Mirogabalin besylate

1138245-21-2

C18H25NO5S

DMSO : 125 mg/mL (340.17 mM; Need ultrasonic)

Membrane Transporter/Ion Channel; Neuronal Signaling

Mirogabalin besylate is a selective and orally available ligand for the alpha2delta subunit of voltage-gated calcium channels, with K_ds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human alpha2delta-1, human alpha2delta-2, rat alpha2delta-1, and rat alpha2delta-2, respectively. IC50 & Target: Kd: 13.5 nM (Human alpha2delta-1), 22.7 nM (Human alpha2delta-2), 27 nM (Rat alpha2delta-1), 47.6 nM (Rat alpha2delta-2)^[1] In Vitro: Mirogabalin besylate is a ligand for the alpha2delta subunit of voltage-gated calcium channels, with K_ds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human alpha2delta-1, human alpha2delta-2, rat alpha2delta-1, and rat alpha2delta-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 uM^[1]. 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^[1].