Tozadenant (SYN115) is an adenosine A2A receptor antagonist(Ki of 11.5 nM and 6 nM on human and rhesus,respectively)

A2A receptor (human):11.5 nM(Ki) , A2A receptor (rhesus):6 nM(Ki)

与单独测试的药物相比，Radiprodil和Tozadenant的组合显著提高了MPTP处理的狨猴的运动活性，并改善了其运动障碍。此外，该组合带来的运动功能恢复几乎完全没有不自主运动障碍[1]。

Before initiating the Radiprodil & Tozadenant combination experiment, 14 primates were challenged with a dose of 8 mg/kg (po) of L-Dopa and behaviour was recorded for 5 hours. This "Pre-L-Dopa-test" was used to select the 12 subjects required for the study. Their response to the L-Dopa challenge was subsequently used as a comparator to the ensuing response to the different drug treatments and combinations. The effects of the drugs alone or in combination were assessed after acute oral gavage.This experiment investigated the effects on motor deficits of Radiprodil plus Tozadenant twice daily at an interval of 5 hrs according to a modified Latin square design in n = 12 MPTP-treated marmosets. At the time of the second drugs administration a novel object (cotton reel, table tennis ball) was placed into the cage. The four different treatments were (1) Tozadenant (150 mg/kg) plus Radiprodil (2.0 mg/kg), (2) Tozadenant (150 mg/kg) plus vehicle, (3) Radiprodil (2.0 mg/kg) plus vehicle, (4) vehicle[1].