The compound you've described, **1-[(5,7-dimethyl-3-pyrazolo[1,5-a]pyrimidinyl)-oxomethyl]-4-piperidinecarboxylic acid ethyl ester**, is a synthetic molecule that has been shown to exhibit **potent and selective activity as a PDE4 inhibitor**.
**Here's what makes it important for research:**
* **PDE4 inhibition:** This compound specifically inhibits phosphodiesterase 4 (PDE4), an enzyme that breaks down cyclic AMP (cAMP). cAMP is a crucial intracellular messenger involved in various cellular processes, including inflammation, immune responses, and neuronal signaling.
* **Therapeutic potential:** By inhibiting PDE4, this compound can increase cAMP levels, which may lead to therapeutic benefits in various conditions, including:
* **Asthma:** PDE4 inhibitors are already used as effective treatments for asthma, by reducing airway inflammation and bronchospasm.
* **Chronic obstructive pulmonary disease (COPD):** PDE4 inhibitors are being investigated for their potential to improve lung function and reduce inflammation in COPD.
* **Neurological disorders:** PDE4 inhibitors have shown promise in treating conditions like Alzheimer's disease and Parkinson's disease by promoting neuroprotection and enhancing cognitive function.
* **Inflammation:** PDE4 inhibition may help suppress inflammatory responses in various inflammatory conditions.
* **Depression:** PDE4 inhibitors are being explored for their potential antidepressant effects by increasing cAMP levels in the brain.
* **Research tool:** This compound serves as a valuable research tool to investigate the role of PDE4 in various biological processes and to identify new drug candidates for various therapeutic applications.
**Overall, this compound is important for research due to its potent PDE4 inhibitory activity, its potential therapeutic value in a wide range of conditions, and its utility as a research tool for studying the biological functions of PDE4.**
**Note:** This compound is still under investigation, and further research is needed to fully understand its safety and efficacy in humans.
ID Source | ID |
---|---|
PubMed CID | 3244226 |
CHEMBL ID | 1439331 |
CHEBI ID | 105638 |
Synonym |
---|
OPREA1_803054 |
smr000021483 |
ethyl 1-[(5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)carbonyl]piperidine-4-carboxylate |
MLS000044072 |
EU-0053628 |
ethyl 1-(5,7-dimethylpyrazolo[1,5-a]pyrimidine-3-carbonyl)piperidine-4-carboxylate |
HMS2321D17 |
CCG-26113 |
CHEMBL1439331 |
Q27183394 |
1-[(5,7-dimethyl-3-pyrazolo[1,5-a]pyrimidinyl)-oxomethyl]-4-piperidinecarboxylic acid ethyl ester |
SR-01000540590-1 |
sr-01000540590 |
CHEBI:105638 |
Z316151036 |
Class | Description |
---|---|
pyrazolopyrimidine | |
[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, HADH2 protein | Homo sapiens (human) | Potency | 22.5358 | 0.0251 | 20.2376 | 39.8107 | AID886; AID893 |
Chain B, HADH2 protein | Homo sapiens (human) | Potency | 22.5358 | 0.0251 | 20.2376 | 39.8107 | AID886; AID893 |
Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 31.6228 | 0.1778 | 14.3909 | 39.8107 | AID2147 |
thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 0.1000 | 20.8793 | 79.4328 | AID588456 |
ClpP | Bacillus subtilis | Potency | 31.6228 | 1.9953 | 22.6730 | 39.8107 | AID651965 |
aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 39.8107 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 28.1838 | 0.0018 | 15.6638 | 39.8107 | AID894 |
DNA polymerase eta isoform 1 | Homo sapiens (human) | Potency | 0.7079 | 0.1000 | 28.9256 | 213.3130 | AID588591 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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 | |||
[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] |