Chemistry:QH-II-66
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| Formula | C18H14N2O |
| Molar mass | 274.33 g·mol−1 |
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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 alcohol,[5] 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.[6]
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
- ↑ Cook JM, Hao H, Huang S, Sarma PV, Zhang C, "Stereospecific anxiolytic and anticonvulsant agents with reduced muscle-relaxant, sedative-hypnotic and ataxic effects", US patent 2010004226, published 7 January 2010
- ↑ "Pharmacophore/receptor models for GABAA/BzR subtypes (α1β3γ2, α5β3γ2, and α6β3γ2) via a comprehensive ligand-mapping approach". Journal of Medicinal Chemistry 43 (1): 71–95. January 2000. doi:10.1021/jm990341r. PMID 10633039.
- ↑ Cook JM, Huang Q, He X, Li X, Yu J, Han D, Lelas S, McElroy JF, "Anxiolytic agents with reduced sedative and ataxic effects", US patent 7119196, issued 10 September 2006, assigned to WiSys Technology Foundation Inc
- ↑ "Benzo-fused benzodiazepines employed as topological probes for the study of benzodiazepine receptor subtypes". Medicinal Chemistry Research 6 (3): 384–391. 1996.
- ↑ "Contribution of alpha 1GABAA and alpha 5GABAA receptor subtypes to the discriminative stimulus effects of ethanol in squirrel monkeys". The Journal of Pharmacology and Experimental Therapeutics 313 (2): 658–67. May 2005. doi:10.1124/jpet.104.080275. PMID 15650112.
- ↑ "Understanding how the brain perceives alcohol: neurobiological basis of ethanol discrimination". Alcoholism: Clinical and Experimental Research 30 (2): 203–13. February 2006. doi:10.1111/j.1530-0277.2006.00024.x. PMID 16441269.
- ↑ "Enhanced sucrose pellet consumption induced by benzodiazepine-type drugs in squirrel monkeys: role of GABAA receptor subtypes". Psychopharmacology 187 (3): 321–30. August 2006. doi:10.1007/s00213-006-0431-2. PMID 16783540.
- ↑ "Low-dose alcohol actions on alpha4beta3delta GABAA receptors are reversed by the behavioral alcohol antagonist Ro15-4513". Proceedings of the National Academy of Sciences of the United States of America 103 (22): 8540–5. May 2006. doi:10.1073/pnas.0600194103. PMID 16698930. Bibcode: 2006PNAS..103.8540W.
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