Английская Википедия:Fenobam
Fenobam is an imidazole derivative developed by McNeil Laboratories in the late 1970s as a novel anxiolytic drug with an at-the-time-unidentified molecular target in the brain. Subsequently, it was determined that fenobam acts as a potent and selective negative allosteric modulator of the metabotropic glutamate receptor subtype mGluR5,[1][2] and it has been used as a lead compound for the development of a range of newer mGluR5 antagonists.[3][4][5][6]
Fenobam has anxiolytic effects comparable to those of benzodiazepine drugs,[1][7][8] but was never commercially marketed for the treatment of anxiety due to dose-limiting side effects such as amnesia and psychotomimetic symptoms.[9][10] Following the discovery of its activity as a potent negative allosteric modulator of mGluR5, fenobam has been re-investigated for many applications, with its profile of combined antidepressant, anxiolytic, analgesic and anti-addictive effects potentially useful given the common co-morbidity of these symptoms.[11][12] It has also shown promising initial results in the treatment of fragile X syndrome.[13] It was developed by a team at McNeil Laboratories in the 1970s.[14]
Chemistry
Fenobam is known to exist in five crystalline forms, all of them exhibiting a tautomeric structure with the proton attached to the five membered ring nitrogen. [15]
See also
References
Шаблон:Metabotropic glutamate receptor modulators
- ↑ 1,0 1,1 Шаблон:Cite journal
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- ↑ US Patent 3983135 4-Oxo-2-imidazolidinylidene ureas
- ↑ Шаблон:Cite journal
- Английская Википедия
- Anxiolytics
- Imidazolines
- Lactams
- Ureas
- Chloroarenes
- Orphan drugs
- MGlu5 receptor antagonists
- Abandoned drugs
- Glutamate receptor negative allosteric modulators
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