Page last updated: 2024-12-10

(4-benzoyl-1-methyl-3-pyrrolidinyl)-phenylmethanone

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

(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.

Cross-References

ID SourceID
PubMed CID4269490
CHEMBL ID1416229
CHEBI ID115553

Synonyms (15)

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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic ketoneA 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 Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Ferritin light chainEquus caballus (horse)Potency39.81075.623417.292931.6228AID485281
glp-1 receptor, partialHomo sapiens (human)Potency28.18380.01846.806014.1254AID624417
BRCA1Homo sapiens (human)Potency22.38720.89137.722525.1189AID624202
ATAD5 protein, partialHomo sapiens (human)Potency6.51310.004110.890331.5287AID504467
TDP1 proteinHomo sapiens (human)Potency18.35640.000811.382244.6684AID686978
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency10.00000.28189.721235.4813AID2326
P53Homo sapiens (human)Potency56.23410.07319.685831.6228AID504706
chromobox protein homolog 1Homo sapiens (human)Potency35.48130.006026.168889.1251AID540317
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. 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.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. 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.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. 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.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay 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]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (20.00)29.6817
2010's3 (60.00)24.3611
2020's1 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.56

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.

MetricThis Compound (vs All)
Research Demand Index12.56 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.56)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]