AZD6765, a low-trapping NMDA channel blocker in development for major depression, is predicted to have an improved tolerability profile compared to ketamine. Preclinically, NMDA channel blockers increase gamma-band EEG - a potential therapeutic biomarker of cortical disinhibition. Significant increases in gamma-band EEG were observed at 1 hour for AZD6765 and ketamine, and baseline-corrected gamma-band EEG following AZD6765 150 mg was statistically indistinguishable from that observed following ketamine. AZD6765 demonstrated NMDA channel blockade and an improved tolerability profile compared to ketamine. AZD6765 demonstrated NMDA channel blockade and an improved tolerability profile compared to ketamine.
| Molecular Weight | 198.26 |
| Formula | C13H14N2 |
| CAS Number | 153322-05-5 |
| Form | Liquid |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[4] Ioline D Henter, et al. Glutamatergic Modulators in Depression
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