Reparixin is a noncompetitive allosteric inhibitor of IL-8 (CXCL8) activation of CXCR1 and CXCR2 chemokine receptors with IC50 of 1 and 100 nM, respectively. Reparixin effectively decreased systolic blood pressure and increased the blood flow. Treatment with reparixin significantly counteracts secondary degeneration by reducing oligodendrocyte apoptosis, migration to the injury site of neutrophils and ED-1-positive cells.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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 Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Reparixin, an inhibitor of CXCR1 and CXCR2 receptor activation, attenuates blood pressure and hypertension-related mediators expression in spontaneously hypertensive rats.
Kim HY, et al. Biol Pharm Bull. 2011;34(1):120-7. PMID: 21212529.
Design of noncompetitive interleukin-8 inhibitors acting on CXCR1 and CXCR2.
Moriconi A, et al. J Med Chem. 2007 Aug 23;50(17):3984-4002. PMID: 17665889.
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