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-HT 1A Receptor:32 nM (Ki), 5-HT 6 Receptor:1301 nM (Ki), 5-HT 1B Receptor:949 nM (Ki)

CYB210010具有一定的口服生物利用度，可进入中枢神经系统，并与额叶皮层的5-HT2A受体结合，从而增加额叶皮层相关基因的神经可塑性表达 [1]。CYB210010 (0.1-3 mg/kg; sc; 单剂量) 会引起小鼠的头部抽搐反应 (HTR)，且以阈值剂量亚慢性给药时不会产生行为耐受性 [1]。Animal Model: Male C57BL/6J mice [1] Dosage: 0.1, 0.3, 1, 3 mg/kg Administration: sc; single dose Result: Elicited maximum HTRs at ∼15 min postadministration which terminated after 220 min (significant from vehicle from 5-160 min).