6,10-Methano-2H-pyrazino[2,3-h][3]benzazepin-2-one, 1,6,7,8,9,10-hexahydro-1-methyl-, hydrochloride (1:1)

Biological Activity

Ultrapotent PSEM agonist for PSAM4-GlyR and PSAM4-5HT3 (Kivalues are 0.7 nM and <10 nM for PSAM4-GlyR and PSAM4-5HT3 respectively) which can be used for targeted control of brain activity in rodent and primate models.It shows >10,000-fold agonist selectivity for PSAM4-GlyR over α-7-GlyR, α7-5HT3R and 5-HT3R.uPSEM792 is a very weak agonist at α4β2 nAChR and shows 230-fold selectivity for PSAM4-GlyR over α4β2 nAChR.It retains the potency of varenicline for PSAM4-GlyR with enhanced chemogenetic selectivity.It does not act as a P-glycoprotein pump (PgP) substrate.Uses and applicationsIt strongly suppresses layer 2/3 cortical neurons expressing PSAM4-GlyR in brain slices at low concentrations (ranging from 1-15 nM).

storage

-20°C