ZK200775 (hydrate)

In the cortical slice preparation assay, ZK200775 (hydrate) gave Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively. In the spreading depression assay, it gave IC50 values of 200 nM , 76 nM, 13 μM, and 18 μM against quisqualate, kainate, NMDA, and glycine [1].

ZK200775 (hydrate) elevated the threshold for AMPA- and kainate-induced clonic seizures in mice with a THRD50 (threshold dose) of 2.9 (1.7–4.6) and 1.6 (1.3–2.0) mg/kg iv, whereas the threshold for NMDA-induced seizures was elevated only in doses, THRD50 of 24.1 (21.9–26.5) mg/kg iv, which affected motor coordination in the rotating rod, ED50 14.6 (12.1–17.6) mg/kg. It in doses of 10 and 30 mg/kg iv reduced muscle tone in genetically spastic rats [1]. It (3.0 but not 1.5 or 6.0 mg/kg) significantly decreased the nicotine-induced (0.6 mg/kg) DA release in the NAcc and nicotine-stimulated LMA . It (1.5, 3.0, 6.0 mg/kg) alone influenced neither DA release nor LMA. It showed 34-fold selectivity for AMPA receptors compared to NMDA receptors and no affinity to nicotine receptors [2].