Uses
SB 334867 is an orexin 1 receptor antagonist.
Definition
ChEBI: 1-(2-methyl-1,3-benzoxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea is a naphthyridine derivative.
Biological Activity
sb-334867 free base is a selective antagonist of orexin-1 receptor [1].orexin-a and orexin-b are two peptides isolated from rat hypothalamus. they are involved in some physiological functions such as the control of feeding, energy metabolism and regulation of the sleep-wake cycle.sb-334867 free base could inhibit the orexin-a and orexin-b induced calcium responses in cho-ox1 cells with pkb values of 7.27 and 7.23, respectively. sb-334867 was more selective for ox1 receptor over ox2 receptor. it caused 32.7% and 22% inhibition of orexin-a and orexin-b induced calcium responses in cho-ox2 cells, respectively. moreover, sb-334867 was found to reduce both orexin-a-induced and fasting-induced food intake. the acute anorectic effect of it was associated with significant reductions in all active behaviours [1, 2].
Biochem/physiol Actions
Lateral hypothalamic orexin neuron activation leads to the development of morphine conditioned place preference, which is preferably blocked by SB-334867.
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.
