Name | Gaboxadol (hydrochloride) |
CAS number | 85118-33-8 |
Description | Gaboxadol Hydrochloride is the hydrochloride salt of gaboxadol, a selective extrasynaptic GABAA receptor agonist, assigned the CAS Registry Number 85118-33-8. |
Structural formula |  |
Molecular Formula | C6H9ClN2O2 |
Molecular Weight | 176.6 g/mol |
Appearance | White powder |
Quality Standard | 99% |
Storage Condition | Cool dry place( away from the light) |
Shelf Life | >2 years if stored properly |
Sample package | Aluminium foil bag |
Commercial package | Aluminium Tin, Fiber drum |
Origin | China |
Gaboxadol Hydrochloride More Info
Gaboxadol Hydrochloride is the hydrochloride salt of gaboxadol, a selective extrasynaptic GABAA receptor agonist, assigned the CAS Registry Number 85118-33-8. Its molecular structure is based on an isoxazole ring fused to an azole, a distinct chemical scaffold from benzodiazepines or non-benzodiazepine hypnotics. Salt formation enhances its stability, solubility, and crystallinity as a pharmaceutical substance. The compound was designed to selectively target specific GABAergic subtypes to produce sleep-promoting effects while aiming to minimize the side effects associated with traditional sedative-hypnotics.
The drug's primary mechanism of action is as a selective agonist for GABAA receptors, specifically those containing the delta subunit located extrasynaptically. These receptors are widely distributed in the central nervous system and are crucial for mediating tonic neuronal inhibition. By activating these delta-subunit-containing GABAA receptors, gaboxadol potentiates the baseline tonic inhibitory current mediated by endogenous GABA, leading to a generalized dampening of neuronal activity. This produces a potent sedative-hypnotic effect through a mechanism considered more physiological than the hypnotic action mediated by the alpha-1 subunit.
The clinical development of gaboxadol was focused on the treatment of insomnia, particularly for sleep initiation and maintenance difficulties. It was developed to provide a novel hypnotic with a mechanism distinct from existing drugs, potentially offering unique benefits for sleep architecture, such as enhancing slow-wave sleep. It advanced to Phase III clinical trials for primary insomnia, where its potential to improve both subjective and objective sleep parameters was evaluated. It was investigated as a potential alternative to traditional benzodiazepine receptor agonists.
In clinical trials, the medication was administered orally in tablet form. Its pharmacokinetic profile showed rapid absorption, with peak plasma concentrations reached approximately one hour after dosing. It had a relatively short elimination half-life of about 1.5 hours, making it suitable for sleep induction while aiming to minimize next-day residual sedation. However, its rapid clearance also potentially limited its efficacy for sleep maintenance.
The development of gaboxadol encountered significant safety and efficacy challenges. Clinical trial data indicated its efficacy was not consistently superior to placebo. More critically, adverse event reports emerged concerning perceptual disturbances, including hallucinations and confusional states, particularly at higher doses. These neuropsychiatric side effects, coupled with its limited efficacy, ultimately led to the termination of its global clinical development program, and it failed to gain regulatory approval for the treatment of insomnia. Consequently, it now exists primarily as a historical reference compound in pharmacological research.
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