N-(2-METHYL-6-BENZOXAZOLYL)-N'-1,5-NAPHTHYRIDIN-4-YL UREA
N-(2-METHYL-6-BENZOXAZOLYL)-N'-1,5-NAPHTHYRIDIN-4-YL UREA Basic information
- Product Name:
- N-(2-METHYL-6-BENZOXAZOLYL)-N'-1,5-NAPHTHYRIDIN-4-YL UREA
- Synonyms:
-
- N-(2-METHYL-6-BENZOXAZOLYL)-N'-1,5-NAPHTHYRIDIN-4-YL UREA
- SB 334867
- SB 334867 hydrochloride NEW
- Zinc00008794
- Urea, N-(2-Methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl-, (Hydrochloride)
- SB334867 HCl
- SB-334867 hydrochloride
- CS-1473
- CAS:
- 249889-64-3
- MF:
- C17H13N5O2
- MW:
- 319.32
- EINECS:
- 604-604-1
- Product Categories:
-
- Orexin receptor
- Mol File:
- 249889-64-3.mol
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: | 20?mg/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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