QH-II-66
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QH-II-66[1] (QH-ii-066) is a sedative drug which is a benzodiazepine derivative.[2] 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 than other related drugs such as diazepam and triazolam, although it still retains anticonvulsant effects.[3]
QH-ii-066 is a highly subtype-selective GABAA agonist which was designed to bind selectively to the α5 subtype of GABAA receptors.[4]
The α5 subtype (and to a lesser extent the α1 subtype) of GABAA are two of the most important targets in the brain that produce the effects of
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 GABAA rather than α5.[7] The inverse agonist Ro15-4513, which blocks the α5 subtype of GABAA, reverses the effects of alcohol, suggesting that this subtype is also important in producing the subjective effects of alcohol intoxication.[8]
See also
References
- ^ US 2010004226, Cook JM, Hao H, Huang S, Sarma PV, Zhang C, "Stereospecific anxiolytic and anticonvulsant agents with reduced muscle-relaxant, sedative-hypnotic and ataxic effects", published 7 January 2010
- PMID 10633039.
- ^ US 7119196, Cook JM, Huang Q, He X, Li X, Yu J, Han D, Lelas S, McElroy JF, "Anxiolytic agents with reduced sedative and ataxic effects", issued 10 September 2006, assigned to WiSys Technology Foundation Inc
- ^ Huang Q, Zhang W, Liu R, McKernan RM, Cook JM (1996). "Benzo-fused benzodiazepines employed as topological probes for the study of benzodiazepine receptor subtypes". Medicinal Chemistry Research. 6 (3): 384–391.
- S2CID 97681615.
- PMID 16441269.
- S2CID 32950492.
- PMID 16698930.
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