|Systematic (IUPAC) name|
|Molecular mass||140.14 g/mol|
|(what is this?)|
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. 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. 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. 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 - (Valium, Sodium Pentothal, Ambien etc.). Lundbeck states that gaboxadol also increases deep sleep (stage 4). It is, however, not reinforcing like benzodiazepines are.
- 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. doi:10.1523/JNEUROSCI.4697-11.2012. PMID 22496576.
- 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.
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