N-(2-METHYL-6-BENZOXAZOLYL)-N'-1,5-NAPHTHYRIDIN-4-YL UREA

Uses

SB 334867 is an orexin-1-receptor antagonist. An important ligand for the study of the orexin 1 (OX1) receptor due to its high OX1/OX2 selectivity and bioavailability.

Definition

ChEBI: 1-(2-methyl-1,3-benzoxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea is a naphthyridine derivative.

Biological Activity

Selective non-peptide orexin OX 1 receptor antagonist. pK b values are 7.2 and < 5 for inhibition of intracellular Ca 2+ release in CHO cells expressing human OX 1 and OX 2 receptors respectively. Blocks orexin-A induced grooming and feeding following systemic administration in vivo .

References

[1] smart d, sabido-david c, brough s j, et al. sb-334867-a: the first selective orexin-1 receptor antagonist. british journal of pharmacology, 2001, 132(6): 1179-1182.
[2] rodgers r j, halford j c g, nunes de souza r l, et al. sb-334867, a selective orexin-1 receptor antagonist, enhances behavioural satiety and blocks the hyperphagic effect of orexin-a in rats. european journal of neuroscience, 2001, 13(7): 1444-1452.