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SB-334867 hydrochloride has excellent selectivity for the orexin-1 receptor, blood-brain barrier permeability and shows in vivo activity following ip dosing. SB-334867-A HCl is a non-peptide OX(1) selective receptor antagonist. PKb values are 7.2 and < 5 for inhibition of intracellular Ca2+ release in CHO cells expressing human OX1 and OX2 receptors respectively. SB-334867 hydrochloride blocks orexin-A induced grooming and feeding following systemic administration in vivo. SB-334867-A (OX1, pKB = 7.4; OX2, pKB = 5.7), devoid of appreciable affinity for either 5-HT2B (pKi < 5.3) or 5-HT2C (pKi < 5.4) receptors, provides the first definitive evidence that a central behavioural effect of orexin-A (grooming) is mediated by OX1 receptors.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | Male and female Sprague–Dawley rats |
| Formulation | 10% (w/v) Encapsin in sterile water |
| Dosages | 30 mg/kg |
| Administration | i.p. |
| Molecular Weight | 355.78 |
| Formula | C17H14ClN5O2 |
| CAS Number | 249889-64-3 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Smart D, et al. Br J Pharmacol. SB-334867-A: the first selective orexin-1 receptor antagonist.
| Related OX Receptor Products |
|---|
| MK-6096
MK-6096 is an orally bioavailable potent and selective reversible antagonist of OX(1)R and OX(2)R. |
| Almorexant
Almorexant is a competitive OX1 and OX2 orexin receptor antagonist with IC50 of 13 and 8 nM, respectively. |
| SB408124
SB408124 (Tocris-1963) is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and27 nM in both whole cell and membrane, respectively, exhibits 50-fold selectivity over OX2 receptor. |
| MK-3697
MK-3697 is an isonicotinamide small molecule, acting as a potent and selective Orexin 2 receptor antagonist with Ki = 0.95 nM. |
| TCS-1102
TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively). |
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