SH-I-048A (SH-i-048A) is a

benzodiazepine Benzodiazepines (BZD, BDZ, BZs), sometimes called "benzos", are a class of depressant drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring. They are prescribed to treat conditions such as anxiety disorders, ...

derivative related in structure to compounds such as

flubromazepam Flubromazepam is a benzodiazepine derivative which was first synthesized in 1960, but was never marketed and did not receive any further attention or study until late 2012 when it appeared on the grey market as a novel designer drug. It is a st ...

and

meclonazepam Meclonazepam ((''S'')-3-methylclonazepam) was discovered by a team at Hoffmann-La Roche in the 1970s and is a drug which is a benzodiazepine derivative similar in structure to clonazepam. It has sedative and anxiolytic actions like those of other ...

. 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 ...

at the benzodiazepine site of GABA_A 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 ''ligare'', which means 'to bind'. In protein-ligand binding, the ligand is usually a mo ...

of 0.77nM at the α₁ subtype, 0.17nM at α₂, 0.38nM at α₃ and 0.11nM at α₅. It has been used to study the functional differences between the different subtypes of the GABA_A receptor.

References

{{GABAAR PAMs Benzodiazepines GABAA receptor positive allosteric modulators

See also

References