1698901-76-6
1698901-76-6 structure
- Name: GNE-8324
- Chemical Name: GNE-8324
- CAS Number: 1698901-76-6
- Molecular Formula: C18H18FN3OS
- Molecular Weight: 343.11
- Create Date: 2020-01-20 19:18:56
- Modify Date: 2024-02-05 00:06:01
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GNE-8324 is a potent and selective NMDA receptor PAM.
| Name | GNE-8324 |
|---|
| Description | GNE-8324 is a potent and selective NMDA receptor PAM. |
|---|---|
| In Vitro | Both GNE-6901 and GNE-8324 increase Glu potency, whereas neither PAM had significant effects on glycine (Gly) potency. Furthermore, both compounds slowed channel deactivation kinetics. However, GNE-8324 caused significantly slower NMDAR current deactivation following the termination of Glu application, compared to GNE-6901. Interestingly, when Gly was removed following the rapid Glu/Gly application in the constant presence of Glu, NMDAR currents rapidly deactivated in the presence of either GNE-6901 or GNE-8324, which is in sharp contrast to the slower NMDAR current deactivation in the presence of GNE-8324 when Gly was not removed. The authors argued that this demonstrated a specific interaction of PAMs with Glu but not Gly. However, these data also suggest that the slower NMDAR current deactivation in the presence of GNE-8324, but not GNE-6901, is highly dependent on ambient Gly concentration. GNE-8324 also markedly increased potency of Glu at GluN1/GluN2A NMDARs by about 10-fold while GNE-6901 had a much smaller effect on Glu potency. Finally GNE-8324 potency was strongly dependent on Glu concentration, whereas Glu concentration had only a modest effect on GNE-6901 potency. The deferential effects of GNE-6901 and GNE-8324 on GluN1/GluN2A NMDAR function could reflect subtle differences in modes of action of these closely related compounds, which might lead to distinct actions on NMDAR modulation in physiological settings. |
| Molecular Formula | C18H18FN3OS |
|---|---|
| Molecular Weight | 343.11 |