uPSEM 792 hydrochloride is a 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.
Caractéristiques techniques
| Marque | Tocris Bioscience |
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| Réf. B-LABO | BL-RE-125701 |
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| Réf. fabricant | 18769956 |
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| Nom chimique ou matériau | 1-Methyl-7,8,9,10-tetrahydro-1 H-6,10-methanoazepino[4,5-g]quinoxalin-2(6 H)-one hydrochloride |
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| CAS | 2341841-08-3 |
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| Quantité | 25 mg |
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| Cible | Pharmacologically Selective Effector Molecules/PSEM |
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| Formule moléculaire | C<sub>14</sub>H<sub>15</sub>N<sub>3</sub>O.HCl |
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| Poids de la formule | 277.75 |
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| Pureté | 98% |
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