1-Methyltryptamine (1-methyl-T, 1-MT or 1-Me-T; code name PAL-637) is a serotonin receptor agonist and monoamine releasing agent of the tryptamine family. It is the 1-methyl derivative of tryptamine (T; PAL-235).
The drug is known to act as a serotonin 5-HT<sub>2A</sub> receptor agonist (K<sub>i</sub> = 473nM; = 209âÂÂ4,560nM; = 55âÂÂ99%), as a serotonin releasing agent ( = 53.1nM), and to be inactive in inducing the release of norepinephrine and dopamine ( = >10,000nM). Its activities at other serotonin receptors were not reported. 1-Methyltryptamine shows dramatically reduced affinity and activational potency as well as reduced efficacy at the serotonin 5-HT<sub>2A</sub> receptor compared to tryptamine (which showed K<sub>i</sub> = 13.1nM; = 7.36âÂÂ99nM; = 101âÂÂ104%). It also shows slightly reduced potency as a serotonin releasing agent and abolished activity as a releaser of norepinephrine and dopamine relative to tryptamine (which had = 32.6nM, 716nM, and 164nM, respectively).
Analogues of 1-methyltryptamine, like 1-methylserotonin and 1-iPr-5-MeO-T, have been studied. Similarly to the case of 1-methyltryptamine contrasted with tryptamine, they show dramatically reduced affinities and activational potencies at the human serotonin 5-HT<sub>2A</sub> receptor relative to their 1-unsubstituted counterparts (serotonin and 5-methoxytryptamine, respectively).