产品描述:
SB-408124 is a potent antagonist of orexin 1 receptors (OX1Rs) with a Ki value of 26.9 nM in a calcium mobilization assay using CHO cells that stably express human OX1R.{34091} It is selective for OX1R over OX2R, with Kd values of 21.7 and 1,704 nM, respectively, in a radioligand binding assay. In vivo co-perfusion of SB-408124 with human OX1R in the rat ventral tegmental area inhibits OX1R-induced glutamate and dopamine elevations and reduces cocaine-seeking behavior in rats.{36123}