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CYB210010 is a potent, selective, long-acting, and orally active agonist for the serotonin 5-HT2A and 5-HT2C receptors. It belongs to the phenethylamine family and is structurally related to compounds such as 2C-T and 2C-T-21. The compound was first synthesized by Geoffrey Varty and colleagues at Cybin in 2023. Preclinical studies show that CYB210010 has high affinity (K\(_i\) = 0.35 nM) for the serotonin 5-HT2A receptor with EC\(_{50}\) values of 4.1 nM (5-HT2A) and 7.3 nM (5-HT2C), while showing much lower activity at the serotonin 5-HT2B receptor (88 nM). It produces psychedelic-like responses in animal models without behavioral tolerance upon subchronic administration at threshold doses. The drug is orally bioavailable across multiple species, crosses into the CNS efficiently, engages frontal cortex receptors involved in neuroplasticity gene expression, and lacks significant activity at monoamine transporters or over seventy other proteins tested preclinically[1][3][4][6][7]. As of mid-2024 it remains a preclinical tool molecule for investigating therapeutic potential of serotonergic psychedelics in psychiatric and neurological disorders.
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