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| | N-(2-Methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl urea Basic information |
| | N-(2-Methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl urea Chemical Properties |
| Melting point | >235°C (dec.) | | storage temp. | Desiccate at RT | | solubility | Dichloromethane (Slightly), DMSO (Slightly) | | form | Solid | | color | White |
| | N-(2-Methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl urea 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. |
| | N-(2-Methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl urea Preparation Products And Raw materials |
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