TABLE 2

Ki values and Schild slope values of lemborexant when competing against three orexin peptide agonists on human and mouse OX1R and OX2R in a cell-based functional reporter assay

Data represent the mean ± S.E.M.

hOX1RmOX1RhOX2RmOX2R
Ki (10−9 mol/l)
 OXA14.1 ± 3.116.3 ± 4.00.39 ± 0.080.37 ± 0.07
 OXBN.D.N.D.0.58 ± 0.130.28 ± 0.08
 [Ala11,D-Leu15]-OXBN.D.N.D.0.42 ± 0.050.49 ± 0.05
Schild Slope
 OXA1.08 ± 0.050.95 ± 0.051.00 ± 0.021.00 ± 0.03
 OXBN.D.N.D.0.93 ± 0.020.99 ± 0.03
 [Ala11,D-Leu15]-OXBN.D.N.D.1.01 ± 0.011.03 ± 0.02

  • mOX1R, mouse OX1R; N.D., not determined.