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N-(2-Methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl urea

Product NameN-(2-Methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl urea
CAS249889-64-3
MFC17H13N5O2
MW319.32
EINECS604-604-1
MOL File249889-64-3.mol

Chemical Properties

Melting point	>235°C (dec.)
storage temp.	Desiccate at RT
solubility	Dichloromethane (Slightly), DMSO (Slightly)
form	Solid
color	White

Usage And Synthesis

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 .

in vivo

SB-334867 (intraperitoneal injection; 20 mg/kg; 20 days) administers 15 min before morphine injection can significantly decrease the effect of the morphine challenge dose in mice in comparison with the sporadically morphine-treated group^[2].SB334867 (intraperitoneal injection; 3, 10 and 30 mg/kg) significantly reduces ethanol intake relative to vehicle and does not effect water consumption in female P rats^[3].SB334867 (intraperitoneal injection; 3, 10 and 30 mg/kg) reduces ethanol consumption at the 30 mg/kg dose, high dose suppresses sucrose intake relative to vehicle, and it results in lower blood ethanol concentrations (BECs) relative to both the 10 and 30 mg/kg doses^[3].

Animal Model:	Male Swiss mice^[2]
Dosage:	20mg/kg
Administration:	Intraperitoneal injection
Result:	Inhibited the acquisition of morphine-induced sensitization to locomotor activity of mice.

Animal Model:	C57BL/6J Mice^[3]
Dosage:	3, 10 and 30 mg/kg
Administration:	Intraperitoneal injection
Result:	Reduced ethanol consumption, BECs and suppressed sucrose intake in mice.

IC 50

OX1

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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