1-Ethyl-6-hydroxytryptoline (1-Et-6-OH-THβC) is a serotonin 5-HT2 receptor agonist of the β-carboline family related to tryptoline. It is the 1-ethyl and 6-hydroxy derivative of tryptoline.
The drug has been found to act as a potent agonist of the serotonin 5-HT2A and 5-HT2C receptors, with () values of 195nM (85%) and 61nM (98%) in terms of Gq-mediated calcium flux, respectively. This is in notable contrast to other β-carbolines like harmine and harmaline, which are inactive as serotonin 5-HT2A receptor agonists. It is also in apparent contrast to tryptoline, which shows very low affinity for the serotonin 5-HT2A receptor (Ki = 3,900nM) and is inactive as an agonist of the serotonin 5-HT2B receptor (KB = >3,000nM).
The chemical synthesis of 1-ethyl-6-hydroxytryptoline has been described. An analogue, 1-(2,4,5-trimethoxyphenyl)-6-chlorotryptoline, is far more potent as a serotonin 5-HT2A and 5-HT2C receptor agonist in comparison.
1-Ethyl-6-hydroxytryptoline was described in the scientific literature by Meghan J. Orr and colleagues in 2022.
See also Substituted β-carboline List of miscellaneous serotonin 5-HT2A receptor agonists Shepherdine Pinoline Fenharmane 1-Ethyl-β-carboline
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