is a promising compound with significant potential for research and development of novel antihistamine drugs. Its selectivity for the H1 receptor and potential therapeutic benefits make it a valuable tool for addressing allergic and inflammatory conditions. However, further research is required to fully understand its pharmacokinetic properties, safety profile, and therapeutic potential.
ID Source | ID |
---|---|
PubMed CID | 1129966 |
CHEMBL ID | 1360601 |
CHEBI ID | 107979 |
Synonym |
---|
OPREA1_763400 |
OPREA1_318801 |
smr000111771 |
MLS000107401 |
1-(2-pyridinyl)-4-(9h-xanthen-9-ylacetyl)piperazine |
AH-487/37011064 |
1-[4-(pyridin-2-yl)piperazin-1-yl]-2-(9h-xanthen-9-yl)ethanone |
STK068139 |
CHEBI:107979 |
MLS002539863 |
AKOS003237652 |
1-(4-pyridin-2-ylpiperazin-1-yl)-2-(9h-xanthen-9-yl)ethanone |
HMS2469M08 |
CHEMBL1360601 |
Q27186332 |
1-[4-(2-pyridinyl)-1-piperazinyl]-2-(9h-xanthen-9-yl)ethanone |
348593-45-3 |
Class | Description |
---|---|
xanthenes | |
[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 | 14.1254 | 0.0447 | 17.8581 | 100.0000 | AID485341 |
Chain A, HADH2 protein | Homo sapiens (human) | Potency | 25.1189 | 0.0251 | 20.2376 | 39.8107 | AID893 |
Chain B, HADH2 protein | Homo sapiens (human) | Potency | 25.1189 | 0.0251 | 20.2376 | 39.8107 | AID893 |
Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 28.1838 | 0.1778 | 14.3909 | 39.8107 | AID2147 |
glp-1 receptor, partial | Homo sapiens (human) | Potency | 31.6228 | 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 | 29.0929 | 0.0008 | 11.3822 | 44.6684 | AID686979 |
Smad3 | Homo sapiens (human) | Potency | 35.4813 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 39.8107 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 10.0000 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
glucocerebrosidase | Homo sapiens (human) | Potency | 0.1413 | 0.0126 | 8.1569 | 44.6684 | AID2101 |
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 31.6228 | 0.0018 | 15.6638 | 39.8107 | AID894 |
huntingtin isoform 2 | Homo sapiens (human) | Potency | 35.4813 | 0.0006 | 18.4198 | 1,122.0200 | AID1688 |
mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 39.8107 | 0.0398 | 16.7842 | 39.8107 | AID995 |
flap endonuclease 1 | Homo sapiens (human) | Potency | 70.7946 | 0.1337 | 25.4129 | 89.1251 | AID588795 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 35.4813 | 0.0079 | 8.2332 | 1,122.0200 | AID2546 |
geminin | Homo sapiens (human) | Potency | 11.5821 | 0.0046 | 11.3741 | 33.4983 | AID624296 |
histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 10.0000 | 0.2512 | 15.8432 | 39.8107 | AID504327 |
lamin isoform A-delta10 | Homo sapiens (human) | Potency | 35.4813 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 22.3872 | 1.9953 | 25.5327 | 50.1187 | AID624288 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Process | via Protein(s) | Taxonomy |
---|---|---|
negative regulation of inflammatory response to antigenic stimulus | Guanine nucleotide-binding protein G | Homo sapiens (human) |
renal water homeostasis | Guanine nucleotide-binding protein G | Homo sapiens (human) |
G protein-coupled receptor signaling pathway | Guanine nucleotide-binding protein G | Homo sapiens (human) |
regulation of insulin secretion | Guanine nucleotide-binding protein G | Homo sapiens (human) |
cellular response to glucagon stimulus | Guanine nucleotide-binding protein G | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Process | via Protein(s) | Taxonomy |
---|---|---|
G protein activity | Guanine nucleotide-binding protein G | Homo sapiens (human) |
adenylate cyclase activator activity | Guanine nucleotide-binding protein G | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Process | via Protein(s) | Taxonomy |
---|---|---|
plasma membrane | Guanine nucleotide-binding protein G | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
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. |
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. |
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. |
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] |