Page last updated: 2024-12-10

1-(2-chloro-4-nitrophenyl)-4-(2-methoxyphenyl)piperazine

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

1-(2-chloro-4-nitrophenyl)-4-(2-methoxyphenyl)piperazine is a chemical compound that is often referred to as **CP-101,606**. It is a potent and selective **dopamine D2 receptor antagonist**. This means it blocks the effects of dopamine, a neurotransmitter that plays a crucial role in many brain functions, including motivation, reward, and movement.

**Why is it important for research?**

CP-101,606 is important for research for several reasons:

* **Understanding dopamine function:** As a selective D2 antagonist, it is a valuable tool for investigating the role of dopamine in various neurological and psychiatric conditions.
* **Potential therapeutic applications:** Its ability to block dopamine signaling has led to investigations of its potential for treating conditions such as:
* **Schizophrenia:** Dopamine hyperactivity is thought to be involved in the symptoms of schizophrenia, and D2 antagonists like CP-101,606 have been studied as potential antipsychotic drugs.
* **Addiction:** Dopamine plays a key role in reward and addiction, and D2 antagonists like CP-101,606 have been investigated for their potential to reduce drug craving and relapse.
* **Parkinson's disease:** Although Parkinson's is primarily associated with dopamine depletion, some researchers have explored the use of D2 antagonists to manage certain symptoms.
* **Neurobiology research:** CP-101,606 is used in preclinical research to study the neurobiology of dopamine signaling, including its role in learning, memory, and movement.

**It is important to note:** CP-101,606 is not currently approved for any medical use. Research into its therapeutic potential is ongoing.

**Additionally:** CP-101,606 has also been studied for its effects on other neurotransmitter systems, including serotonin and norepinephrine. It is a complex compound with diverse pharmacological actions, making it a valuable tool for exploring the intricacies of the brain.

Cross-References

ID SourceID
PubMed CID4780145
CHEMBL ID1516552
CHEBI ID104889

Synonyms (14)

Synonym
HMS2583J09
MLS000417134 ,
smr000264366
CHEBI:104889
1-(2-chloro-4-nitrophenyl)-4-(2-methoxyphenyl)piperazine
AB00551983-02
1-(2-chloranyl-4-nitro-phenyl)-4-(2-methoxyphenyl)piperazine
cid_4780145
1-(2-chloro-4-nitro-phenyl)-4-(2-methoxyphenyl)piperazine
bdbm79697
CHEMBL1516552
Q27182555
Z31196017
AKOS034154001
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
piperazines
[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 (23)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency50.11870.631035.7641100.0000AID504339
glp-1 receptor, partialHomo sapiens (human)Potency2.81840.01846.806014.1254AID624417
ATAD5 protein, partialHomo sapiens (human)Potency7.30780.004110.890331.5287AID504467
TDP1 proteinHomo sapiens (human)Potency13.08160.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency8.91250.180013.557439.8107AID1460
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency22.38720.707912.194339.8107AID720542
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency17.78280.011212.4002100.0000AID1030
67.9K proteinVaccinia virusPotency2.66510.00018.4406100.0000AID720579; AID720580
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency7.94330.707936.904389.1251AID504333
IDH1Homo sapiens (human)Potency23.10930.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency3.16230.035520.977089.1251AID504332
chromobox protein homolog 1Homo sapiens (human)Potency22.38720.006026.168889.1251AID540317
mitogen-activated protein kinase 1Homo sapiens (human)Potency12.58930.039816.784239.8107AID1454
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency112.20200.050127.073689.1251AID588590
gemininHomo sapiens (human)Potency12.83210.004611.374133.4983AID624296; AID624297
survival motor neuron protein isoform dHomo sapiens (human)Potency22.38720.125912.234435.4813AID1458
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)Potency0.70790.058010.694926.6086AID602310
lamin isoform A-delta10Homo sapiens (human)Potency3.16230.891312.067628.1838AID1487
Guanine nucleotide-binding protein GHomo sapiens (human)Potency3.98111.995325.532750.1187AID624287
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cardiac alpha tropomyosinSus scrofa (pig)EC50 (µMol)71.48501.83002.37402.9180AID504698
troponin I, cardiac muscleHomo sapiens (human)EC50 (µMol)71.48501.83002.37402.9180AID504698
troponin T, cardiac muscle isoform 3Homo sapiens (human)EC50 (µMol)71.48501.83002.37402.9180AID504698
troponin C, slow skeletal and cardiac musclesHomo sapiens (human)EC50 (µMol)71.48501.83002.37402.9180AID504698
[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.
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
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.
AID1745845Primary 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]