SH-I-048A (SH-i-048A) is a
benzodiazepine
Benzodiazepines (BZD, BDZ, BZs), colloquially known as "benzos", are a class of central nervous system (CNS) depressant, depressant drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring. They are prescribed t ...
derivative related in structure to compounds such as
flubromazepam and
meclonazepam. SH-I-048A is described as a non subtype selective
superagonist
In the field of pharmacology, a superagonist is a type of agonist that is capable of producing a maximal response greater than the endogenous agonist for the target receptor, and thus has an efficacy of more than 100%. For example, goserelin is a ...
at the benzodiazepine site of
GABAA receptors,
with a
binding affinity
In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from Latin ''ligare'', which means 'to bind'. In protein-ligand binding, the ligand is usuall ...
of 0.77 nM at the α
1 subtype, 0.17 nM at α
2, 0.38 nM at α
3 and 0.11 nM at α
5.
It has been used to study the functional differences between the different subtypes of the GABA
A receptor.
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 ...
*
QH-II-66
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 ...
*
SH-053-R-CH3-2'F
References
{{GABAAR PAMs
Benzodiazepines