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].

HBT1 (0.01-100 μM) 通过依赖谷氨酸激活 AMPA 受体 (EC_₅₀ = 2.5 μM)，在原代神经元和 CHO 细胞中诱导钙离子内流，其 EC_₅₀ 分别为 1.3 和 4.6 μM^[1]。
HBT1 (0-10 μM) 在原代神经元和 CHO 细胞中均浓度依赖性地仅在存在 AMPA 的情况下增加 BDNF 蛋白水平，在没有 AMPA 的情况下未显示出 BDNF 蛋白水平的增加^[1]。
[³H]-HBT1 (1 nM-100 μM) 与天然 AMPA-R 结合，K_d 为 416 nM，并抑制大鼠海马膜，IC_₅₀ 为 0.28 μM^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

386.39

C₁₆H₁₇F₃N₄O₂S

489408-02-8

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

• [1]. Akiyoshi Kunugi, et al. HBT1, a Novel AMPA Receptor Potentiator with Lower Agonistic Effect, Avoided Bell-Shaped Response in In Vitro BDNF Production. J Pharmacol Exp Ther. 2018 Mar;364(3):377-389.  [Content Brief]