Tioxamast is a synthetic compound with the chemical name 2-(4-methylpiperazin-1-yl)-10H-phenothiazine. It is a potent inhibitor of mast cell degranulation, which is the process by which mast cells release histamine and other inflammatory mediators. Tioxamast has been investigated for its potential therapeutic effects in a variety of inflammatory diseases, including asthma, allergic rhinitis, and inflammatory bowel disease. It is thought to work by inhibiting the activation of phospholipase A2, an enzyme involved in the production of inflammatory mediators. Tioxamast has also been shown to have antioxidant and anti-inflammatory properties. However, it has not been approved for clinical use in humans.'
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tioxamast: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 68927 |
| CHEMBL ID | 16134 |
| SCHEMBL ID | 2111615 |
| MeSH ID | M0112378 |
| Synonym |
|---|
| f 1865 |
| acetic acid, ((4-(4-methoxyphenyl)-2-thiazolyl)amino)oxo-, ethyl ester |
| brn 5350796 |
| ethyl-(4-paramethoxyphenyl-2-thiazolyl)-oxamate |
| ethyl ((4-(4-methoxyphenyl)-2-thiazolyl)amino)oxoacetate |
| tioxamastum [latin] |
| tioxamast [inn] |
| ethyl (4-(p-methoxyphenyl)-2-thiazolyl)oxamate |
| f-1865 , |
| tioxamast |
| CHEMBL16134 |
| 74531-88-7 |
| ethyl 2-[[4-(4-methoxyphenyl)-1,3-thiazol-2-yl]amino]-2-oxoacetate |
| AKOS005066763 |
| hq7f53to3l , |
| tioxamastum |
| unii-hq7f53to3l |
| acetic acid,2-[[4-(4-methoxyphenyl)-2-thiazolyl]amino]-2-oxo-, ethyl ester |
| DTXSID20225536 |
| SCHEMBL2111615 |
| FT-0762671 |
| Q27280051 |
Tioxamast (F 1865) is an antiallergic drug that, administered systemically, reduces anaphylaxis in various models in rats. It inhibits the release and synthesis of certain mediators of inflammation.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Tioxamast (F 1865) is an antiallergic drug that, administered systemically, reduces anaphylaxis in various models in rats. " | ( Antiallergic and anti-inflammatory action of tioxamast in rats. I. Antiallergic activity in vivo and in vitro. Aliaga, M; Barbara, M; Bruniquel, F; Caillol, V; Delhon, A; N'Guyen, X; Puech, L; Tarayre, JP; Tisné-Versailles, J; Tisseyre, N, 1990) | 1.98 |
| "Tioxamast is an antiallergic drug that inhibits anaphylaxis in various models in rats, and it inhibits the release and synthesis of certain mediators of inflammation [see Tarayre et al., this issue]. " | ( Antiallergic and anti-inflammatory action of tioxamast in rats. II. Anti-inflammatory action in vivo. Aliaga, M; Barbara, M; Bruniquel, F; Caillol, V; Delhon, A; N'Guyen, X; Puech, L; Tarayre, JP; Tisné-Versailles, J; Tisseyre, N, 1990) | 1.98 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID176693 | Antiallergic activity by rat passive cutaneous anaphylaxis (PCA) assay when administered iv; ND means no data | 1983 | Journal of medicinal chemistry, Aug, Volume: 26, Issue:8 | N-(4-substituted-thiazolyl)oxamic acid derivatives, a new series of potent, orally active antiallergy agents. |
| AID176703 | Antiallergic activity by rat passive cutaneous anaphylaxis (PCA) assay when administered per orally | 1983 | Journal of medicinal chemistry, Aug, Volume: 26, Issue:8 | N-(4-substituted-thiazolyl)oxamic acid derivatives, a new series of potent, orally active antiallergy agents. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 2 (50.00) | 18.7374 |
| 1990's | 2 (50.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (0.00) | 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 (12.50) 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 | 6 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||