f11440

Eptapirone (F 11440) 是一种高效且选择性的 5-HT1A 受体激动剂，具有显着的抗抑郁和抗焦虑潜力。

Eptapirone, also known as F11440, is a potent 5HT(1A) receptor agonist with marked anxiolytic and antidepressant potential. The affinity of F 11440 for 5-HT1A binding sites (pKi, 8.33) was higher than that of buspirone (pKi, 7.50), and somewhat lower than that of flesinoxan (pKi, 8.91). In vivo, F 11440 was 4- to 20-fold more potent than flesinoxan, and 30- to 60-fold more potent than buspirone, in exerting 5-HT1A agonist activity at pre- and postsynaptic receptors in rats (measured by, for example, its ability to decrease hippocampal extracellular serotonin (5-HT) levels and to increase plasma corticosterone levels, respectively).

GSK-J1 sodium salt is a potent inhibitor of the H3K27 histone demethylases JMJD3 and UTX.