NEtPhOH-THPI, also known as N′-(2-methoxyphenylethyl)-THPI, is a serotonin 5-HT2 receptor agonist and possible serotonergic psychedelic of the tetrahydropyridinylindole (THPI) family related to psychedelic tryptamines.[1] It is a cyclized tryptamine with an NBOMe-like substitution.[1]

The drug is a potent and high-efficacy partial agonist of the serotonin 5-HT2A receptor.[1] Its affinity (Ki) for the receptor was 8.58 nM and its EC50Tooltip half-maximal effective concentration and EmaxTooltip maximal efficacy values were 20.7 nM (66.5%) for Gq signaling and 58.4 nM (80.7%) for β-arrestin2 signaling.[1] NEtPhOH-THPI is also a potent near-full agonist of the serotonin 5-HT2B receptor (EC50 = 7.94 nM; Emax = 88.9%) and a lower-potency full agonist of the serotonin 5-HT2C receptor (EC50 = 263 nM; Emax = 105.1%).[1] It is a weak serotonin reuptake inhibitor (IC50Tooltip half-maximal inhibitory concentration = 1,288 nM) as well.[1]

NEtPhOH-THPI induced the head-twitch response, a behavioral proxy of psychedelic effects, in rodents.[1] It produced the head-twitch response at a dose of 3 mg/kg in mice but not at a dose of 1 mg/kg or 10 mg/kg.[1] The drug produced about half the maximal number of head twitches as LSD.[1] The preclinical pharmacokinetics of NEtPhOH-THPI via intraperitoneal injection have been studied.[1]

NEtPhOH-THPI was first described in the scientific literature by Rongyan Li and colleagues by 2025.[1] A close non-hallucinogenic pyrrolopyridine analogue with antidepressant-like effects in rodents was also reported.[1] The chemical syntheses of both this compound and NEtPhOH-THPI were described.[1]

See also

References

  1. 1 2 3 4 5 6 7 8 9 10 11 12 13
source: https://en.wikipedia.org/wiki/NEtPhOH-THPI