L-838,417 is an anxiolytic drug used in scientific research. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic. The compound was developed by Merck, Sharp and Dohme.
L-838,417 is a subtype-selective GABAA positive allosteric modulator, acting as a partial agonist at ?2, ?3 and ?5 subtypes. However, it acts as a negative allosteric modulator at the ?1 subtype, and has little affinity for the ?4 or ?6 subtypes. This gives it selective anxiolytic effects, which are mediated mainly by ?2 and ?3 subtypes, but with little sedative or amnestic effects as these effects are mediated by ?1. Some sedation might still be expected due to its activity at the ?5 subtype, which can also cause sedation, however no sedative effects were seen in animal studies even at high doses, suggesting that L-838,417 is primarily acting at ?2 and ?3 subtypes with the ?5 subtype of lesser importance.
As might be predicted from its binding profile, L-838,417 substitutes for the anxiolytic benzodiazepine chlordiazepoxide in animals, but not for the hypnotic imidazopyridine drug zolpidem. The synthesis of L-838,417 and similar compounds was described in 2005 in the Journal of Medicinal Chemistry.
Video L-838,417
See also
- ?5IA
- SL-651,498
Maps L-838,417
References
Source of the article : Wikipedia
0 Comments