Gaboxadol
| Gaboxadol | |||||||||||||||||||||||||||||||
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| Chemical Nomenclature | |||||||||||||||||||||||||||||||
| Common names | Gaboxadol, THIP | ||||||||||||||||||||||||||||||
| Substitutive name | Gaboxadol, tetrahydroisoxazolopyridine | ||||||||||||||||||||||||||||||
| Systematic name | 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol | ||||||||||||||||||||||||||||||
| Class Membership | |||||||||||||||||||||||||||||||
| Psychoactive class | Depressant / Hallucinogen | ||||||||||||||||||||||||||||||
| Chemical class | 3-Hydroxyisoxazole[1] | ||||||||||||||||||||||||||||||
| Routes of Administration | |||||||||||||||||||||||||||||||
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| Summary sheet: Gaboxadol |
Gaboxadol (also knows as THIP, OV101 and LU-2-030) is a depressant substance of the 3-hydroxyisoxazole class that produces sedative, anxiolytic, hypnotic and distinct hallucinogenic effects. It is chemically related to muscimol, which is the primary alkaloid responsible for the psychoactive effects of amanita muscaria. It has been specifically developed alongside hundreds of other analogs to display more pronounced and selective therapeutic effects as well as a higher bioavailability than its parent compound muscimol.[citation needed]
It was first synthesized in 1977 by the Danish chemist Povl Krogsgaard-Larsen. Since then it was subject to numerous medical evaluations for potential applications as an anxiolytic and hypnotic as well as treating conditions such as Alzheimer's disease among others. It's latest attempt at clinical trials was for the treatment of insomnia, although the trials have been cancelled.[2][3]
According to its pharmacological action, it is among a few hypnotic substances that do not negatively alter or suppress sleep and sleep architecture. It increases stage 4 deep sleep[4] and simultaneously does not inhibit REM sleep,[citation needed] this is a trait currently unique to Gaboxadol and some related GABAergics such as pregabalin[citation needed], GHB[citation needed] or cinazepam.[citation needed]
In high doses, Gaboxadol produces distinct deliriant effects but not in the manner of traditional deliriants. It can be categorized as a "GABAergic deliriant". It is said to have similar effects to muscimol and zolpidem.
Chemistry
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.
Pharmacology
Gaboxadol acts on the GABA system, but in a different way from benzodiazepines and other GABAergic depressants. Lundbeck states that gaboxadol also increases deep sleep (stage 4).[5]
Subjective effects
Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.
It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.
Physical effects 
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- Sedation - Many users report mild to extreme sedation and even sleepiness or half-awake states while under the influence of Gaboxadol.
- Stimulation - While most users report sedation and a lack of energy, some users also report a relatively intense stimulation.
- Spontaneous physical sensations
- Pain relief
- Muscle relaxation
- Muscle spasms
- Nausea
- Increased perspiration
- Pupil constriction
- Increased salivation
Visual effects 
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Enhancements
Suppression
Distortions
- Colour shifting
- After images
- Tracers
- Drifting
- Depth perception distortions
- Perspective distortions
- Recursion
Geometry
Hallucinatory states
- External hallucination (autonomous entities; settings, sceneries, and landscapes; perspective hallucinations and scenarios and plots)
- Internal hallucination (autonomous entities; settings, sceneries, and landscapes; perspective hallucinations and scenarios and plots)
- Transformations
- Peripheral information misinterpretation
Cognitive effects 
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- Analysis enhancement
- Consciousness disconnection: Many users report a distinct dissociation from their surroundings.
- Cognitive euphoria - This results in feelings of physical euphoria which range between mild pleasure to powerfully all-encompassing bliss.
- Decreased libido or Increased libido - Many users of Gaboxadol report to experience a noticeable decrease in libido while others report the opposite.
- Dream potentiation - Many people fall asleep before the prominent effects take effect. These individuals report extremely vivid and often lucid dreams.
- Empathy, love, and sociability enhancement - While this effect is less powerful than that of MDMA or MDA, it is still prominent.
- Sleepiness - As a GABAA agonist, Gaboxadol can make people extremely drowsy.
- Unity and interconnectedness - While this effect is less powerful than that of MDMA or MDA, it is still prominent.
- Existential self-realization
- Immersion enhancement
- Increased music appreciation
- Analysis suppression
- Introspection
- Memory suppression
Auditory effects 
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- Auditory distortion
- Auditory hallucination - While a wide array of auditory hallucinations are possible, many users report hearing a strange, comforting, omnipresent humming sound.
Multi-sensory effects 
Experience reports
Anecdotal reports which describe the effects of this compound within our experience index include:
Additional experience reports can be found here:
Toxicity and harm potential
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This toxicity and harm potential section is a stub. As a result, it may contain incomplete or even dangerously wrong information! You can help by expanding upon or correcting it. |
Since Gaboxadol is a GABAA agonist, it may be harmful to combine it with other GABAergic depressants such as benzodiazepines or barbiturates.
Gaboxadol is not known to be addictive or dependence-forming, and reports even show that desire to redose goes down with usage, though there is no research on this topic.
It is strongly recommended that one use harm reduction practices when using this substance.
Legal status
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This legality section is a stub. As such, it may contain incomplete or wrong information. You can help by expanding it. |
See also
External links
References
- ↑ New approach to 3-hydroxyisoxazole-5-carbaldehydes: key intermediates in the synthesis of new 3-hydroxyisoxazoles of pharmacological interest
- ↑ http://harpers.org/archive/2013/08/gaboxadol/
- ↑ US Patent 4278676 - Heterocyclic compounds
- ↑ Vashchinkina E, Panhelainen A, Vekovischeva OY, Aitta-aho T, Ebert B, Ator NA, Korpi ER (April 2012). "GABA site agonist gaboxadol induces addiction-predicting persistent changes in ventral tegmental area dopamine neurons but is not rewarding in mice or baboons". The Journal of Neuroscience. 32 (15): 5310–20. doi:10.1523/JNEUROSCI.4697-11.2012
. PMC 6622081 . PMID 22496576.
- ↑ Vashchinkina E, Panhelainen A, Vekovischeva OY, Aitta-aho T, Ebert B, Ator NA, Korpi ER (April 2012). "GABA site agonist gaboxadol induces addiction-predicting persistent changes in ventral tegmental area dopamine neurons but is not rewarding in mice or baboons". The Journal of Neuroscience. 32 (15): 5310–20. doi:10.1523/JNEUROSCI.4697-11.2012 . PMC 6622081 . PMID 22496576.