BGC-201259  (Synonyms: RS-1259)

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].

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].

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

862.88

C₄₂H₅₀N₆O₁₄

444667-97-4

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• [1]. Abe Y, et al. Pharmacological characterization of RS-1259, an orally active dual inhibitor of acetylcholinesterase and serotonin transporter, in rodents: possible treatment of Alzheimer's disease. J Pharmacol Sci. 2003 Sep;93(1):95-105.  [Content Brief]

  [2]. Toda N, Kaneko T, Kogen H. Development of an efficient therapeutic agent for Alzheimer's disease: design and synthesis of dual inhibitors of acetylcholinesterase and serotonin transporter. Chem Pharm Bull (Tokyo). 2010 Mar;58(3):273-87.  [Content Brief]