BGC-201259

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), σ 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 Alzheimer's disease^[1][2]. In Vivo:BGC-201259 (1 and 10 mL/kg, p.o., single dose) inhibits AChE and SERT in the brains of mice (AChE ED₅₀ = 13 mg/kg; SERT ED₅₀ = 2.4 mg/kg) and rats (AChE ED₅₀ = 43 mg/kg) respectively^[1][2].
BGC-201259 (64 mg/kg, p.o., single dose) simultaneously enhances cholinergic and serotonergic neurotransmission in the living rat brain^[1][2].
BGC-201259 (4-16 mg/kg, p.o., single dose) significantly enhances the locomotor activity induced by 5-HTP and exhibits antidepressant-like activity in mice^[1][2].
BGC-201259 (0.5-1 mg/kg, p.o., single dose) significantly improves the spatial short-term memory impairment in aged rats^[1][2].
BGC-201259 (1-4 mg/kg, p.o., single dose) dose-dependently increases the period of wakefulness and reduce sleep in rats^[1][2].