Furafylline

Biological Activity

Furafylline is a selective inhibitor of cytochrome P450IA2 (IC50 = 2.4 μM) and PDE (phosphodiesterase). Furafylline is a methyl xanthine derivative with an expanded duration of action in vivo than that of theophylline. Inhibition of CYP has the effect of slowing oxidative metabolism of xenobiotics, while inhibition of PDE prevents the hydrolysis of secondary messenger molecules, which in turn prolongs signal transduction and enhances its effects.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information

References

Characterization of chicken cytochrome P450 1A4 and 1A5: inter-paralog comparisons of substrate preference and inhibitor selectivity.
Yang J,et.al. Comp Biochem Physiol C Toxicol Pharmacol. 2013 May;337-43. PMID: 23474502.