| Description | SB-334867 free base (SB334867A free base) is a selective orexin-1 (OX1) receptor antagonist. |
| In vitro | 在CHO-OX1细胞中，SB-334867抑制了orexin-A（10 nM）和orexin-B（100 nM）引发的钙反应，其pKB分别为7.27和7.23，对UTP（3 microM）引发的钙反应无影响。[1] |
| In vivo | 在雄性和雌性大鼠中，SB-334867（30 mg/kg，i.p.）显著减少自然和orexin-A诱导的食物摄入。[2] SB-334867（2 mg/kg，i.v.）阻断抗精神病化合物对大鼠多巴胺神经活动的影响。[3] SB-334867还抑制大鼠对吗啡止痛耐受性的发展。[4] |
| Target activity | OXA:10 nM, OXB:100 nM |
| Synonyms | SB334867A free base, SB-334867, SB 334867, SB334867 |
| molecular weight | 319.32 |
| Molecular formula | C17H13N5O2 |
| CAS | 792173-99-0 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: 3.2 mg/mL (10 mM)), Heating is recommended. DMSO: 31.9 mg/mL (100 mM), Heating is recommended. |
| References | 1. Smart D, et al. Br J Pharmacol. 2001, 132(6), 1179-1182. 2. Haynes AC, et al. Regul Pept. 2000, 96(1-2), 45-51. 3. Rasmussen K, et al. Neuropsychopharmacology. 2007, 32(4), 786-792. 4. Ranjbar-Slamloo Y, et al. Peptides. 2012, 35(1), 56-59. |