Mirogabalin besylate is a ligand for the α2δ subunit of voltage-gated calcium channels, with Kds values of 13.5 nM, 22.7 nM, 27 nM and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1 and rat α2δ-2, respectively. Mirogabalin besylate has an affinity for the gabapentin binding site in rat cerebral cortical homogenate with an IC50 value of 16.0 nM. At a concentration of 50 μM, Mirogabalin besylate has no effect on other receptors, channels, transporters or enzymes[1].
Mirogabalin besylate 动物研究
Animal study
In a partial sciatic nerve ligation model rat, Mirogabalin besylate at doses of 3 mg and 10 mg/kg significantly increased AUC0-8 hour values in a dose-dependent manner. Mirogabalin besylate at doses of 2.5, 5 and 10 mg/kg significantly increased AUC0-12 hour values. sub>0-12 hour values and enhanced analgesic effect in a dose-dependent manner with ED50 values of 4.4, 3.1, and <2.5 mg/kg on days 1, 3, and 5, respectively. In addition, oral doses of Mirogabalin besylate at 3 mg and 10 mg/kg had no significant effect on rota-rod performance and locomotor activity in rats, while doses of 10 mg, 30 mg, and 100 mg/kg had a significant inhibitory effect on rota-rod performance, and doses of 30 mg and 100 mg/kg decreased locomotor activity in rats[1].
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