L-371,257
L-371,257 is an anxiolytic drug used in scientific research, which acts as a selective inverse agonist for the benzodiazepine site of the GABA_A receptor.
Chemistry[edit | edit source]
L-371,257 is a benzodiazepine derivative, and its full chemical name is 8-acetylene-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine. It is structurally distinct from most benzodiazepine drugs, with the triazolo ring system replaced by a cyclohexene ring, and an acetylene group in the 8-position of the benzodiazepine ring system.
Pharmacology[edit | edit source]
L-371,257 acts as a selective inverse agonist for the omega-6 (also known as the benzodiazepine) site of the GABA_A receptor. This means it reduces the activity of the GABA_A receptor, the most prolific inhibitory receptor within the brain. Its effects are therefore opposite to those of benzodiazepine drugs, which enhance GABA_A activity.
Uses[edit | edit source]
L-371,257 is used primarily in scientific research. It is particularly useful in the study of GABA_A receptor subtypes, and the role of these receptors in the development of anxiety and other psychological disorders.
See also[edit | edit source]
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