AZD7325 is an α2,3-subtype-selective GABA-A-receptor modulator. It shows much higher binding affinity at the α2,3-subunits (Ki = 0.3nM and 1.3nM, respectively) over the α5-subunit (Ki = 230nM) [1]. AZD7325 at a dosage of 31.6mg/kg significantly prolonged the decay time of miniature inhibitory postsynaptic currents (IPSCs) recorded from the CA1 neurons collected from mice on the 129 background strain. AZD7325 treatment also significantly prolonged the decay time of asynchronous IPSCs in the perisomatic synapses in both F1 and 129 strains. AZD7325 at doses of 10, 17.8, and 31.6mg/kg exhibited a significant protective effect against seizure induction in F1.Scn1a+/- mice[2].
作用机制
AZD7325 is allosteric GABA-A-receptor modulator that demonstrates relatively potent positive modulation at the α2,3-subunits, neutral antagonism at the α1 subunit, and weak affinity for the α5 subunit[1].
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