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CYB210010 is an orally bioavailable, long-acting serotonin 5-HT2 receptor agonist that selectively targets 5-HT2A and 5-HT2C receptors (EC50: 4.1 n, 7.3 nM). CYB210010 can enter the central nervous system, cause a head twitch response (HTR), and is not prone to behavioral tolerance during chronic administration[1]. | [in vivo]
CYB210010 has certain oral bioavailability and can smoothly enter the central nervous system, bind to 5-HT2A receptors in the frontal cortex, and increase the expression of neuroplasticity-related genes in the frontal cortex[1].
CYB210010 (0.1-3 mg/kg; sc; single dose) causes a head twitch response (HTR) in mouse, and can be administered subchronically at threshold doses without developing behavioral tolerance[1].
| Animal Model: | Male C57BL/6J mice[1] | | Dosage: | 0.1, 0.3, 1, 3, mg/kg | | Administration: | sc; sigle dose | | Result: | Elicited maximum HTRs at ～15 min postadministration which terminated after 220 min (significant from vehicle from 5-160 min).
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| [IC 50]
5-HT1A Receptor: 32 nM (Ki); 5-HT1B Receptor: 949 nM (Ki); 5-HT6 Receptor: 1301 nM (Ki); 5-HT7 Receptor: 4918 nM (Ki); 5-HT2A Receptor: 4.1 nM (EC50); 5-HT2C Receptor: 7.3 nM (EC50); 5-HT2B Receptor: 88 nM (EC50) | [References]
[1] Varty GB, et al. Synthesis and Structure-Activity Relationships of 2,5-Dimethoxy-4-Substituted Phenethylamines and the Discovery of CYB210010: A Potent, Orally Bioavailable and Long-Acting Serotonin 5-HT2 Receptor Agonist. J Med Chem. 2024 Apr 25;67(8):6144-6188. DOI:10.1021/acs.jmedchem.3c01961 |
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