| Description: |
SB-334867 is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.
IC50 value: 7.2 (pKb)
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) .
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 . 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 .For the detailed information of SB-334867, the solubility of SB-334867 in water, the solubility of SB-334867 in DMSO, the solubility of SB-334867 in PBS buffer, the animal experiment (test) of SB-334867, the cell expriment (test) of SB-334867, the in vivo, in vitro and clinical trial test of SB-334867, the EC50, IC50,and Affinity of SB-334867, Please contact DC Chemicals. |
