Orexin B, human (TFA) is an endogenous agonist at Orexin receptor with Kis of 420 and 36 nM for OX1 and OX2, respectively.
IC50&Target
Ki: 420 nM (OX1), 36 nM (OX2).
体外研究
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 IC50 of 36 nM in the binding assay and an EC50 of 60 nM in the [Ca]i transient assay. Human Orexin B has significantly lower affinity for the human OX1: the calculated IC50 in the competitive binding assay and the EC50 in the [Ca]i transient assay are 420 nM and 2500 nM for human orexin-B, respectively.
体内研究
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.
Animal Model:
Male Wistar rats (180-200 g).
Dosage:
3 nM and 30 nM.
Administration:
Administered in a 5 mL bolus through a catheter placed in the left lateral ventricle in early light phase.
Result:
Significantly augmented food intake.
运输条件
Room temperature in continental US; may vary elsewhere.