|CompTox Dashboard (EPA)|
|Chemical and physical data|
|Molar mass||140.14 g/mol g·mol−1|
|3D model (JSmol)|
|(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 alkaloid muscimol that was first synthesized in 1977 by the Danish 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 in a different way from benzodiazepines, Z-Drugs, and barbiturates. 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.
- Tirrell, Meg (16 April 2015). “Former Teva CEO’s new gig at Ovid Therapeutics”. CNBC. Retrieved 2015-05-06.
- 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.