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L-655,708 (FG-8094) is a nootropic drug invented in 1996 by a team working for Merck, Sharp and Dohme, that was the first compound developed which acts as a subtype-selective inverse agonist at the α5 subtype of the benzodiazepine binding site on the GABAA receptor. It acts as an inverse agonist at the α1, α2, α3 and α5 subtypes, but with much higher affinity for α5, and unlike newer α5 inverse agonists such as α5IA, L-655,708 exerts its subtype selectivity purely via higher binding affinity for this receptor subtype, with its efficacy as an inverse agonist being around the same at all the subtypes it binds to.

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  • L-655,708 (en)
  • L-655,708 (it)
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  • L-655,708 (FG-8094) is a nootropic drug invented in 1996 by a team working for Merck, Sharp and Dohme, that was the first compound developed which acts as a subtype-selective inverse agonist at the α5 subtype of the benzodiazepine binding site on the GABAA receptor. It acts as an inverse agonist at the α1, α2, α3 and α5 subtypes, but with much higher affinity for α5, and unlike newer α5 inverse agonists such as α5IA, L-655,708 exerts its subtype selectivity purely via higher binding affinity for this receptor subtype, with its efficacy as an inverse agonist being around the same at all the subtypes it binds to. (en)
  • Il L-655,708 è uno psicofarmaco appartenente alla categoria delle ; è un farmaco nootropico inventato nel 1996 da un team che lavora per Merck, Sharp e Dohme, ed è stato il primo composto sviluppato che agisce come agonista inverso selettivo dal sottotipo α1 al sottotipo α5 del recettore GABA A. Uno studio del 2015 ha rilevato che L-655.708 e un altro modulatore allosterico negativo selettivo del recettore GABA A contenente α5, l'MRK-016, hanno prodotto effetti antidepressivi rapidi simili alla ketamina in modelli animali di depressione. (it)
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