Oxaflozane: Difference between revisions
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==Overview== | ==Overview== | ||
'''Oxaflozane''' ('''Conflictan''') is an [[antidepressant]] and [[anxiolytic]] [[drug]] that was introduced in [[France]] in 1982 by [[Solvay (company)|Solvay]] for the treatment of [[major depression|depression]], but has since been [[discontinued|abandoned]].<ref name="isbn3-88763-075-0">{{cite book | author = Swiss Pharmaceutical Society | title = Index Nominum 2000: International Drug Directory (Book with CD-ROM) | publisher = Medpharm Scientific Publishers | location = Boca Raton | year = 2000 | page = 766 | isbn = 3-88763-075-0 | oclc = | doi = | url = http://books.google.com/books?id=5GpcTQD_L2oC&lpg=PA766&dq=oxaflozane%20conflictan&as_brr=3&pg=PA766#v=onepage&q=&f=false}}</ref><ref name="isbn0-8155-1144-2">{{cite book | author = Sittig, Marshall | title = Pharmaceutical manufacturing encyclopedia | publisher = Noyes Publications | location = Park Ridge, N.J., U.S.A | year = 1988 | page = 1122 | isbn = 0-8155-1144-2 | oclc = | doi = | url = http://books.google.com/books?id=XCsJgUnclbcC&lpg=PA1122&dq=oxaflozane%20conflictan&as_brr=3&pg=PA1122#v=onepage&q=&f=false}}</ref> It is a [[prodrug]] to [[2-(3-trifluoromethylphenyl)morpholine|''N''-dealkyloxaflozane]], which acts as a [[functional selectivity|non-selective]] [[serotonin receptor]] [[receptor agonist|agonist]] for the [[5-HT1A receptor|5-HT<sub>1A</sub>]] (pKi = 7.1), [[5-HT2A receptor|5-HT<sub>2A</sub>]] (pKi = 6.0), and [[5-HT2C receptor|5-HT<sub>2C</sub>]] (pKi = 7.5) subtypes.<ref name="pmid16160946">{{cite journal | author = Leysen DC | title = Selective 5-HT2C agonists as potential antidepressants | journal = IDrugs : the Investigational Drugs Journal | volume = 2 | issue = 2 | pages = 109–20 |date=February 1999 | pmid = 16160946 | doi = | url = }}</ref> Oxaflozane may also have [[anticholinergic]] effects in high doses.<ref name="pmid1542141">{{cite journal | author = Dutertre JP, Barbier P, Suc AL, Jonville AP, Autret E | title = Oxaflozane overdose in a child | journal = Journal of Toxicology. Clinical Toxicology | volume = 30 | issue = 1 | pages = 123–6 | year = 1992 | pmid = 1542141 | doi = 10.3109/15563659208994452| url = }}</ref> | '''Oxaflozane''' ('''Conflictan''') is an [[antidepressant]] and [[anxiolytic]] [[drug]] that was introduced in [[France]] in 1982 by [[Solvay (company)|Solvay]] for the treatment of [[major depression|depression]], but has since been [[discontinued|abandoned]].<ref name="isbn3-88763-075-0">{{cite book | author = Swiss Pharmaceutical Society | title = Index Nominum 2000: International Drug Directory (Book with CD-ROM) | publisher = Medpharm Scientific Publishers | location = Boca Raton | year = 2000 | page = 766 | isbn = 3-88763-075-0 | oclc = | doi = | url = http://books.google.com/books?id=5GpcTQD_L2oC&lpg=PA766&dq=oxaflozane%20conflictan&as_brr=3&pg=PA766#v=onepage&q=&f=false}}</ref><ref name="isbn0-8155-1144-2">{{cite book | author = Sittig, Marshall | title = Pharmaceutical manufacturing encyclopedia | publisher = Noyes Publications | location = Park Ridge, N.J., U.S.A | year = 1988 | page = 1122 | isbn = 0-8155-1144-2 | oclc = | doi = | url = http://books.google.com/books?id=XCsJgUnclbcC&lpg=PA1122&dq=oxaflozane%20conflictan&as_brr=3&pg=PA1122#v=onepage&q=&f=false}}</ref> It is a [[prodrug]] to [[2-(3-trifluoromethylphenyl)morpholine|''N''-dealkyloxaflozane]], which acts as a [[functional selectivity|non-selective]] [[serotonin receptor]] [[receptor agonist|agonist]] for the [[5-HT1A receptor|5-HT<sub>1A</sub>]] (pKi = 7.1), [[5-HT2A receptor|5-HT<sub>2A</sub>]] (pKi = 6.0), and [[5-HT2C receptor|5-HT<sub>2C</sub>]] (pKi = 7.5) subtypes.<ref name="pmid16160946">{{cite journal | author = Leysen DC | title = Selective 5-HT2C agonists as potential antidepressants | journal = IDrugs : the Investigational Drugs Journal | volume = 2 | issue = 2 | pages = 109–20 |date=February 1999 | pmid = 16160946 | doi = | url = }}</ref> Oxaflozane may also have [[anticholinergic]] effects in high doses.<ref name="pmid1542141">{{cite journal | author = Dutertre JP, Barbier P, Suc AL, Jonville AP, Autret E | title = Oxaflozane overdose in a child | journal = Journal of Toxicology. Clinical Toxicology | volume = 30 | issue = 1 | pages = 123–6 | year = 1992 | pmid = 1542141 | doi = 10.3109/15563659208994452| url = }}</ref> | ||
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Revision as of 16:10, 8 April 2015
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| Routes of administration | Oral |
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| E number | {{#property:P628}} |
| ECHA InfoCard | {{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value). |
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| Formula | C14H18F3NO |
| Molar mass | 273.29 g/mol |
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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]
Overview
Oxaflozane (Conflictan) is an antidepressant and anxiolytic drug that was introduced in France in 1982 by Solvay for the treatment of depression, but has since been abandoned.[1][2] It is a prodrug to N-dealkyloxaflozane, which acts as a non-selective serotonin receptor agonist for the 5-HT1A (pKi = 7.1), 5-HT2A (pKi = 6.0), and 5-HT2C (pKi = 7.5) subtypes.[3] Oxaflozane may also have anticholinergic effects in high doses.[4]
References
- ↑ Swiss Pharmaceutical Society (2000). Index Nominum 2000: International Drug Directory (Book with CD-ROM). Boca Raton: Medpharm Scientific Publishers. p. 766. ISBN 3-88763-075-0.
- ↑ Sittig, Marshall (1988). Pharmaceutical manufacturing encyclopedia. Park Ridge, N.J., U.S.A: Noyes Publications. p. 1122. ISBN 0-8155-1144-2.
- ↑ Leysen DC (February 1999). "Selective 5-HT2C agonists as potential antidepressants". IDrugs : the Investigational Drugs Journal. 2 (2): 109–20. PMID 16160946.
- ↑ Dutertre JP, Barbier P, Suc AL, Jonville AP, Autret E (1992). "Oxaflozane overdose in a child". Journal of Toxicology. Clinical Toxicology. 30 (1): 123–6. doi:10.3109/15563659208994452. PMID 1542141.
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