(4-Methoxyphenyl)-(4-methyl-1-piperazinyl)methanethione, also known as **thiocolchicoside**, is a **nonsteroidal anti-inflammatory drug (NSAID)**.
Here's why it's important for research:
* **Mechanism of Action:** Thiocolchicoside is a potent **inhibitor of microtubule assembly**. Microtubules are crucial for various cellular processes, including cell division, cell migration, and intracellular transport. By inhibiting microtubule assembly, thiocolchicoside can have **anti-inflammatory and analgesic effects**.
* **Potential Therapeutic Applications:** Thiocolchicoside has shown promise in preclinical studies for treating various conditions, including:
* **Muscle Spasm and Pain:** It acts as a muscle relaxant, potentially making it useful for treating conditions like low back pain and muscle strains.
* **Inflammation:** Its anti-inflammatory properties could be valuable in managing inflammatory conditions like arthritis.
* **Cancer:** Some research suggests it may have potential in treating certain types of cancer due to its ability to interfere with cell division.
* **Safety and Toxicity:** Thiocolchicoside is generally considered safe and well-tolerated, but some side effects can occur, such as gastrointestinal upset, dizziness, and drowsiness. Further research is needed to fully understand its long-term safety profile.
**Current Research:**
* **Novel Drug Delivery Systems:** Researchers are exploring new ways to deliver thiocolchicoside, such as transdermal patches and nanoparticles, to improve its effectiveness and reduce side effects.
* **Combination Therapies:** Combining thiocolchicoside with other medications, like opioids or anti-inflammatory agents, is being investigated to enhance pain relief and treatment efficacy.
* **Mechanism of Action Studies:** Ongoing research aims to further elucidate the precise molecular mechanisms by which thiocolchicoside exerts its anti-inflammatory and analgesic effects.
**Conclusion:**
(4-Methoxyphenyl)-(4-methyl-1-piperazinyl)methanethione (thiocolchicoside) is a promising NSAID with potential therapeutic applications. Further research is necessary to fully understand its clinical efficacy, safety, and potential for improving patient care.
ID Source | ID |
---|---|
PubMed CID | 804311 |
CHEMBL ID | 1602583 |
CHEBI ID | 105991 |
Synonym |
---|
smr000142145 |
MLS000534728 , |
1-[(4-methoxyphenyl)carbonothioyl]-4-methylpiperazine |
(4-methoxyphenyl)(4-methylpiperazin-1-yl)methanethione |
STK221425 |
CHEBI:105991 |
AKOS000347976 |
(4-methoxyphenyl)-(4-methylpiperazin-1-yl)methanethione |
HMS2326E16 |
CHEMBL1602583 |
(4-methoxyphenyl)-(4-methyl-1-piperazinyl)methanethione |
Q27183786 |
sr-01000250297 |
SR-01000250297-1 |
Class | Description |
---|---|
methoxybenzenes | Any aromatic ether that consists of a benzene skeleton substituted with one or more methoxy groups. |
[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, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 0.1000 | 0.0032 | 45.4673 | 12,589.2998 | AID2517 |
phosphopantetheinyl transferase | Bacillus subtilis | Potency | 25.1189 | 0.1413 | 37.9142 | 100.0000 | AID1490 |
regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 50.1187 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
serine/threonine-protein kinase PLK1 | Homo sapiens (human) | Potency | 26.6795 | 0.1683 | 16.4040 | 67.0158 | AID720504 |
DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 100.0000 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
geminin | Homo sapiens (human) | Potency | 23.1093 | 0.0046 | 11.3741 | 33.4983 | AID624296 |
neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 3.9811 | 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 |
---|---|---|---|---|
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. |
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. |
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. |
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
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] |