Page last updated: 2024-12-09

1-(2-methyl-1H-indol-3-yl)-2-(2-thiazolylamino)ethanone

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 **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.

Cross-References

ID SourceID
PubMed CID912279
CHEMBL ID1409483
CHEBI ID113240

Synonyms (12)

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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
indolesAny 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 Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency0.70790.044717.8581100.0000AID485294
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency39.81070.140911.194039.8107AID2451
RGS12Homo sapiens (human)Potency6.30960.794310.991425.1189AID2390
phosphopantetheinyl transferaseBacillus subtilisPotency39.81070.141337.9142100.0000AID1490
TDP1 proteinHomo sapiens (human)Potency29.09290.000811.382244.6684AID686979
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency35.48130.011212.4002100.0000AID1030
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency4.15240.00798.23321,122.0200AID2546; AID2551
Guanine nucleotide-binding protein GHomo sapiens (human)Potency11.22021.995325.532750.1187AID624287
[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
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
[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]