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Radequinil

Cat. No. M29341
Radequinil Structure
Synonym:

AC-3933

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Biological Activity

Radequinil (AC-3933) is a benzodiazepine receptor (BzR) partial inverse agonist. AC-3933 binds to GABA(-) and GABA(+) ligand with Kis of 5.15 and 6.11 nM, respectively.

Chemical Information
Molecular Weight 334.33
Formula C18H14N4O3
CAS Number 219846-31-8
Form Solid
Solubility (25°C) DMSO 10 mg/mL (ultrasonic and warming and heat to 60°C)
Storage 4°C, protect from light, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Takashi Hashimoto, et al. Pharmacol Biochem Behav. AC-3933, a benzodiazepine partial inverse agonist, improves memory performance in MK-801-induced amnesia mouse model

[2] Takashi Hashimoto, et al. Eur J Pharmacol. Procognitive effect of AC-3933 in aged mice, and synergistic effect of combination with donepezil in scopolamine-treated mice

[3] Y Hatayama, et al. Neuroscience. In vivo pharmacological characterization of AC-3933, a benzodiazepine receptor partial inverse agonist for the treatment of Alzheimer's disease

[4] T Hashimoto, et al. Neuroscience. Pharmacological properties of AC-3933, a novel benzodiazepine receptor partial inverse agonist

[5] Masashi Mise, et al. Drug Metab Dispos. Polymorphic expression of CYP1A2 leading to interindividual variability in metabolism of a novel benzodiazepine receptor partial inverse agonist in dogs

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