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Gaboxadol
| File:Gaboxadol.svg | |
| Systematic (IUPAC) name | |
|---|---|
| 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3(2H)-one | |
| Clinical data | |
| Identifiers | |
| 64603-91-4 7px | |
| None | |
| PubChem | CID 3448 |
| ChemSpider | 3330 7px |
| UNII | K1M5RVL18S 7px |
| KEGG | D04282 7px |
| ChEMBL | CHEMBL312443 7px |
| Chemical data | |
| Formula | C6H8N2O2 |
| 140.14 g/mol | |
| |
| 14px (what is this?) (verify) | |
Gaboxadol also known as 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol (THIP) is a conformationally constrained derivative of the Amanita muscaria alkaloid muscimol that was first synthesized in 1977 by the Danish medicinal chemist Povl Krogsgaard-Larsen.[1] In the early 1980s gaboxadol was the subject of a series of pilot studies that tested its efficacy as an analgesic and anxiolytic, as well as a treatment for tardive dyskinesia, Huntington's disease, Alzheimer's disease, and spasticity.[1] It was not until 1996 that researchers attempted to harness gaboxadol's frequently reported sedative "adverse effect" for the treatment of insomnia, resulting in a series of clinical trials sponsored by Lundbeck and Merck.[1][2] In March, 2007, Merck and Lundbeck cancelled work on the drug, citing safety concerns and the failure of an efficacy trial. It acts on the GABA system, but possibly in a different way from benzodiazepines, nonbenzodiazepines and barbiturates - (Sodium Pentothal, etc.). Lundbeck states that gaboxadol also increases deep sleep (stage 4). It is, however, not reinforcing like benzodiazepines are.[3]
In 2015, Lundbeck sold its gaboxadol rights to medical startup Ovid Therapeutics, whose plan is to develop it for treating fragile X syndrome and Angelman Syndrome.[4]
See also
References
- ^ a b c Morris, Hamilton (August 2013). "Gaboxadol". Harper's Magazine. Retrieved 2014-11-20.
- ^ US Patent 4278676 - Heterocyclic compounds
- ^ Vashchinkina, E; Panhelainen, A; Vekovischeva, O. Y.; Aitta-Aho, T; Ebert, B; Ator, N. A.; Korpi, E. R. (2012). "GABA site agonist gaboxadol induces addiction-predicting persistent changes in ventral tegmental area dopamine neurons but is not rewarding in mice or baboons". Journal of Neuroscience 32 (15): 5310–20. PMID 22496576. doi:10.1523/JNEUROSCI.4697-11.2012.
- ^ Tirrell, Meg (16 April 2015). "Former Teva CEO's new gig at Ovid Therapeutics". CNBC. Retrieved 2015-05-06.
External links
- 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol at the US National Library of Medicine Medical Subject Headings (MeSH)
- H. Lundbeck Website
- Medical News Today article
- Report of cancellation of development.
- Gaboxadol
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