You're asking about **1-(2-methyl-1H-indol-3-yl)-2-(2-thiazolylamino)ethanone**, often called **MK-801**.
**MK-801** is a **non-competitive NMDA receptor antagonist**.
Here's a breakdown of what that means:
* **NMDA Receptor:** This is a type of glutamate receptor, a key neurotransmitter in the brain. It plays a crucial role in learning, memory, and synaptic plasticity.
* **Antagonist:** A substance that blocks or inhibits the activity of a receptor.
* **Non-Competitive:** It doesn't compete with glutamate for binding to the receptor. Instead, it binds to a different site on the receptor, preventing the receptor from opening and allowing ions to flow through.
**Why is MK-801 Important for Research?**
MK-801 has been extensively studied for its effects on the brain and nervous system. It's important for research because:
* **Understanding Brain Function:** MK-801 has helped researchers understand the role of NMDA receptors in various brain functions, including:
* **Learning and Memory:** Blocking NMDA receptors impairs learning and memory, highlighting their crucial role in these processes.
* **Synaptic Plasticity:** NMDA receptors are involved in the strengthening and weakening of connections between neurons (synaptic plasticity), a fundamental process for learning.
* **Neuroprotection:** NMDA receptor overactivation is implicated in brain damage in conditions like stroke and epilepsy. MK-801 has been investigated as a potential neuroprotective agent.
* **Animal Models of Neurological Disorders:** MK-801 is used to create animal models of various neurological disorders, including:
* **Schizophrenia:** MK-801 produces some of the symptoms of schizophrenia, making it a valuable tool for studying this complex disorder.
* **Depression and Anxiety:** MK-801 has also been used to model aspects of depression and anxiety, providing insights into the role of NMDA receptors in these disorders.
**Important Note:** While MK-801 has been a crucial research tool, it's **not a therapeutic drug**. It has significant side effects, including sedation, amnesia, and potentially dangerous neurotoxicity.
**Current Research:**
Current research on MK-801 focuses on:
* **Developing safer and more specific NMDA receptor antagonists:** Researchers are exploring new compounds that target specific subtypes of NMDA receptors, potentially reducing side effects.
* **Understanding the molecular mechanisms of NMDA receptor modulation:** By studying how MK-801 interacts with NMDA receptors, researchers gain valuable insights into the complex mechanisms of these receptors.
In summary, MK-801 is a powerful research tool that has advanced our understanding of NMDA receptors and their role in various brain functions and disorders. However, its significant side effects prevent it from being a viable therapeutic option. Current research focuses on developing safer and more specific NMDA receptor modulators with potential therapeutic applications.
ID Source | ID |
---|---|
PubMed CID | 912279 |
CHEMBL ID | 1409483 |
CHEBI ID | 113240 |
Synonym |
---|
OPREA1_378443 |
smr000147072 |
1-(2-methyl-1h-indol-3-yl)-2-(thiazol-2-ylamino)-ethanone |
MLS000554955 |
CHEBI:113240 |
AKOS005459294 |
1-(2-methyl-1h-indol-3-yl)-2-(1,3-thiazol-2-ylamino)ethanone |
STK525966 |
HMS2335N06 |
CHEMBL1409483 |
Q27193708 |
1-(2-methyl-1h-indol-3-yl)-2-(2-thiazolylamino)ethanone |
Class | Description |
---|---|
indoles | Any compound containing an indole skeleton. |
[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 | 0.7079 | 0.0447 | 17.8581 | 100.0000 | AID485294 |
Chain A, Putative fructose-1,6-bisphosphate aldolase | Giardia intestinalis | Potency | 39.8107 | 0.1409 | 11.1940 | 39.8107 | AID2451 |
RGS12 | Homo sapiens (human) | Potency | 6.3096 | 0.7943 | 10.9914 | 25.1189 | AID2390 |
phosphopantetheinyl transferase | Bacillus subtilis | Potency | 39.8107 | 0.1413 | 37.9142 | 100.0000 | AID1490 |
TDP1 protein | Homo sapiens (human) | Potency | 29.0929 | 0.0008 | 11.3822 | 44.6684 | AID686979 |
aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 35.4813 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 89.1251 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 4.1524 | 0.0079 | 8.2332 | 1,122.0200 | AID2546; AID2551 |
Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 11.2202 | 1.9953 | 25.5327 | 50.1187 | AID624287 |
[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 |
---|---|---|---|---|
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
[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] |