TGF-8027 is a selective 5-HT2A receptor agonist capable of crossing the blood-brain barrier. It exhibits EC50 values of 3.3 nM for 5-HT2A, 160 nM for 5-HT2C, and 7600 nM for 5-HT2B receptors. In mice, TGF-8027 has an EC50 of 14 nM for 5-HT2A and 210 nM for 5-HT2C receptors. It can induce head-twitch responses in mice and is useful for researching diseases targeting the 5-HT2A receptor, such as depression.

5-HT2A receptor:3.3 nM (EC50)