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792173-99-0

792173-99-0 structure
792173-99-0 structure
  • Name: SB 334867
  • Chemical Name: 1-(2-Methyl-1,3-benzoxazol-6-yl)-1-(1,5-naphthyridin-4-yl)urea
  • CAS Number: 792173-99-0
  • Molecular Formula: C17H13N5O2
  • Molecular Weight: 319.317
  • Catalog: Biochemical Inhibitor G protein coupled receptor(GPCR & G Protein) OX Receptor Antagonist
  • Create Date: 2018-01-04 07:59:46
  • Modify Date: 2025-08-26 06:32:09
  • 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.

Name 1-(2-Methyl-1,3-benzoxazol-6-yl)-1-(1,5-naphthyridin-4-yl)urea
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.
Related Catalog
References

[1]. Smart D, et al. SB-334867-A: the first selective orexin-1 receptor antagonist. Br J Pharmacol. 2001 Mar;132(6):1179-82.

[2]. Rasmussen K, et al. The orexin-1 receptor antagonist SB-334867 blocks the effects of antipsychotics on the activity of A9 and A10 dopamine neurons: implications for antipsychotic therapy. Neuropsychopharmacology. 2007 Apr;32(4):786-92.

[3]. Azhdari-Zarmehri H, et al. Orexin receptor type-1 antagonist SB-334867 decreases morphine-induced antinociceptive effect in formalin test. Pharmacol Biochem Behav. 2013 Nov;112:64-70.

[4]. Rodgers RJ, et al. SB-334867, a selective orexin-1 receptor antagonist, enhances behavioural satiety and blocks the hyperphagic effect of orexin-A in rats. Eur J Neurosci. 2001 Apr;13(7):1444-52.

Density 1.4±0.1 g/cm3
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℃
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H315
RIDADR NONH for all modes of transport
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