TABLE 1

[3H]Almorexant and [3H]Cp-1 binding properties at hOX1 and hOX2 and [3H]SB-674042 binding at hOX1

Saturation binding isotherms of [3H]almorexant, [3H]Cp-1, and [3H]SB-674042 were performed on membrane preparations from HEK293 cells transiently transfected with hOX1 or hOX2 as described under Materials and Methods. The Kd and Bmax values are mean ± S.E., calculated from three independent experiments (each performed in triplicate).

Radioligand and Receptor KdBmax
nM pmol / mg protein
[3H]Almorexant (37°C)
    hOX1 1.3 ± 0.1 27.2 ± 0.6
    hOX2 0.17 ± 0.01 15.72 ± 0.2
[3H]Cp-1 (37°C)
    hOX1 17.52 ± 1.3 29.83 ± 0.7
    hOX2 0.40 ± 0.04 18.64 ± 0.5
[3H]SB-674042 (23°C)
    hOX1 0.74 ± 0.07 13.76 ± 0.38