Name | 1-(2-Methyl-1,3-benzoxazol-6-yl)-1-(1,5-naphthyridin-4-yl)urea |
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Synonyms |
1-(2-Methyl-1,3-benzoxazol-6-yl)-1-(1,5-naphthyridin-4-yl)urea
Urea, N-(2-methyl-6-benzoxazolyl)-N-1,5-naphthyridin-4-yl- N-(2-methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl 1-(2-methylbenzo[d]oxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea SB-334867 |
Description | SB-334867 free base is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.IC50 value: 7.2 (pKb) [1]Target: orexin OX1 receptor in vitro: SB-334867-A inhibited the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses (pK(B)=7.27+/-0.04 and 7.23+/-0.03 respectively, n=8), but had no effect on the UTP (3 microM)-induced calcium response in CHO-OX(1) cells. SB-334867-A (10 microM) also inhibited OX(2) mediated calcium responses (32.7+/-1.9% versus orexin-A) [1].in vivo: Single-unit recordings in anesthetized rats demonstrated the central effects of the selective orexin-1 receptor antagonist SB-334867 (2 mg/kg, intravenous), as it reversed the excitatory effects of orexin-A administration (6 microg, intracerebroventricular) on the activity of locus coeruleus (LC) cells [2]. The ICV injection of SB-334867 alone had no effect on the formalin-induced nociceptive behaviors. Pre-treatment with SB-334867 at a dose of 0.5 nmol significantly attenuated the analgesia induced by morphine (at dose 1.5mg/kg of morphine; interphase and phase 2B and at dose 3mg/kg of morphine just phase 2B of formalin test) [3]. Administered alone, SB-334867 (30 mg/kg, but not lower doses) significantly reduced food intake and most active behaviours (eating, grooming, sniffing, locomotion and rearing), while increasing resting. Pretreatment with SB-334867 dose-dependently blocked these effects of orexin-A, with significant antagonism evident at dose levels (3-10 mg/kg) below those required to produce intrinsic behavioural effects under present test conditions in rats [4].Toxicity: Acute systemic treatment with the selective orexin-1 (OX1R) antagonist SB-334867 reduces food intake in rats, an effect associated with an acceleration in behavioural satiety and unrelated to gross behavioural disruption, alterations in palatability, or toxicity. |
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Related Catalog | |
References |
Density | 1.4±0.1 g/cm3 |
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Boiling Point | 549.5±58.0 °C at 760 mmHg |
Molecular Formula | C17H13N5O2 |
Molecular Weight | 319.317 |
Flash Point | 286.1±32.3 °C |
Exact Mass | 319.106934 |
LogP | 0.51 |
Vapour Pressure | 0.0±1.5 mmHg at 25°C |
Index of Refraction | 1.757 |
Storage condition | -20℃ |