CPI-CG-8, also known as N-methyl-N-(2-indolylethyl)tryptamine, is a "relatively" selective serotonin 5-HT2C receptor agonist of the tryptamine family. Slides. Slide #28. "[Slide 28:] First Round of Generative Design Validation: Starting point Psilocin. 5-HT2C agonists - obesity, psychiatric disorders, sexual dysfunction and urinary incontinence. 10 molecules synthesized - tested vs 5-HT2A, 2B, 2C at Eurofins at 1µM. 1 compound was selective vs 5-HT2C 99.4% inhibition - retested in dose response. CPI-CG-8 EC50 = 12.46nM, Serotonin (control) = 1.9 nM, (reference Lorcaserin = 9 nM). MACCS similarity to psilocin: 0.67 - IP dosing in mice - good brain levels. [Figures]. Jones et al., Manuscript submitted, Provisional patent submitted."
At the serotonin 5-HT2C receptor, it showed 99.4% binding inhibition (a measure of affinity) at a concentration of 1,000nM, had an activational potency () of 12.46nM, and showed an activational efficacy () of approximately 80%. The pharmacokinetics of CPI-CG-8 in rodents have been studied.
The drug was developed by Collaborations Pharmaceuticals and was derived via modification of the psychedelic drug psilocin using generative machine learning through a platform called MegaSyn. CPI-CG-8 was first described in the scientific literature by 2024. It is of interest for the potential treatment of opioid use disorder and other conditions.
See also Substituted tryptamine Serotonin 5-HT2C receptor agonist N-Benzyltryptamine NEtPhOH-THPI
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