Page last updated: 2024-12-11

1-cyclohexyl-3-[1-[4-(phenylmethyl)-1-piperazinyl]-1-thiophen-2-ylpropan-2-yl]urea

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

You're asking about a very specific compound, **1-cyclohexyl-3-[1-[4-(phenylmethyl)-1-piperazinyl]-1-thiophen-2-ylpropan-2-yl]urea**. This compound is a **potent and selective antagonist** of **cannabinoid receptor type 1 (CB1)**.

Here's why it's important for research:

* **Understanding the Cannabinoid System:** The endocannabinoid system (ECS) plays a vital role in regulating various physiological processes, including appetite, pain perception, mood, and memory. CB1 receptors are the primary targets of the ECS and are found throughout the central nervous system (CNS). By selectively blocking CB1, this compound helps researchers understand the specific roles of this receptor in different brain regions and their impact on behavior and disease.
* **Potential Therapeutic Applications:** CB1 antagonists are being investigated for potential therapeutic benefits in a range of conditions, including:
* **Obesity:** CB1 antagonists can reduce appetite and promote weight loss.
* **Addiction:** They can help reduce cravings and relapse in substance use disorders.
* **Pain Management:** CB1 antagonists can offer pain relief without the side effects of opioids.
* **Neurological Disorders:** Some research suggests their potential use in treating conditions like epilepsy and Parkinson's disease.

**Important Considerations:**

* **Safety Profile:** While promising, CB1 antagonists can have side effects, such as nausea, vomiting, and mood changes. Researchers are working to develop safer and more effective versions.
* **Drug Development:** The compound you mentioned is a research tool, and not currently an approved medication. More research is needed to evaluate its safety and efficacy for human use.

**In summary:** 1-cyclohexyl-3-[1-[4-(phenylmethyl)-1-piperazinyl]-1-thiophen-2-ylpropan-2-yl]urea is a valuable tool for researchers studying the cannabinoid system and its potential therapeutic applications. By selectively blocking CB1 receptors, it helps scientists unravel the complex mechanisms of the ECS and develop new drugs for treating various diseases.

Cross-References

ID SourceID
PubMed CID9550850
CHEMBL ID1518776
CHEBI ID112837

Synonyms (14)

Synonym
smr000127008
MLS000529983
CHEBI:112837
AKOS024593419
HMS2237F13
F0655-1147
892465-93-9
1-(1-(4-benzylpiperazin-1-yl)-1-(thiophen-2-yl)propan-2-yl)-3-cyclohexylurea
HMS3368L04
CHEMBL1518776
Q27193298
1-cyclohexyl-3-[1-[4-(phenylmethyl)-1-piperazinyl]-1-thiophen-2-ylpropan-2-yl]urea
3-[1-(4-benzylpiperazin-1-yl)-1-(thiophen-2-yl)propan-2-yl]-1-cyclohexylurea
1-[1-(4-benzylpiperazin-1-yl)-1-thiophen-2-ylpropan-2-yl]-3-cyclohexylurea
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic amineAn amino compound in which the amino group is linked directly to an aromatic system.
[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 (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency2.81840.044717.8581100.0000AID485294
glp-1 receptor, partialHomo sapiens (human)Potency31.62280.01846.806014.1254AID624417
TDP1 proteinHomo sapiens (human)Potency23.26260.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency28.18380.180013.557439.8107AID1460
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency10.00000.036619.637650.1187AID1466; AID2242
survival motor neuron protein isoform dHomo sapiens (human)Potency25.11890.125912.234435.4813AID1458
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency10.00003.548118.039535.4813AID1466
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Potency10.00003.548118.039535.4813AID1466
Guanine nucleotide-binding protein GHomo sapiens (human)Potency0.89131.995325.532750.1187AID624287
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency2.23871.000010.475628.1838AID1457
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (5)

Processvia Protein(s)Taxonomy
negative regulation of inflammatory response to antigenic stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
renal water homeostasisGuanine nucleotide-binding protein GHomo sapiens (human)
G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein GHomo sapiens (human)
regulation of insulin secretionGuanine nucleotide-binding protein GHomo sapiens (human)
cellular response to glucagon stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (2)

Processvia Protein(s)Taxonomy
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (13)

Assay IDTitleYearJournalArticle
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.
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.
AID1745845Primary 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.
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.
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
[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]