(4-Benzoyl-1-methyl-3-pyrrolidinyl)-phenylmethanone, also known as **Rolipram**, is a potent and selective inhibitor of **phosphodiesterase 4 (PDE4)**.
**PDE4** is an enzyme responsible for breaking down the second messenger **cyclic AMP (cAMP)**. cAMP plays a crucial role in various cellular processes, including inflammation, immune responses, and neuronal signaling.
**Rolipram's importance for research stems from its ability to inhibit PDE4 and thereby increase cAMP levels.** This property makes it a valuable tool for investigating the role of cAMP in various biological processes.
**Here are some key areas where Rolipram is important in research:**
* **Neurological disorders:** Rolipram has shown promise in preclinical studies for treating **depression, anxiety, and Alzheimer's disease**. This is due to its ability to enhance cAMP signaling in brain regions involved in mood regulation and memory.
* **Inflammation:** Rolipram can suppress **inflammatory responses** by inhibiting PDE4 in immune cells. This makes it a potential therapeutic target for inflammatory diseases like asthma and rheumatoid arthritis.
* **Cancer:** Some studies suggest that Rolipram might have **anti-cancer effects** by modulating cAMP signaling in cancer cells.
* **Other applications:** Rolipram is also used as a research tool to study **cellular signaling pathways**, **neurotransmitter release**, and **muscle contraction**.
**However, it's important to note that Rolipram has not yet been approved for clinical use in humans.** This is mainly due to its side effects, including nausea, vomiting, and headaches.
**Despite these limitations, Rolipram remains a valuable research tool and a promising therapeutic candidate for a range of diseases.** Further research is ongoing to explore its potential benefits and optimize its therapeutic use.
ID Source | ID |
---|---|
PubMed CID | 4269490 |
CHEMBL ID | 1416229 |
CHEBI ID | 115553 |
Synonym |
---|
(4-benzoyl-1-methyltetrahydro-1h-pyrrol-3-yl)(phenyl)methanone |
smr000179435 |
MLS000326890 , |
OPREA1_152427 |
CHEBI:115553 |
AKOS005096220 |
(4-benzoyl-1-methylpyrrolidin-3-yl)-phenylmethanone |
HMS2303O07 |
551921-53-0 |
6N-726 |
3,4-dibenzoyl-1-methylpyrrolidine |
CHEMBL1416229 |
(4-benzoyl-1-methyl-3-pyrrolidinyl)-phenylmethanone |
Q27197567 |
mfcd01871558 |
Class | Description |
---|---|
aromatic ketone | A ketone in which the carbonyl group is attached to an aromatic ring. |
[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, Ferritin light chain | Equus caballus (horse) | Potency | 39.8107 | 5.6234 | 17.2929 | 31.6228 | AID485281 |
glp-1 receptor, partial | Homo sapiens (human) | Potency | 28.1838 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
BRCA1 | Homo sapiens (human) | Potency | 22.3872 | 0.8913 | 7.7225 | 25.1189 | AID624202 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 6.5131 | 0.0041 | 10.8903 | 31.5287 | AID504467 |
TDP1 protein | Homo sapiens (human) | Potency | 18.3564 | 0.0008 | 11.3822 | 44.6684 | AID686978 |
nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 10.0000 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
P53 | Homo sapiens (human) | Potency | 56.2341 | 0.0731 | 9.6858 | 31.6228 | AID504706 |
chromobox protein homolog 1 | Homo sapiens (human) | Potency | 35.4813 | 0.0060 | 26.1688 | 89.1251 | AID540317 |
[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 | |||
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. |
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 | |||
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. |
[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] |