Names | |
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IUPAC name
4-(1-methylpiperidin-4-ylidene)-9,10-dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-ol
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Other names
10-hydroxy-ketotifen, WR621365
[1]
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Identifiers | |
3D model (
JSmol)
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|
PubChem
CID
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|
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Except where otherwise noted, data are given for materials in their
standard state (at 25 °C [77 °F], 100 kPa).
|
10-Hydroxyketotifen (WR621365) [1] is a biologically inactive metabolite of ketotifen. [2] [3] [4] Despite the mainstream scientific consensus that 10-hydroxyketotifen is a biologically inactive compound, its pharmacological properties are not very well studied outside the context of ketotifen, therefore, 10-hydroxyketotifen may still possess biological activity similarly to norketotifen, another metabolite of ketotifen. [1]
Ketotifen is an antihistamine medication which metabolizes to several compounds, including 10-hydroxyketotifen. Ketotifen, like other antihistamines, [5] [6] is mainly metabolized by the cytochrome P450 (CYP) enzymes, especially CYP3A4 [7] [8] in the liver. The CYP enzymes are responsible for the oxidation and demethylation of ketotifen, producing the major metabolites norketotifen and 10-hydroxyketotifen. Norketotifen is pharmacologically active and has a similar potency as ketotifen, while 10-hydroxyketotifen is inactive. The metabolites are then conjugated with glucuronic acid or sulfate and excreted in the urine and feces. [9] [10]
The definition and measurement of biological activity of drugs can be complex: biological activity is often defined in terms of the ability of a molecule to effect a change in a biological process, which can be quantified and measured in various ways; as such, even if 10-hydroxyketotifen is currently deemed inactive, it is possible that under certain conditions or within specific biological assays, some level of activity might be observed. [1] [11]
Names | |
---|---|
IUPAC name
4-(1-methylpiperidin-4-ylidene)-9,10-dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-ol
| |
Other names
10-hydroxy-ketotifen, WR621365
[1]
| |
Identifiers | |
3D model (
JSmol)
|
|
PubChem
CID
|
|
| |
Except where otherwise noted, data are given for materials in their
standard state (at 25 °C [77 °F], 100 kPa).
|
10-Hydroxyketotifen (WR621365) [1] is a biologically inactive metabolite of ketotifen. [2] [3] [4] Despite the mainstream scientific consensus that 10-hydroxyketotifen is a biologically inactive compound, its pharmacological properties are not very well studied outside the context of ketotifen, therefore, 10-hydroxyketotifen may still possess biological activity similarly to norketotifen, another metabolite of ketotifen. [1]
Ketotifen is an antihistamine medication which metabolizes to several compounds, including 10-hydroxyketotifen. Ketotifen, like other antihistamines, [5] [6] is mainly metabolized by the cytochrome P450 (CYP) enzymes, especially CYP3A4 [7] [8] in the liver. The CYP enzymes are responsible for the oxidation and demethylation of ketotifen, producing the major metabolites norketotifen and 10-hydroxyketotifen. Norketotifen is pharmacologically active and has a similar potency as ketotifen, while 10-hydroxyketotifen is inactive. The metabolites are then conjugated with glucuronic acid or sulfate and excreted in the urine and feces. [9] [10]
The definition and measurement of biological activity of drugs can be complex: biological activity is often defined in terms of the ability of a molecule to effect a change in a biological process, which can be quantified and measured in various ways; as such, even if 10-hydroxyketotifen is currently deemed inactive, it is possible that under certain conditions or within specific biological assays, some level of activity might be observed. [1] [11]