UCPH-101

UCPH-101 is a noncompetitive inhibitor of excitatory amino acid transporter 1 (EAAT1), which takes up extracellular glutamate in the central nervous system.^1,2 UCPH-1 is selective for EAAT1 over EAAT2 and EAAT3 with IC₅₀ values of 0.66, >300, and >300 µM, respectively, in a radioligand uptake assay using HEK293 cells transfected with the human transporter.³ It selectively inhibits anion currents in tsA201 cells expressing human EAAT1 (K_d = 0.34 µM) over rat EAAT4 and mouse EAAT5 at concentrations up to 10 µM.² UCPH-101 is orally bioavailable in rats at a dose of 10 mg/kg but does not cross the blood-brain barrier.¹

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1. Erichsen, M.N., Huynh, T.H.V., Abrahamsen, B., et al. Structure-activity relationship study of first selective inhibitor of excitatory amino acid transporter subtype 1: 2-Amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101). J. Med. Chem. 53(19), 7180-7191 (2010).

2. Abrahamsen, B., Schneider, N., Erichsen, M.N., et al. Allosteric modulation of an excitatory amino acid transporter: The subtype-selective inhibitor UCPH-101 exerts sustained inhibition of EAAT1 through an intramonomeric site in the trimerization domain. J. Neurosci. 33(3), 1068-1087 (2013).

3. Jensen, A.A., Erichsen, M.N., Nielsen, C.W., et al. Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1. J. Med. Chem. 52(4), 912-915 (2009).