| Identification | Back Directory | [Name]
6,10-Methano-2H-pyrazino[2,3-h][3]benzazepin-2-one, 1,6,7,8,9,10-hexahydro-1-methyl-, hydrochloride (1:1) | [CAS]
2341841-08-3 | [Synonyms]
6,10-Methano-2H-pyrazino[2,3-h][3]benzazepin-2-one, 1,6,7,8,9,10-hexahydro-1-methyl-, hydrochloride (1:1) | [Molecular Formula]
C14H16ClN3O | [MOL File]
2341841-08-3.mol | [Molecular Weight]
277.75 |
| Hazard Information | Back Directory | [Uses]
uPSEM792 hydrochloride is a PSAM4-GlyR agonist[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 | [References]
[1] Magnus C J, et al. Ultrapotent chemogenetics for research and potential clinical applications[J]. Science, 2019, 364(6436): eaav5282. DOI:10.1126/science.aav5282 |
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Merck KGaA
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www.sigmaaldrich.cn |
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