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.
ID Source | ID |
---|---|
PubMed CID | 4780145 |
CHEMBL ID | 1516552 |
CHEBI ID | 104889 |
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 |
Class | Description |
---|---|
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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 50.1187 | 0.6310 | 35.7641 | 100.0000 | AID504339 |
glp-1 receptor, partial | Homo sapiens (human) | Potency | 2.8184 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 7.3078 | 0.0041 | 10.8903 | 31.5287 | AID504467 |
TDP1 protein | Homo sapiens (human) | Potency | 13.0816 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
Microtubule-associated protein tau | Homo sapiens (human) | Potency | 8.9125 | 0.1800 | 13.5574 | 39.8107 | AID1460 |
apical membrane antigen 1, AMA1 | Plasmodium falciparum 3D7 | Potency | 22.3872 | 0.7079 | 12.1943 | 39.8107 | AID720542 |
aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 17.7828 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
67.9K protein | Vaccinia virus | Potency | 2.6651 | 0.0001 | 8.4406 | 100.0000 | AID720579; AID720580 |
bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 7.9433 | 0.7079 | 36.9043 | 89.1251 | AID504333 |
IDH1 | Homo sapiens (human) | Potency | 23.1093 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 3.1623 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
chromobox protein homolog 1 | Homo sapiens (human) | Potency | 22.3872 | 0.0060 | 26.1688 | 89.1251 | AID540317 |
mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 12.5893 | 0.0398 | 16.7842 | 39.8107 | AID1454 |
DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 112.2020 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
geminin | Homo sapiens (human) | Potency | 12.8321 | 0.0046 | 11.3741 | 33.4983 | AID624296; AID624297 |
survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 22.3872 | 0.1259 | 12.2344 | 35.4813 | AID1458 |
DNA dC->dU-editing enzyme APOBEC-3G isoform 1 | Homo sapiens (human) | Potency | 0.7079 | 0.0580 | 10.6949 | 26.6086 | AID602310 |
lamin isoform A-delta10 | Homo sapiens (human) | Potency | 3.1623 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 3.9811 | 1.9953 | 25.5327 | 50.1187 | AID624287 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
cardiac alpha tropomyosin | Sus scrofa (pig) | EC50 (µMol) | 71.4850 | 1.8300 | 2.3740 | 2.9180 | AID504698 |
troponin I, cardiac muscle | Homo sapiens (human) | EC50 (µMol) | 71.4850 | 1.8300 | 2.3740 | 2.9180 | AID504698 |
troponin T, cardiac muscle isoform 3 | Homo sapiens (human) | EC50 (µMol) | 71.4850 | 1.8300 | 2.3740 | 2.9180 | AID504698 |
troponin C, slow skeletal and cardiac muscles | Homo sapiens (human) | EC50 (µMol) | 71.4850 | 1.8300 | 2.3740 | 2.9180 | AID504698 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Process | via Protein(s) | Taxonomy |
---|---|---|
negative regulation of inflammatory response to antigenic stimulus | Guanine nucleotide-binding protein G | Homo sapiens (human) |
renal water homeostasis | Guanine nucleotide-binding protein G | Homo sapiens (human) |
G protein-coupled receptor signaling pathway | Guanine nucleotide-binding protein G | Homo sapiens (human) |
regulation of insulin secretion | Guanine nucleotide-binding protein G | Homo sapiens (human) |
cellular response to glucagon stimulus | 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 |
---|---|---|
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 |
---|---|---|
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 |
---|---|---|---|---|
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. |
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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
[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] |