Farampator has potential in treating disorders characterised by cognitive deficits such as Alzheimer's disease and schizophrenia. CX691 attenuates a scopolamine-induced impairment of cued fear conditioning following acute administration (0.1 mg/kg p.o.) and a temporally induced deficit in novel object recognition following both acute (0.1 and 1.0 mg/kg p.o.) and sub-chronic (bi-daily for 7 days) administration (0.01, 0.03, 0.1 mg/kg p.o.). It also improves attentional set-shifting following sub-chronic administration (0.3 mg/kg p.o.). Farampator (500 mg) unequivocally improves short-term memory but appeares to impair episodic memory. Furthermore, it tends to decrease the number of switching errors in the CTMT. Drug-induced side effects (SEs) included headache, somnolence and nausea. Subjects with SEs has significantly higher plasma levels of farampator than subjects without SEs.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Rats |
| Formulation | 1% methylcellulose |
| Dosages | 0.1, 0.3 and 1.0; 2 ml/kg |
| Administration | i.v. |
| Molecular Weight | 231.25 |
| Formula | C12H13N3O2 |
| CAS Number | 211735-76-1 |
| Form | Solid |
| Solubility (25°C) | 34 mg/mL in 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.
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