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
GABAA agonist which was designed to bind selectively to the
α5 subtype of GABA
A receptors.
The α
5 subtype (and to a lesser extent the α
1 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 α
1 subtype of GABA
A rather than α
5.
The
inverse agonist Ro15-4513, which blocks the α
5 subtype of GABA
A, reverses the effects of alcohol, suggesting that this subtype is also important in producing the subjective effects of alcohol intoxication.
See also
*
GL-II-73
GL-II-73 (GL-ii-073) is a benzodiazepine derivative related in chemical structure to compounds such as midazolam and adinazolam. It is described as an α5 preferring positive allosteric modulator of the benzodiazepine site of GABAA receptors, w ...
*
SH-I-048A
*
SH-053-R-CH3-2′F
References
Benzodiazepines
Sedatives
Hypnotics
Ethynyl compounds
Lactams
GABAA receptor positive allosteric modulators
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