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Submit ReviewuPSEM 792 hydrochloride
Description: Highly potent PSAM4-GlyR and PSAM4-5-HT3 chimeric ion channel agonist; brain-penetrant
Chemical Name: 1-Methyl-7,8,9,10-tetrahydro-1H-6,10-methanoazepino[4,5-g]quinoxalin-2(6H)-one hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for uPSEM 792 hydrochloride
uPSEM 792 hydrochloride is an ultrapotent PSEM (uPSEM) agonist for PSAM4-GlyR and PSAM4-5HT3 (Ki = 0.7 nM for PSAM4-GlyR and <10 nM for PSAM4-5HT3). Exhibits >10,000-fold agonist selectivity for PSAM4-GlyR over α7-GlyR, α7-5HT3, and 5HT3-R, and 230-fold selectivity over α4β2 nAChR. Also weak partial agonist (~10 %) at α4β2 nAChR. Retains the potency of varenicline (Cat.No. 3754) for PSAM4-GlyR with enhanced chemogenetic selectivity. Does not act as a substrate for P-glycoprotein pumps. Silences neurons in vivo. Brain-penetrant.
Licensing Information
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.
Technical Data for uPSEM 792 hydrochloride
| M. Wt | 277.75 |
| Formula | C14H15N3O.HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2341841-08-3 |
| InChI Key | CDHPEJUYEXNGCV-UHFFFAOYSA-N |
| Smiles | O=C1C=NC2=C(C=C3C(C4CNCC3C4)=C2)N1C.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for uPSEM 792 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 27.77 | 100 |
Preparing Stock Solutions for uPSEM 792 hydrochloride
The following data is based on the product molecular weight 277.75. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.6 mL | 18 mL | 36 mL |
| 5 mM | 0.72 mL | 3.6 mL | 7.2 mL |
| 10 mM | 0.36 mL | 1.8 mL | 3.6 mL |
| 50 mM | 0.07 mL | 0.36 mL | 0.72 mL |
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Product Datasheets for uPSEM 792 hydrochloride
References for uPSEM 792 hydrochloride
References are publications that support the biological activity of the product.
Magnus et al (2019) Ultrapotent chemogenetics for research and potential clinical applications. Science doi: 10.1126/science PMID: 30872534
If you know of a relevant reference for uPSEM 792 hydrochloride, please let us know.
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3 Citations for uPSEM 792 hydrochloride
Citations are publications that use Tocris products. Selected citations for uPSEM 792 hydrochloride include:
Perez-Sanchez et al (2023) A humanized chemogenetic system inhibits murine pain-related behavior and hyperactivity in human sensory neurons Sci.Transl.Med 15 eadh3839 PMID: 37792955
Ji-Hye et al (2023) Neocortical synaptic engrams for remote contextual memories. Nat Neurosci 26 259-273 PMID: 36564546
Manuel et al (2022) Extrinsic control and intrinsic computation in the hippocampal CA1 circuit. Neuron 110 658-673.e5 PMID: 34890566
Do you know of a great paper that uses uPSEM 792 hydrochloride from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Chemogenetics Research Bulletin
Produced by Tocris, the chemogenetics research bulletin provides an introduction to chemogenetic methods to manipulate neuronal activity. It outlines the development of RASSLs, DREADDs and PSAMs, and the use of chemogenetic compounds. DREADD ligands and PSEMs available from Tocris are highlighted.