CYB210010, a long-acting, orally bioavailable serotonin 5-HT2 receptor agonist, selectively targets 5-HT2A and 5-HT2C receptors (EC 50: 4.1 n, 7.3 nM). It can penetrate the central nervous system, induce a head twitch response (HTR), and does not exhibit behavioral tolerance with chronic use [1].

5-HT1B receptor:949 nM (Ki), 5-HT6 receptor:1301 nM (Ki), 5-HT1A receptor:32 nM (Ki), 5-HT2A receptor:4.1 nM (EC50), 5-HT2C receptor:7.3 nM (EC50), 5-HT7 receptor:4918 nM (Ki), 5-HT2B receptor:88 nM (EC50)

CYB210010 shows oral bioavailability, successfully penetrates the central nervous system, binds to frontal cortex 5-HT2A receptors, and enhances the expression of genes related to neural plasticity in the frontal cortex [1]. Administered subcutaneously in single doses of 0.1-3 mg/kg, CYB210010 induces head-twitch responses (HTR) in male C57BL/6J mice and can be repeatedly administered at threshold doses without leading to behavioral tolerance [1]. Maximum HTRs occur approximately 15 minutes post-administration and end after 220 minutes, with a significant effect from the vehicle observed between 5 and 160 minutes.