TGF-8027 is a selective 5-HT 2A agonist that can cross the blood-brain barrier. TGF-8027 exhibits EC 50 s of 3.3 nM, 160 nM and 7600 nM against human 5-HT 2A, 5-HT 2C and 5-HT 2B and exhibits EC 50 s against mouse 5-HT 2A and mouse 5-HT 2C of 14 and 210 nM. TGF-8027 can induce a head-shaking response in mice. TGF-8027 can be used to study diseases that target the 5-HT 2A receptor (such as depression ) [1].
In Vivo, TGF-8027 (0.4-40 mg/kg, s.c., single dose) induces a head-shaking response in mice in a dose-dependent manner with an EC50 of 1.86 mg/kg[1].
References:
[1]. Fenske TG, et al. Discovery of Highly Selective 5-HT2A Agonists Using Structure-Guided Design. J Med Chem. 2025 Oct 9;68(19):20619-20635.
In Vivo, TGF-8027 (0.4-40 mg/kg, s.c., single dose) induces a head-shaking response in mice in a dose-dependent manner with an EC50 of 1.86 mg/kg[1].
References:
[1]. Fenske TG, et al. Discovery of Highly Selective 5-HT2A Agonists Using Structure-Guided Design. J Med Chem. 2025 Oct 9;68(19):20619-20635.