The compound you described, 1,3-dimethyl-8-[[methyl-(phenylmethyl)amino]methyl]-7-(2-methylpropyl)purine-2,6-dione, is a complex organic molecule with a rather long and unwieldy name. It's more commonly known as **rolipram**, a drug that has been studied extensively for its potential therapeutic benefits in various areas.
Here's why rolipram is important for research:
* **Antidepressant potential:** Rolipram is a potent and selective inhibitor of the enzyme **phosphodiesterase 4 (PDE4)**. PDE4 is responsible for breaking down cyclic AMP (cAMP), a crucial intracellular messenger molecule involved in various cellular processes, including mood regulation. By inhibiting PDE4, rolipram increases cAMP levels, which can lead to antidepressant effects. However, rolipram has not been widely approved for depression treatment due to side effects.
* **Neuroprotective effects:** Rolipram has shown promise in preclinical studies for treating neurodegenerative disorders like Alzheimer's disease. It can enhance cognitive function and protect neurons from damage by reducing inflammation and promoting nerve cell survival.
* **Anti-inflammatory properties:** PDE4 inhibition by rolipram also contributes to its anti-inflammatory effects. It has been investigated for its potential in treating inflammatory bowel disease, asthma, and other inflammatory conditions.
* **Treatment of addiction:** Rolipram has shown some effectiveness in reducing cravings for cocaine and alcohol in animal studies.
* **Research tool:** Rolipram's selective PDE4 inhibition makes it a valuable research tool to study the role of cAMP signaling in various biological processes.
**However, there are also challenges associated with rolipram's development as a therapeutic agent:**
* **Side effects:** Rolipram can cause nausea, vomiting, and headaches. Its use has been associated with gastrointestinal upset and potential for seizures.
* **Limited clinical studies:** Despite its promise, rolipram's clinical development has been limited, and its efficacy in human trials is still being evaluated.
Overall, rolipram remains an intriguing compound with potential for therapeutic applications. Continued research is needed to overcome its limitations and explore its full potential for treating a range of disorders.
ID Source | ID |
---|---|
PubMed CID | 3544833 |
CHEMBL ID | 1478289 |
CHEBI ID | 107046 |
Synonym |
---|
MLS000101908 , |
smr000016474 |
CHEBI:107046 |
AKOS001360895 |
8-[[benzyl(methyl)amino]methyl]-1,3-dimethyl-7-(2-methylpropyl)purine-2,6-dione |
8-{[benzyl(methyl)amino]methyl}-1,3-dimethyl-7-(2-methylpropyl)-3,7-dihydro-1h-purine-2,6-dione |
STK581194 |
HMS2237D19 |
HMS3366C05 |
CHEMBL1478289 |
1,3-dimethyl-8-[[methyl-(phenylmethyl)amino]methyl]-7-(2-methylpropyl)purine-2,6-dione |
Q27184945 |
sr-01000128488 |
SR-01000128488-1 |
8-((benzyl(methyl)amino)methyl)-7-isobutyl-1,3-dimethyl-3,7-dihydro-1h-purine-2,6-dione |
F0634-0620 |
Z235449710 |
Class | Description |
---|---|
oxopurine | |
[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 | 16.7006 | 0.0447 | 17.8581 | 100.0000 | AID485294; 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 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 20.5962 | 0.0041 | 10.8903 | 31.5287 | AID504467 |
TDP1 protein | Homo sapiens (human) | Potency | 6.9104 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
67.9K protein | Vaccinia virus | Potency | 5.0119 | 0.0001 | 8.4406 | 100.0000 | AID720579 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 31.6228 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 29.0929 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
parathyroid hormone/parathyroid hormone-related peptide receptor precursor | Homo sapiens (human) | Potency | 100.0000 | 3.5481 | 19.5427 | 44.6684 | AID743266 |
huntingtin isoform 2 | Homo sapiens (human) | Potency | 10.0000 | 0.0006 | 18.4198 | 1,122.0200 | AID1688 |
urokinase-type plasminogen activator precursor | Mus musculus (house mouse) | Potency | 10.0000 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
plasminogen precursor | Mus musculus (house mouse) | Potency | 10.0000 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
urokinase plasminogen activator surface receptor precursor | Mus musculus (house mouse) | Potency | 10.0000 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 12.5893 | 0.1259 | 12.2344 | 35.4813 | AID1458 |
caspase-1 isoform alpha precursor | Homo sapiens (human) | Potency | 39.8107 | 0.0003 | 11.4484 | 31.6228 | AID900 |
lamin isoform A-delta10 | Homo sapiens (human) | Potency | 19.9526 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
Caspase-7 | Homo sapiens (human) | Potency | 31.6228 | 3.9811 | 18.5856 | 31.6228 | AID889 |
Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 1.0000 | 1.9953 | 25.5327 | 50.1187 | AID624287 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Process | via Protein(s) | Taxonomy |
---|---|---|
RNA binding | Caspase-7 | Homo sapiens (human) |
aspartic-type endopeptidase activity | Caspase-7 | Homo sapiens (human) |
cysteine-type endopeptidase activity | Caspase-7 | Homo sapiens (human) |
protein binding | Caspase-7 | Homo sapiens (human) |
peptidase activity | Caspase-7 | Homo sapiens (human) |
cysteine-type peptidase activity | Caspase-7 | Homo sapiens (human) |
cysteine-type endopeptidase activity involved in apoptotic process | Caspase-7 | Homo sapiens (human) |
cysteine-type endopeptidase activity involved in execution phase of apoptosis | Caspase-7 | Homo sapiens (human) |
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 |
---|---|---|
extracellular space | Caspase-7 | Homo sapiens (human) |
nucleus | Caspase-7 | Homo sapiens (human) |
cytoplasm | Caspase-7 | Homo sapiens (human) |
cytosol | Caspase-7 | Homo sapiens (human) |
nucleus | Caspase-7 | Homo sapiens (human) |
nucleoplasm | Caspase-7 | Homo sapiens (human) |
cytosol | Caspase-7 | Homo sapiens (human) |
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 |
---|---|---|---|---|
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. |
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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 | |||
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. |
[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] |
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] |