HBT1

HBT1 is an effective AMPA receptor AMPA-R potentiator. HBT1 specifically binds to the ligand-binding domain (LBD) of AMPAR and enhances receptor activity only when AMPA is present., HBT1 has almost no agonistic effect (i.e., reaching the optimal concentration, and then the efficacy decreases as the concentration continues to increase) compared with traditional AMPA-R potentiator, avoiding the bell-shaped reaction of brain-derived neurotrophic factor (BDNF) production in primary neurons. HBT1 can be applicable to a wider range of neurological and psychiatric diseases (such as depression, Alzheimer's disease, etc.)^[1]. In Vitro:HBT1 (0.01-100 μM) activates AMPA receptors through glutamate dependence (EC_₅₀ = 2.5 μM), inducing calcium ion influx in primary neurons and CHO cells with EC_₅₀ values of 1.3 and 4.6 μM, respectively^[1].
HBT1 (0-10 μM) concentration-dependently increases BDNF protein levels in the presence of AMPA and shows no increase of BDNF protein levels in the absence of AMPA in primary neurons and CHO cells^[1].
[³H]-HBT1 (1 nM-100 μM) binds native AMPA-R with a K_d of 416 nM and inhibits rat hippocampal membranes with an IC_₅₀ of 0.28 μM^[1].