QH-II-66 (QH-ii-066) is a sedative drug which is a benzodiazepine derivative. It produces some of the same effects as other benzodiazepines, but is much more selective than most other drugs of this class and so produces somewhat less sedation and

ataxia Ataxia is a neurological sign consisting of lack of voluntary coordination of muscle movements that can include gait abnormality, speech changes, and abnormalities in eye movements. Ataxia is a clinical manifestation indicating dysfunction of ...

than other related drugs such as

diazepam Diazepam, first marketed as Valium, is a medicine of the benzodiazepine family that acts as an anxiolytic. It is commonly used to treat a range of conditions, including anxiety, seizures, alcohol withdrawal syndrome, muscle spasms, insomnia, ...

and

triazolam Triazolam, sold under the brand name Halcion among others, is a central nervous system (CNS) depressant tranquilizer of the triazolobenzodiazepine (TBZD) class, which are benzodiazepine (BZD) derivatives. It possesses pharmacological properties ...

, although it still retains anticonvulsant effects. QH-ii-066 is a highly subtype-selective GABA_A agonist which was designed to bind selectively to the α₅ subtype of GABA_A receptors. The α₅ subtype (and to a lesser extent the α₁ subtype) of GABA_A are two of the most important targets in the brain that produce the effects of alcohol, and so one of the purposes for which QH-ii-066 was developed was to reproduce the GABAergic effects of alcohol separately from its other actions. QH-ii-066 replicates some of the effects of alcohol, such as sedation and ataxia, but does not increase appetite, as this effect seems to be produced by the α₁ subtype of GABA_A rather than α₅. The inverse agonist Ro15-4513, which blocks the α₅ subtype of GABA_A, reverses the effects of alcohol, suggesting that this subtype is also important in producing the subjective effects of alcohol intoxication.

References

Benzodiazepines Sedatives Hypnotics Ethynyl compounds Lactams GABAA receptor positive allosteric modulators {{sedative-stub

See also

References