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Rilmazafone

Cat. No. M30992
Rilmazafone Structure
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Biological Activity

Rilmazafone is a benzodiazepine (omega) ligand and an orally active sleep inducer.

Chemical Information
Molecular Weight 475.33
Formula C21H20Cl2N6O3
CAS Number 99593-25-6
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Robert Kronstrand, et al. J Anal Toxicol. Rilmazafone: A designer benzodiazepine pro-drug involved in fatal intoxications

[2] Masami Tsuchiya, et al. Drugs Real World Outcomes. Itraconazole Contaminated with Rilmazafone in Japan: A Retrospective Analysis Using the Japanese Adverse Drug Event Report Database

[3] Sachiko Ito Uemura, et al. Sleep Med. Residual effects of zolpidem, triazolam, rilmazafone and placebo in healthy elderly subjects: a randomized double-blind study

[4] K Sugaya, et al. J Int Med Res. Effects of melatonin and rilmazafone on nocturia in the elderly

[5] M Koike, et al. Xenobiotica. Structure determination of metabolites of rilmazafone, a 1H-1,2,4-triazolyl benzophenone derivative in monkey urine

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