L-838,417
L-838,417 is a sedative and anxiolytic drug in the benzodiazepine class. It has selective effects for GABA receptors in the brain, and has a fast onset of effects and short duration of action. It was developed by a team at Merck & Co. and can be used in scientific research.
Pharmacology[edit | edit source]
L-838,417 is a partial agonist at GABAA receptors. It has a high binding affinity for the alpha 2 and alpha 3 subtypes of GABAA receptors, which are thought to be the subtypes most closely associated with the anxiolytic effects of benzodiazepine drugs. It also has a moderate affinity for the alpha 5 subtype, and a low affinity for the alpha 1 subtype, which is associated with sedation and amnesia.
Uses[edit | edit source]
L-838,417 has been used in scientific research to investigate the role of different GABAA receptor subtypes in the action of benzodiazepine drugs. It has also been used in animal studies to investigate the effects of benzodiazepines on anxiety and other behaviors.
Side Effects[edit | edit source]
As with other benzodiazepines, L-838,417 can cause side effects such as sedation, amnesia, and dependence. However, because it is a partial agonist and has a low affinity for the alpha 1 subtype of GABAA receptors, it may cause fewer side effects than other benzodiazepines.
See Also[edit | edit source]
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Contributors: Prab R. Tumpati, MD