You're describing a chemical compound, **1,1-dimethyl-3-[3-(4-morpholinyl)propyl]-3-(1-naphthalenylmethyl)urea**, also known as **MK-801**, **dizocilpine**, or **Dexoxadrol**.
**What is it?**
It's a non-competitive antagonist of the NMDA receptor. This means it blocks the action of the neurotransmitter glutamate at the NMDA receptor, a key protein involved in learning and memory.
**Why is it important for research?**
MK-801 is an important research tool for understanding the role of NMDA receptors in various brain functions, including:
* **Learning and memory:** As a potent NMDA antagonist, MK-801 can impair learning and memory in animal models. This helps researchers study how NMDA receptors contribute to these processes.
* **Neuroprotection:** Research suggests that MK-801 may have neuroprotective effects, potentially preventing damage to neurons in conditions like stroke and Alzheimer's disease. However, its potential side effects limit its clinical use.
* **Pain perception:** MK-801 has been investigated for its potential to reduce pain, particularly neuropathic pain.
* **Addiction and substance abuse:** MK-801 has shown promise in animal studies as a potential treatment for addiction to drugs like cocaine and methamphetamine.
**Important Considerations:**
* **Toxicity:** MK-801 is a highly potent drug with significant side effects, including sedation, dissociation, amnesia, and even neurotoxicity. This makes it unsuitable for human use as a therapeutic agent.
* **Research only:** Due to its toxicity, MK-801 is primarily used in preclinical research studies, mainly in animal models.
* **Ethical considerations:** The use of MK-801 in animal research requires careful ethical review and adherence to strict animal welfare guidelines.
**Overall, MK-801 is a valuable research tool for investigating the role of NMDA receptors in various brain functions. However, its toxicity and ethical considerations restrict its use to preclinical research settings.**
| ID Source | ID |
|---|---|
| PubMed CID | 3438105 |
| CHEMBL ID | 1505983 |
| CHEBI ID | 116751 |
| Synonym |
|---|
| 1,1-dimethyl-3-(3-morpholin-4-yl-propyl)-3-naphthalen-1-ylmethyl-urea |
| smr000420046 |
| MLS000779860 |
| CHEBI:116751 |
| 1,1-dimethyl-3-(3-morpholin-4-ylpropyl)-3-(naphthalen-1-ylmethyl)urea |
| HMS2800P19 |
| CHEMBL1505983 |
| Q27202639 |
| 1,1-dimethyl-3-[3-(4-morpholinyl)propyl]-3-(1-naphthalenylmethyl)urea |
| AKOS032399092 |
| 1,1-dimethyl-3-[3-(morpholin-4-yl)propyl]-3-(naphthalen-1-ylmethyl)urea |
| STL563869 |
| Class | Description |
|---|---|
| naphthalenes | Any benzenoid aromatic compound having a skeleton composed of two ortho-fused benzene rings. |
| [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, Beta-lactamase | Escherichia coli K-12 | Potency | 28.1838 | 0.0447 | 17.8581 | 100.0000 | AID485341 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 89.1251 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
| neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 15.8489 | 0.0158 | 12.3113 | 615.5000 | AID1461 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| 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. |
| 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. |
| 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. |
| 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] | ||