Gaboxadol , also known as 4,5,6,7-t etrah ydroi soxazolo(5,4-c)p yridin-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.[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 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.[3]
In 2015, Lundbeck sold its rights to the molecule to Ovid Therapeutics, whose plan is to develop it for FXS and Angelman Syndrome .[4]
See also [ edit ]
References [ edit ]
^ 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. 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 .
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