Ultrapotent PSEM agonist for PSAM4-GlyR and PSAM4-5HT3 (Ki values 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 applications
It strongly suppresses layer 2/3 cortical neurons expressing PSAM4-GlyR in brain slices at low concentrations (ranging from 1-15 nM).
Solubility & Handling
Soluble in water (100 mM)
This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use
Sold under license from the Howard Hughes Medical Institute, Janelia Research Campus.
For scientific research use only. This product may not be used to research, develop, make, use, offer to sell, sell, or import any products for human therapeutic uses.
References for uPSEM792 hydrochloride
References are publications that support the biological activity of the product
Ultrapotent chemogenetics for research and potential clinical applications.