Mirogabalin besylate,1138245-2

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Mirogabalin besylate

CAS No. : 1138245-21-2

MCE 国际站：Mirogabalin besylate

产品活性：Mirogabalin besylate 是一种选择性的，可口服的电压门控性钙通道 (voltage-gated calcium channels) 亚基 α2δ 的有效配体，对人 α2δ-1 和 α2δ-2，大鼠 α2δ-1 和 α2δ-2 的 K_d 值分别为 13.5 nM，22.7 nM，27 nM 和 47.6 nM。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：Calcium Channel

In Vitro: Mirogabalin besylate is a ligand for the α2δ subunit of voltage-gated calcium channels, with K_ds 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 shows binding affinity for the gabapentin binding site in rat cortical brain homogenates with the IC₅₀ value of 16.0 nM. Mirogabalin has no effect on any other receptors, channels, transporters, or enzymes at 50 μM.

In Vivo: Mirogabalin besylate (3 and 10 mg/kg) markedly increases AUC0-8 hours values in a dose-dependent manner in partial sciatic nerve ligation model rats. Mirogabalin (2.5, 5, and 10 mg/kg) causes significant and dose-dependent increase in AUC_0-12 hours values and enhances analgesic effects, with estimated ED₅₀ of 4.4, 3.1, and <2.5 mg/kg on day 1, day 3, and day 5, respectively. Moreover, Mirogabalin besylate shows no obvious effect on rota-rod performance and locomotor activity at 3 and 10 mg/kg via oral administration, exhibits significant inhibition on rota-rod performance at 10, 30, and 100 mg/kg, and decreases locomotor activity at 30 and 100 mg/kg in rats.

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