Mirogabalin besylate is a potent and orally active ligand that selectively targets the α2δ subunit of voltage-gated calcium channels. It displays high affinity (K d ) values, namely 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 specifically targets the α2δ subunit of voltage-gated calcium channels, demonstrating varying binding affinities with dissociation constants (Kd) of 13.5 nM for human α2δ-1, 22.7 nM for human α2δ-2, 27 nM for rat α2δ-1, and 47.6 nM for rat α2δ-2. Additionally, it has shown a strong binding affinity to the gabapentin site in rat cortical brain homogenates, indicated by an IC50 value of 16.0 nM. Notably, at a concentration of 50 μM, mirogabalin does not impact any other receptors, channels, transporters, or enzymes [1].

Mirogabalin besylate, administered at doses of 3 and 10 mg/kg, significantly increases area under the curve (AUC) values for 0-8 hours in a dose-dependent manner in rats with partial sciatic nerve ligation. Additionally, doses of 2.5, 5, and 10 mg/kg of Mirogabalin significantly elevate AUC values for 0-12 hours, demonstrating dose-dependent analgesic enhancement, with estimated effective doses (ED) of 4.4 mg/kg on day 1, 3.1 mg/kg on day 3, and less than 2.5 mg/kg by day 5. Furthermore, at 3 and 10 mg/kg, Mirogabalin besylate does not significantly impact rota-rod performance or locomotor activity when administered orally but does show significant inhibition of rota-rod performance at higher doses of 10, 30, and 100 mg/kg, as well as decreases in locomotor activity at 30 and 100 mg/kg in rats [1].