SB-334867 hydrochloride

- Overview
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    Background
    
    SB-334867 is a selective antagonist of orexin-1 receptor [1].
    Orexin-A and orexin-B are two peptides isolated from rat hypothalamus. They are involved in some physiological functions such as the control of feeding, energy metabolism and regulation of the sleep-wake cycle. SB-334867 can inhibit the orexin-A and orexin-B induced calcium responses in CHO-OX1 cells with pKB values of 7.27 and 7.23, respectively. SB-334867 is more selective for OX1 receptor over OX2 receptor. It causes 32.7% and 22% inhibition of orexin-A and orexin-B induced calcium responses in CHO-OX2 cells, respectively. Moreover, SB-334867 is found to reduce both orexin-A-induced and fasting-induced food intake. The acute anorectic effect of it is associated with signi®cant reductions in all active behaviours [1, 2].
    
    [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.
- Properties
  - Categories
    
    Orexin-1 receptor antagonist
    
    Alternative Name
    
    1-(2-methylbenzo[d]oxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea hydrochloride
    
    CAS Number
    
    249889-64-3
    
    Molecular Formula
    
    C17H14ClN5O2
    
    Molecular Weight
    
    355.78
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥2.72 mg/mL in EtOH with ultrasonic; ≥5.2 mg/mL in DMSO with gentle warming
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    O=C(NC1=CC=NC2=CC=CN=C12)NC3=CC=C4N=C(C)OC4=C3.Cl
    
    * For Research Use Only