BGC-201259 (RS-1259) is an orally active inhibitor that simultaneously targets acetylcholinesterase ( AChE ) ( IC 50 = 101 nM) and serotonin transporter ( SERT ) ( IC 50 = 42 nM). BGC-201259 inhibits 5-HT receptor with an IC 50 of 90 nM. BGC-201259 exhibits strong weak activity against the NA transporter ( IC 50 = 7.7 μM), L-type calcium channel ( IC 50 = 3.6 μM), σ receptor ( IC 50 = 2 μM), and sodium channel ( IC 50 = 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.
Products | Products > Disease Areas > Neurological, Eye or Ear Disease | Products > Signaling Pathways > Neuronal Signaling | Products > Signaling Pathways > GPCR/G Protein | Products > Signaling Pathways > Membrane Transporter/Ion Channel | Products > Research Areas > Neurological Disease | Products > Signaling Pathways > Sigma Receptor | Products > Signaling Pathways > Cholinesterase (ChE) | Products > Signaling Pathways > Serotonin Transporter | Products > Signaling Pathways > 5-HT Receptor | Products > Signaling Pathways > Calcium Channel | Products > Signaling Pathways > Sodium Channel
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