N-(2-METHYL-6-BENZOOXAZOLYL)-N''-1,5-NAPHTHYRIDIN-4-YL UREA Chemical Properties

Boiling point:

450.5±30.0 °C(Predicted)

Density 

1.472

storage temp. 

room temp

solubility 

insoluble in H2O; insoluble in EtOH; ≥14.55 mg/mL in DMSO

pka

10.21±0.43(Predicted)

form 

powder

color 

white to beige

CAS DataBase Reference

792173-99-0

N-(2-METHYL-6-BENZOOXAZOLYL)-N''-1,5-NAPHTHYRIDIN-4-YL UREA Usage And Synthesis

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.

storage

Room temperature (desiccate)

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.

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