Selective, ultrapotent PSEM agonist for PSAM4-GlyR and PSAM4-5HT3 (Ki values are 0.15 nM and and EC50 = 0.3 nM at PSAM4-GlyR) which can be used for targeted control of brain activity in rodent and primate models.
It has excellent selectivity with 5000- to 10,000-fold selectivity for PSAM4-GlyR over α-7-GlyR, α7-5HT3R and 5-HT3R. It also does not show evident α4β2 nAChR agonism up to 30 µM.
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
Storage buffer
Soluble in DMSO (100 mM), and in water (50 mM, gentle warming)
Storage instructions
-20°C
Storage of solutions
Prepare and use solutions on the same day if possible. Store solutions at -20°C for up to one month if storage is required. Equilibrate to RT and ensure the solution is precipitate free before use.
Shipping Conditions
Stable for ambient temperature shipping. Follow storage instructions on receipt.
Important
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.