202801-92-1

Ki: 420 nM (OX1), 36 nM (OX2)

Orexin B is derived by proteolytic amino acid precursor, prepro-orexin, which is encoded by a gene localized to chromosome 17q21 in humans. In radioligand binding studies, Orexin B has a higher affinity for the OX2 receptor. Human Orexin B has two amino acid substitutions when compared with the rodent sequence. OX2 receptor is indeed a high-affinity receptor for human orexin B, with an IC ₅₀ of 36 nM in the binding assay and an EC ₅₀ of 60 nM in the [Ca ²⁺ ]i transient assay. Human Orexin B has significantly lower affinity for the human OX1: the calculated IC ₅₀ in the competitive binding assay and the EC ₅₀ in the [Ca ²⁺ ]i transient assay are 420 nM and 2500 nM for human orexin-B, respectively.

Human Orexin B significantly augments food intake; at the 2 hr time point, 5- and 12-fold stimulation of food consumption is observed by 3 nM and 30 nM orexin-B, respectively.