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AP521 is an agonist of human 5-HT1A receptor with an IC50 of 94 nM. | [in vivo]
AP521 significantly increases the number of shock acceptances [F(5,105)=4.46, P<0.01] at doses between 0.5 to 10 mg/kg. Oral administration of AP521 at 3 and 10 mg/kg significantly decreases freezing time [F(3,60)=2.89, P<0.05]. AP521 significantly increases the time spent on the open arms by approximately 2-fold as compare to the vehicle treated group [F(3, 36)=4.21, P<0.05 for AP521]. The anxiolytic-like effect of AP521 appears to be dose-related. AP521 significantly increases the extracellular 5-HT level of the medial prefrontal cortex (mPFC) at 10 mg/kg from 0.5 to 1 h after administration. AP521 at 3 mg/kg tends to increase the extracellular 5-HT level, however, this increase is not significant[1]. | [IC 50]
5-HT1A Receptor: 94 nM (IC50, in human); 5-HT1A Receptor: 135 nM (IC50, in rat); 5-HT1B Receptor: 254 nM (IC50, in rat); 5-HT1B Receptor: 5530 nM (IC50, in human); 5-HT1D Receptor: 418 nM (IC50, in human); 5-HT5A Receptor: 422 nM (IC50, in human); 5-HT7 Receptor: 198 nM (IC50, in rat) | [References]
[1] Kasahara K, et al. The effects of AP521, a novel anxiolytic drug, in three anxiety models and on serotonergic neural transmission in rats. J Pharmacol Sci. 2015 Jan;127(1):109-16. DOI:10.1016/j.jphs.2014.11.008 |
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