SB-334867 - CAS 249889-64-3
SB-334867(cas 249889-64-3) is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2. SB-334867 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). 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. 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). 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.
Catalog Number: I002847
CAS Number: 249889-64-3
PubChem Substance ID:355039650
Molecular Formula: C17H14ClN5O2
Molecular Weight:355.78
Purity: ≥95%
* For research use only. Not for human or veterinary use.
Synonym
Synonyms | SB-334867; SB 334867; SB334867;1-(2-methyl-1,3-benzoxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea |
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Property
Molecular Formula: | C17H14ClN5O2 |
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Molecular Weight | 355.78 |
Target: | OX Receptor |
Solubility | 10 mM in DMSO |
Purity | ≥95% |
Storage | Store at -20°C |
Overview of Clinical Research | Originator: GlaxoSmithKline<br /> Class: Benzoxazoles; Obesity therapies; Urea compounds<br /> Mechanism of Action: Orexin receptor antagonists<br /> Orphan Drug Status: No<br /> |
IC50 | 7.2 (pKb) |