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 and
efficacy at the
α5 subtype of the
GABAA receptor. This gives much tighter control of the effects produced, and so while SH-053-R-CH3-2′F retains
sedative and
anxiolytic effects, it does not cause
ataxia at moderate doses.[1] SH-053-R-CH3-2′F also blocks the
nootropic effects of the α5-selective
inverse agonistPWZ-029, so
amnesia is also a likely side effect.[2]
Replacement of the ester function by an
amide, realized in analogs such as MP-III-022 and
GL-II-73, improves selectivity, efficacy, and kinetic behavior.[3][4][5]
^CA 3016491, Cook JM, Li G, Poe M, Savic M, Sibille E, "Treatment of cognitive and mood symptoms in neurodegenerative and neuropsychiatric disorders with alpha5-containing gabaa receptor agonists."
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 and
efficacy at the
α5 subtype of the
GABAA receptor. This gives much tighter control of the effects produced, and so while SH-053-R-CH3-2′F retains
sedative and
anxiolytic effects, it does not cause
ataxia at moderate doses.[1] SH-053-R-CH3-2′F also blocks the
nootropic effects of the α5-selective
inverse agonistPWZ-029, so
amnesia is also a likely side effect.[2]
Replacement of the ester function by an
amide, realized in analogs such as MP-III-022 and
GL-II-73, improves selectivity, efficacy, and kinetic behavior.[3][4][5]
^CA 3016491, Cook JM, Li G, Poe M, Savic M, Sibille E, "Treatment of cognitive and mood symptoms in neurodegenerative and neuropsychiatric disorders with alpha5-containing gabaa receptor agonists."