SH-053-R-CH3-2′F is a drug used in scientific research which is a benzodiazepine derivative. It produces some of the same effects as other benzodiazepines, but is much more subtype-selective than most other drugs of this class, having high selectivity,

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 m ...

and efficacy at the α₅ subtype of the GABA_A receptor. This gives much tighter control of the effects produced, and so while SH-053-R-CH3-2′F retains sedative and

anxiolytic An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiet ...

effects, it does not cause

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 ...

at moderate doses. SH-053-R-CH3-2′F also blocks the

nootropic Nootropics ( , or ) (colloquial: smart drugs and cognitive enhancers, similar to adaptogens) are a wide range of natural or synthetic dietary supplement, supplements or drugs and other substances that are claimed to improve cognitive function ...

effects of the α₅-selective inverse agonist

PWZ-029 PWZ-029 is a benzodiazepine derivative drug with nootropic effects developed by WiSys,US Patent application US2006/258643 A1 It acts as a subtype-selective, mixed agonist-inverse agonist at the benzodiazepine binding site on the GABAA receptor ...

, so amnesia is also a likely side effect. Replacement of the ester function by an

amide In organic chemistry, an amide, also known as an organic amide or a carboxamide, is a compound with the general formula , where R, R', and R″ represent organic groups or hydrogen atoms. The amide group is called a peptide bond when it i ...

, realized in analogs such as MP-III-022 and

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 ...

, improves selectivity, efficacy, and kinetic behavior.

References

Ethynyl compounds Carboxylate esters Ethyl esters GABAA receptor positive allosteric modulators Hypnotics Imidazobenzodiazepines Fluoroarenes Sedatives {{pharma-stub

See also

References