BGC-201259 (RS-1259) is an orally active inhibitor that simultaneously targets acetylcholinesterase (AChE) (IC50 = 101 nM) and serotonin transporter (SERT) (IC50 = 42 nM). BGC-201259 inhibits 5-HT receptor with an IC50 of 90 nM. BGC-201259 exhibits strong weak activity against the NA transporter (IC50 = 7.7 µM), L-type calcium channel (IC50 = 3.6 µM), sigma receptor (IC50 = 2 µM), and sodium channel (IC50 = 5.1 µM). BGC-201259 demonstrates synergistic potential in improving cognitive and emotional symptoms by balancing the inhibition of these two targets. BGC-201259 can be used in research on Alzheimers disease[1][2].
